1,759 results match your criteria Anticancer Agents Med Chem[Journal]


LHRH Targeted Chonderosomes of Mitomycin C In Breast Cancer: An In Vitro / In Vivo Study.

Anticancer Agents Med Chem 2019 Apr 15. Epub 2019 Apr 15.

Department of Biochemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan. Iran.

Background: Mitomycin C (MMC) is an anti-cancer drug used for treatment of breast cancer with limited therapeutic index, extreme gastric adverse effects and bone marrow suppression. The purpose of the present study was preparation of a dual targeted delivery system of MMC for targeting CD44 and LHRH overexpressed receptors of breast cancer.

Methods: MMC loaded LHRH targeted chonderosome were prepared by precipitation method and were characterized for their physicochemical properties. Read More

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http://dx.doi.org/10.2174/1871520619666190415165849DOI Listing

The Opposite Effect of L-kynurenine and Ahr Inhibitor Ch223191 on Apoptotic Protein Expression in Pancreatic Carcinoma Cells (Panc-1).

Anticancer Agents Med Chem 2019 Apr 15. Epub 2019 Apr 15.

Department of Medical Physiology, Faculty of Health Sciences, Jagiellonian Medical College, Krakow. Poland.

Background: L-kynurenine, derivate of L-tryptophan, is synthetized by indoleamine 2,3-dioxygenase (IDO). The effects of L-kynurenine depend on its binding to an aryl hydrocarbon receptor (AhR).

Objective: The aim of this study was to investigate the changes within the apoptotic pathway in PANC-1 cells subjected to L-kynurenine or L-tryptophan considering the production of anti-apoptotic proteins from the IAPs and Bcl-2 family, as well as the regulation of NF-κB signaling. Read More

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http://dx.doi.org/10.2174/1871520619666190415165212DOI Listing
April 2019
1 Read

Recent Developments of Nanoparticles In The Treatment Of Photodynamic Therapy For Cervical Cancer.

Authors:
Guan Jiang

Anticancer Agents Med Chem 2019 Apr 11. Epub 2019 Apr 11.

Department of Dermatology, Affiliated Hospital of Xuzhou Medical University, Xuzhou 221002. China.

Photodynamic therapy (PDT) is a photoactivation or photosensitization process, wherein the photosensitizer (PS) is activated under appropriate wavelengths. Conventional antitumor therapy for cervical cancer includes surgery, radiotherapy, and chemotherapy. However, these techniques are accompanied by some evident shortcomings. Read More

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http://dx.doi.org/10.2174/1871520619666190411121953DOI Listing
April 2019
4 Reads

Approach For Treatment of Liver Cancer By Novel Glycyrrhizin Derivative.

Anticancer Agents Med Chem 2019 Apr 11. Epub 2019 Apr 11.

Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura 35516. Egypt.

Background: Liver cancer is a life threating disease as it occupies the fifth most common cancers from incidences and the third cause of death worldwide and with no available safe, efficient, economic drug for treatment.

Methods: Therefore, this study intended to investigate different glycyrrhizin and their derivatives for possible use as a cytotoxic agent and as a possible drug for liver cancer treatment. Thus, after treatment against liver cancer cell line HepG-2 with 50 µM of each compounds cell viability was determined. Read More

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http://dx.doi.org/10.2174/1871520619666190411114718DOI Listing

Unfolded Protein Response is Involved in Trans-Platinum (II) Complex-Induced Apoptosis in Prostate Cancer Cells via ROS Accumulation.

Anticancer Agents Med Chem 2019 Apr 8. Epub 2019 Apr 8.

Department of Medical Biochemistry, Faculty of Medical School, Istinye University, Istanbul. Turkey.

Background: Prostate cancer is one of the most common cancer types and it is the sixth leading cause of cancer-related death in men worldwide. Even though novel treatment modalities have been developed, it still a life threatening disease. Therefore novel compounds are needed to improve the overall survival. Read More

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http://www.eurekaselect.com/171460/article
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http://dx.doi.org/10.2174/1871520619666190409103334DOI Listing
April 2019
2 Reads

Transcriptome Analysis of mRNA in Uterine Leiomyoma Using Next-Generation RNA Sequencing.

Anticancer Agents Med Chem 2019 Apr 8. Epub 2019 Apr 8.

Department of Biotechnology, School of Chemical and Life Sciences, Jamia Hamdard, New Delhi, 110062. India.

Background: Uterine leiomyoma is a benign smooth muscle tumor of monoclonal nature in female reproductive tract and is one of the major health problems. More than 70% of female population suffers from uterine leiomyoma in their lifetime and in advanced condition it is associated with pregnancy complications and infertility.

Objective: Characterization and relative expression of mRNA transcripts through transcriptome profiling in uterine leiomyoma and adjacent myometrium. Read More

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http://dx.doi.org/10.2174/1871520619666190409102855DOI Listing
April 2019
2 Reads

Garlic and its Active Compounds: A Potential Candidate in The Prevention of Cancer by Modulating Various Cell Signalling Pathways.

Anticancer Agents Med Chem 2019 Apr 8. Epub 2019 Apr 8.

Department of Medical Laboratories, College of Applied Medical Sciences, Qassim University, Buraidah. Saudi Arabia.

Background: Cancer is a multi-factorial disease including alterations in the cell signalling pathways. Currently, several drugs are in use to treat the cancer but such drugs show negative side effects on normal cells and causes severe toxicity.

Methods: The current research is mainly focused on medicinal plants with potential therapeutic efficacy in the treatment of cancer without any adverse effects on normal cells. Read More

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http://dx.doi.org/10.2174/1871520619666190409100955DOI Listing
April 2019
3 Reads

Evaluation of Antitumor Activity and Hepatoprotective Effect of Mitomycin C Solubilized in Chamomile Oil Nanoemulsion.

Anticancer Agents Med Chem 2019 04 8. Epub 2019 Apr 8.

Department of Clinical Biochemistry, Faculty of Medicine, King Abdulaziz University, Jeddah. Saudi Arabia.

Purpose: The present study aimed to investigate the antitumor activity and hepatoprotective effect of the MTC, when combined with CHAM oil nanoemulsion (NE), (CHAM-MTC) on the tumor growth.

Materials/methods: The in vitro study has assessed the antineoplastic effect of CHAM-MTC on the MCF-7 breast cancer cells while the in vivo therapeutic effectiveness and toxicities of CHAM-MTC were evaluated in Ehrlich ascites carcinoma (EAC) bearing mice. One hundred female Swiss albino mice, divided equally into non-EAC group (negative control), untreated EAC group (positive control) and three EAC groups received once intraperitoneal injection of 0. Read More

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http://dx.doi.org/10.2174/1871520619666190408114732DOI Listing
April 2019
2 Reads

The Emerging Role of CSN6 in Biological Behavior and Cancer Progress.

Anticancer Agents Med Chem 2019 Apr 8. Epub 2019 Apr 8.

Laboratory of Clinical and Experimental Pathology, Xuzhou Medical University, 209 Tong-shan Road, Xuzhou 221004, Jiangsu. China.

Background: The constitutive photomorphogenesis 9 (COP9) signalosome (CSN) subunit 6 (CSN6) noticeably acts as a regulator of the degradation of cancer-related proteins, which contributes to cancerogenesis. The aims of this paper are to expound the research advances of CSN6, particularly focusing on roles of CSN6 in the regulation of biological behavior and cancer progress.

Methods: Literatures from PubMed and Web of Science databases about biological characteristics and application of CSN6 published in recent years were collected to make a review. Read More

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http://dx.doi.org/10.2174/1871520619666190408142131DOI Listing
April 2019
2.469 Impact Factor

Novel Thiazine Substituted 9-Anilinoacridines: Synthesis, Antitumour activity and Structure-Activity Relationships.

Anticancer Agents Med Chem 2019 Apr 8. Epub 2019 Apr 8.

Department of Pharmaceutical Chemistry, JSS College of Pharmacy, ( Constituent college of JSS Academy of Higher Education & Research, Deemed University) Udhagamandalam - 643001 (Tamilnadu). India.

9-anilinoacridines are acting as DNA-intercalating agents which plays an important role as antitumor drugs, due to their anti-proliferative properties. Some anticancer agents contain 9-anilinoacridines such as amsacrine (m-AMSA), and nitracrine (Ledakrine) have been already developed. In this study, novel 9-anilinoacridines substituted with thiazines 4a-r were designed, synthesized, characterized by physical and spectral data and their cytotoxic activities against DLA cell lines were evaluated. Read More

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http://dx.doi.org/10.2174/1871520619666190408134224DOI Listing
April 2019
1 Read

Dual Anti-cancer and Anti-Itch Activity of PD176252 Analogues: Design, Synthesis and Biological Evaluation.

Anticancer Agents Med Chem 2019 Apr 8. Epub 2019 Apr 8.

School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009. China.

Background: Cancer patients that treated with targeted anti-cancer drug suffered itch or pruritus. Itch or pruritus is an unpleasant sensation that brings about a negative impact on quality of life, and serious itch may lead to dose reduction and even discontinuation. Gastrin releasing peptide receptor (GRPR) plays a critical role in itch, inflammation and caner, and GRPR antagonist has obvious effect on anti-cancer, anti-inflammation and anti-itch. Read More

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http://dx.doi.org/10.2174/1871520619666190408133141DOI Listing
April 2019
4 Reads

Synthesis of 5-Alknyltetrandrine Derivatives and Evaluation of Their Anticancer Activity on A549 Cell Lines.

Anticancer Agents Med Chem 2019 Apr 8. Epub 2019 Apr 8.

School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001. China.

Background: Lung cancer is one of the most prevalent malignancies and thus the development of novel therapeutic agents for managing lung cancer is imperative. Tetrandrine, a bis-benzyltetrahydroisoquinoline alkaloid isolated from Stephania tetrandra S. Moore, has been found to exert cytotoxic effects on cancerous cells. Read More

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http://dx.doi.org/10.2174/1871520619666190408132249DOI Listing
April 2019
1 Read

Novel Curcumin Inspired Antineoplastic 1-Sulfonyl-4-Piperidones: Design, Synthesis and Molecular Modeling Studies.

Anticancer Agents Med Chem 2019 Apr 8. Epub 2019 Apr 8.

Department of Pesticide Chemistry, National Research Centre, Dokki, Giza 12622. Egypt.

Background: Curcumin is a well known example of plant origin exhibiting promising diverse biological properties of which anti-inflammatory and antitumor and poor pharmacokinetic/pharmacodynamic properties. This is why effective agents based on its chemical scaffold were explored.

Methods: A set of 3,5-bis(ylidene)-1-(alkylsulfonyl)piperidin-4-ones were synthesized in excellent yield (80‒96%) through dehydrohalogenation reaction of 3,5-bis(ylidene)-4-piperidinones with the corresponding alkane sulfonyl chloride in the presence of triethylamine. Read More

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http://dx.doi.org/10.2174/1871520619666190408131639DOI Listing
April 2019
1 Read

Anti-Metastatic Drug Developments, Biomedical Mechanisms and Therapeutic Categorization.

Anticancer Agents Med Chem 2019 Apr 8. Epub 2019 Apr 8.

University of California at San Diego, CA. United States.

Neoplasm metastasis, a multi-step and multi-level pathological feature is resistant to most available anticancer drugs and formed therapeutic strategies in the clinic. 90% of cancer deaths are caused by neoplasm metastasis due to wide-spread of therapeutic failures in the clinic. Different drug mechanisms and development strategies (>15 categories) are introduced in this Article. Read More

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http://dx.doi.org/10.2174/1871520619666190408130831DOI Listing
April 2019
2.469 Impact Factor

Effects of Resveratrol, Berberine, and Their Combinations on Reactive Oxygen Species, Survival, and Apoptosis in Human Squamous Carcinoma (SCC-25) Cells.

Anticancer Agents Med Chem 2019 Apr 5. Epub 2019 Apr 5.

Department of Conservative Dentistry with Endodontics, Medical University of Silesia, Pl. Akademicki 17, 41-902 Bytom. Poland.

Background: Levels of cellular Reactive Oxygen Species (ROS) influence the oxidized/reduced states of cellular proteins, and create redox-signaling pathways that can activate transcription factors, kinases, and phosphatases. ROS levels can be increased radically by external factors, including ionizing and UV radiation or exposure to chemical compounds. These increased ROS levels can in turn lead to oxidative damage of DNA. Read More

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http://dx.doi.org/10.2174/1871520619666190405111151DOI Listing
April 2019
2 Reads

Turning to Computer-Aided Drug Design in the treatment of Diffuse Large B-cell Lymphoma: Has it been helpful?

Anticancer Agents Med Chem 2019 Apr 5. Epub 2019 Apr 5.

Molecular Bio-computation and Drug Design Laboratory, School of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4001. South Africa.

Introduction: Amidst the numerous effective therapeutic options available for the treatment of Diffuse large B-cell lymphoma (DLBCL), about 30-40% of patients treated with first-line chemoimmunotherapy still experience relapse or refractory DLBCL. This has necessitated a continuous search for new therapeutic agents to augment the existing therapeutic arsenal. The dawn of computer-aided drug design (CADD) in the drug discovery process has accounted for a persistency in the application of computational approaches either alone or in combinatorial strategies with experimental methods towards the identification of potential hit compounds with high therapeutic efficacy in abrogating DLBCL. Read More

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http://dx.doi.org/10.2174/1871520619666190405111526DOI Listing
April 2019
9 Reads
2.469 Impact Factor

Punicic Acid Inhibits Glioblastoma Migration and Proliferation Via the PI3K/AKT1/mTOR Signaling Pathway.

Anticancer Agents Med Chem 2019 Apr 5. Epub 2019 Apr 5.

Celal Bayar University School of Medicine Histology-Embryology Department. Turkey.

Background: Punicic acid (PA) is a polyunsaturated fatty acid that accounts for approximately 70%-80% of pomegranate seed oil (PSO). PA possess strong antioxidant, anti-inflammatory, anti-atherogenic effects, and anti-tumorigenic properties. Pomegranate extracts have been shown to have anticancer activity in many studies. Read More

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http://dx.doi.org/10.2174/1871520619666190405112507DOI Listing
April 2019
1 Read
2.469 Impact Factor

Influence of New Synthetic Xanthones on the Proliferation and Migration Potential of Cancer Cell Lines in Vitro.

Anticancer Agents Med Chem 2019 Apr 5. Epub 2019 Apr 5.

Department of Biotechnology and Genetic Engineering, Medical University of Silesia, 8 Jedności Str., 41-200 Sosnowiec. Poland.

Background: Natural plant metabolites and their semisynthetic derivatives have been used for years in cancer therapy. Xanthones are oxygenated heterocyclic compounds produced as secondary metabolites by higher plants, fungi or lichens. Xanthone core may serve as a template in the synthesis of many derivatives that have broad biological activities. Read More

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http://dx.doi.org/10.2174/1871520619666190405113519DOI Listing
April 2019
3 Reads

Synthesis of New Dihydroquinopimaric Acid Analogs with Nitrile Groups as Apoptosis-Inducing Anticancer Agents.

Anticancer Agents Med Chem 2019 Apr 3. Epub 2019 Apr 3.

Institute of Petrochemistry and Catalysis of Russian Academy of Sciences, 141 Prospekt Oktyabrya, Ufa 450075. Russian Federation.

Background: Cyan-containing compounds are of great interest as potential anticancer agents. Terpenoids can severe as a natural matrix for the development of promising derivatives with antitumor activity.

Methods: The 2-cyanoethoxy methyl dihydroquinopimarate derivatives (5-9) were synthesized by the reaction of the intermediates (1-4) with acrylonitrile in the presence of alkali (30% KOH solution) using triethylbenzylammonium chloride. Read More

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http://dx.doi.org/10.2174/1871520619666190404100846DOI Listing
April 2019
2 Reads

Synthesis of Tetrahydrobenzo[b]thiophene-3-carbohydrazide Derivatives as Potential Anti-cancer Agents and Pim-1 kinase Inhibitors.

Anticancer Agents Med Chem 2019 04 2. Epub 2019 Apr 2.

National Organization for Drug Control & Research, P.O. Box 29, Cairo, A. R. Egypt.

Background: Tetrahydrobenzo[b]thiophene derivatives were well known to be biologically active compounds and many of them occupy a wide range as anticancer agent drugs.

Objective: One of our main aim of this work was to synthesize target molecules not only possess anti-tumor activities but also kinase inhibitors. To achieve this goal, our strategy was to synthesize a series of 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbohydrazide derivatives using cyclohexan-1,4-dione and cyanoacetylhydrazine to give the 2-amino-6-oxo-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbohydrazide (3) as the key starting material for many heterocyclization reactions. Read More

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http://dx.doi.org/10.2174/1871520619666190402153429DOI Listing
April 2019
1 Read

Triphenylethylene-Coumarin Hybrid TCH-5c Suppresses Tumorigenic Progression in Breast Cancer Mainly Through Its Inhibition of Angiogenesis.

Anticancer Agents Med Chem 2019 Apr 4. Epub 2019 Apr 4.

Central Laboratory, Hebei Key Laboratory of Cancer Radiotherapy and Chemotherapy, Affiliated Hospital of Hebei University and Medical College of Hebei University, Baoding 071000. China.

Background: Coumarins are a wide group of naturally occurring compounds which exhibit a wide range of biological properties such as anti-cancer activities. Here, we characterized the biological functions of three triphenylethylene-coumarin hybrids (TCHs) both in cell culture and nude mouse model.

Methods: Cell proliferation assay was performed in the cell cultures of both EA. Read More

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http://dx.doi.org/10.2174/1871520619666190404155230DOI Listing
April 2019
1 Read
2.469 Impact Factor

Evaluation of New 99mTc(CO)3+ Radiolabeled Glycylglycine in Vivo.

Anticancer Agents Med Chem 2019 Apr 4. Epub 2019 Apr 4.

Department of Nuclear Applications, Institue of Nuclear Sciences Ege University 35100 Bornova, İzmir. Turkey.

Background: Peptide-based agents are used in molecular imaging due to their unique properties, such as rapid clearance from the circulation, high affinity and target selectivity. Many of radiolabeled peptides have been clinically experienced with diagnostic accuracy. The aim of this study was investigation of in vivo biological behavior of [99mTc(CO)3(H2O)3]+ radiolabeled glycylglycine (GlyGly) . Read More

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http://dx.doi.org/10.2174/1871520619666190404154723DOI Listing
April 2019
1 Read

The Possibility of Preventive and Therapeutic Use of Green Tea Catechins in Prostate Cancer.

Anticancer Agents Med Chem 2019 Apr 4. Epub 2019 Apr 4.

Department of Molecular Pharmacology and Radiobiology, Pirogov Russian National Research Medical University (RNRMU), Moscow. Russian Federation.

Background: Prostate cancer is one of the most frequent types of cancer. Despite the existence of various treatment strategies, treatment of prostate cancer still presents serious difficulties (especially in advanced stages). Polyphenols have been extensively assessed in terms of their potential use for prostate cancer treatment and prevention. Read More

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http://dx.doi.org/10.2174/1871520619666190404153058DOI Listing

Foeniculum vulgare and Pelargonium graveolens Essential Oil Mixture Trigger the Cell Cycle Arrest and Apoptosis in MCF-7 Cells.

Anticancer Agents Med Chem 2019 03 25. Epub 2019 Mar 25.

Department Biochemistry, Batterjee Medical College for Science and Technology, Jeddah, Saudi Arabia

Background: Fennel (Foeniculum vulgare) and rose geranium (Pelargonium graveolens) oils are known for their various biological effects including anticancer properties.

Objective: This study aimed to evaluate the anticancer mechanism of fennel and geranium oils combined treatment on MCF-7 cells.

Methods: The GC-MS method for essential oil characterization as well as the in vitro cytotoxicity, morphological changes, real-time PCR and immunocytochemical investigation for apoptosis-related markers, in addition, to flow cytometric cell cycle distribution analysis were done. Read More

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http://dx.doi.org/10.2174/1573399815666190326115116DOI Listing
March 2019
1 Read

Does affinity of Cisplatin to B-Vitamins impair the therapeutic effect in the case of patient with lung cancer consuming carrot or beet juice?

Anticancer Agents Med Chem 2019 Mar 25. Epub 2019 Mar 25.

Department of Physical Chemistry, Faculty of Pharmacy, Collegium Medicum, Nicolaus Copernicus University, Kurpińskiego 5, 85-096, Bydgoszcz. Poland.

Background: Cisplatin (CisPt) has a well-recognized anticancer activity by interacting with DNA and inducing programmed cell death. However, theoretical studies performed on the molecular level suggest that such nonspecific interactions can also take place with many competitive compounds, such as vitamins containing aromatic rings with lone-pair orbitals. It is argued that such direct analogy to interaction of canonical purines can impair the therapeutic effect of Cisplatin. Read More

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http://dx.doi.org/10.2174/1871520619666190325150624DOI Listing
March 2019
1 Read

Design, Synthesis, Anti-Proliferative Evaluation and Cell Cycle Analysis of Hybrid 2-Quinolones

Anticancer Agents Med Chem 2019 03 19. Epub 2019 Mar 19.

Department of Chemistry, Faculty of Applied Sciences, Umm Al-Qura University, P. O. Box 13401, Makkah 21955. Saudi Arabia.

Background: Quinolones are a significant group of nitrogen heterocyclic compounds that exist in therapeutic agents, alkaloids, and synthetic small molecules that have important biological activities. A wide range of quinolones have been used as antituberculosis, antibacterial, anti-malarial, antifungal, anticonvulsant, anticancer agents and urease inhibitors.

Methods: Ethyl 3,3-disubstituted-2-cyano propionates containing hybride quinolones derivatives were synthesized by reaction of 1-amino-7-hydroxy-4-methylquinolin-2(1H)-one and its dibromo derivative with α, β-unsaturated carbonyl in ethanol . Read More

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http://dx.doi.org/10.2174/1871520619666190319142934DOI Listing

Antitumour and Toxicity Evaluation of a Ru(II)-Cyclopentadienyl Complex in a Prostate Cancer Model by Imaging Tools.

Anticancer Agents Med Chem 2019 Mar 18. Epub 2019 Mar 18.

Centro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, km 139.7, 2695-066 Bobadela LRS. Portugal.

Background: Ruthenium complexes have been extensively investigated for their prospective value as alternatives to cisplatin. Recently, we reported the in vitro anticancer properties of a family of organometallic ruthenium(II)-cyclopentadienyl complexes and have explored their mechanism of action.

Objective: The purpose of this study was to evaluate the in vivo antitumour efficacy and toxicity of one of these Ru(II) compounds, [RuCp(mTPPMSNa)(2,2'-bipy)][CF3SO2] (TM85) which displayed an interesting spectrum of activity against several cancer cells. Read More

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http://dx.doi.org/10.2174/1871520619666190318152726DOI Listing
March 2019
1 Read

Design, Synthesis, Anti-proliferative, Anti-microbial, Anti-angiogenic activity and In silico Analysis of Novel Hydrazone Derivatives.

Anticancer Agents Med Chem 2019 Mar 18. Epub 2019 Mar 18.

Biology Department, Faculty of Science, Eskişehir Technical University, 26470, Eski ş ehir. Turkey.

Background: Cancer is the second leading cause of death globally. Hydrazone and hydrazone derivatives have high activity and for this reason, these compound are greatly used by researchers to synthesize new anti-cancer drug. The aim of this research work is to synthesis novel anticancer agents. Read More

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http://www.eurekaselect.com/170802/article
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http://dx.doi.org/10.2174/1871520619666190318125824DOI Listing
March 2019
4 Reads

4t-CHQ a Spiro-Quinazolinone Benzenesulfonamide Derivative Induces G0/G1 Cell Cycle arrest and Triggers Apoptosis Through Down-Regulation of Survivin and Bcl2 in the Leukemia Stem-Like KG1-a Cells.

Anticancer Agents Med Chem 2019 Mar 13. Epub 2019 Mar 13.

Stem Cell Research Center, Tabriz University of Medical Sciences, Tabriz. Iran.

Objective: Many experiments have revealed the anti-tumor activity of spiro-quinazolinone derivatives on different cell types. Exposing KG1-a cells to N-(4- tert- butyl- 4'- oxo- 1'H- spiro [cyclohexane- 1, 2'- quinazoline]- 3'(4'H)- yl)- 4- methyl benzenesulfonamide (4t-CHQ), as an active sub-component of spiro-quinazolinone benzenesulfonamides, the experiment investigated the possible mechanisms that manifest the role of 4t-CHQ in leukemic KG1-a progenitor cells. Mechanistically, the inhibitory effects of 4t-CHQ on KG1-a cells emerges from its madulating function on expression of Bax/Bcl2 and suvinin proteins. Read More

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http://dx.doi.org/10.2174/1871520619666190313165130DOI Listing
March 2019
1 Read
2.469 Impact Factor

Targeting Epidermal Growth Factor Receptor in Non-Small-Cell-Lung Cancer: Current State and Future Perspective.

Anticancer Agents Med Chem 2019 Mar 13. Epub 2019 Mar 13.

Department of Pathophysiology, Key Lab of Neurological Disorder of Education Ministry, School of Basic Medicine, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030. China.

Background: Lung cancer is one of the leading cause of cancer death worldwide, the most common histological type of lung cancer is non-small cell lung cancer (NSCLC), whose occurrence and development is closely related to the mutation and amplification of epidermal growth factor receptors (EGFR). Currently , a series of targeted drugs were developed on the inhibition of EGFR,such as epidermal growth factor receptor-tyrosine kinase inhibitor(EGFR-TKI) and monoclonal antibody (McAb). These drugs have been widely used in clinic practices. Read More

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http://dx.doi.org/10.2174/1871520619666190313161009DOI Listing
March 2019
6 Reads

2,4-Disubstituted Quinazoline Derivatives Act as Inducers of Tubulin Polymerization: Synthesis and Cytotoxicity.

Anticancer Agents Med Chem 2019 Mar 14. Epub 2019 Mar 14.

Department of Medicinal Chemistry, Faculty of Pharmacy and Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran 1417614411. Iran.

Considering the importance to find highly active anticancer agents, we investigated the synthesis and cytotoxic activity of twenty seven 2,4-disubstituted quinazoline derivatives. The cytotoxicity of compounds 1-27 was tested in SRB assays employing five different human tumor cell lines showing four compounds, 2, 9, 16 and 26, being highly cytotoxic with IC50 values ranging between 2.1 and 14. Read More

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http://dx.doi.org/10.2174/1871520619666190314125254DOI Listing

Recent Development in Indole Derivatives as Anticancer Agents for Breast Cancer.

Anticancer Agents Med Chem 2019 Mar 12. Epub 2019 Mar 12.

Laboratory of Natural Products, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda (Pb). India.

Background: Breast Cancer (BC) is the second most common cause of cancer related deaths in women. Due to severe side effects and multidrug resistance, current therapies like hormonal therapy, surgery, radiotherapy and chemotherapy become ineffective. Also, the existing drugs for BC treatment are associated with several drawbacks such as poor oral bioavailability, non-selectivity and poor pharmacodynamics properties. Read More

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http://dx.doi.org/10.2174/1871520619666190312125602DOI Listing
March 2019
1 Read
2.469 Impact Factor

A brief review of scaffold/ drug repurposing for breast cancer therapy.

Anticancer Agents Med Chem 2019 Mar 12. Epub 2019 Mar 12.

Department of Pharmaceutical Chemistry, J.S.S.College of Pharmacy,Udhagamandalam, JSS Academy of Higher Education &research. India.

Conventional drug discovery is a time overwhelming and expensive expedition with super less clinical preference achievement proportion intended for breast cancer therapy. Even if numerous novel approaches to conformation of anti-cancer drugs have been introduced for breast cancer therapy, they have up till now to be implemented in clinical practice. This tempting strategy, facilitate remarkable chance to take entire benefit of existing drugs. Read More

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http://dx.doi.org/10.2174/1389557519666190312124142DOI Listing
March 2019
1 Read

The Role of Vitamin D and Sunlight Incidence in Cancer.

Anticancer Agents Med Chem 2019 Mar 12. Epub 2019 Mar 12.

Metrópole Digital Institute, Federal University of Rio Grande do Norte, 59078-970, Natal/RN. Brazil.

Background: Vitamin D (VD) deficiency affects individuals of different ages in many countries. VD deficiency may be related to several diseases, including cancer.

Objective: This study aimed to review the relationship between VD deficiency and cancer. Read More

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http://dx.doi.org/10.2174/1389557519666190312123212DOI Listing
March 2019
4 Reads

Evaluation of Pyrano[3,2 C] Quinoline Analogues as Anticancer Agents.

Anticancer Agents Med Chem 2019 Mar 8. Epub 2019 Mar 8.

National Facility for Drug Discovery (NFDD), Saurashtra University, Rajkot-360005, Gujarat. India.

Background: Quinoline analogues exhibited diversified biological activities depending on the structure type. A number of natural products with pyrano[3,2-c]quinolone structural motifs and patented chromenes were reported as promising cytotoxic agents.

Objective: The present study is aimed to evaluate a new series of pyrano[3,2-c]quinoline scaffolds derived from fusion of bioactive quinolone pharmacophore with structurally diverse aryl substituted chromene for its cytotoxicity. Read More

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http://dx.doi.org/10.2174/1871520619666190308122734DOI Listing
March 2019
2.469 Impact Factor

The Anti-proliferative Activity of Anisosciadone; A New Guaiane Sesquiterpene from Anisosciadium lanatum.

Anticancer Agents Med Chem 2019 Mar 7. Epub 2019 Mar 7.

Department of Zoology, Faculty of Science, University of Ain Shams, Abbassia 11566, Cairo. Egypt.

Background: The increase in cancer rate and the development of resistant tumors require the continuous search for new anticancer agents.

Aim: This study aimed to analyze and identify the chemical constituents of Anisosciadium lanatum, and to investigate the antiproliferative activity of the identified constituents against various human cell lines (HepG2, MCF7, HT29, A549, and PC3) along with the possible molecular mechanisms involved.

Methods: The structure of the isolated compounds was determined by spectroscopic techniques including HR-FABMS, GC-MS, IR, and 400 MHz 1D and 2D NMR analyses (1H, 13C NMR, DEPT, 1H-1H COSY, HMQC, HMBC and NOESY). Read More

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http://dx.doi.org/10.2174/1871520619666190308112732DOI Listing
March 2019
1 Read

Corilagin Inhibits Esophageal Squamous Cell Carcinoma by Inducing DNA Damage and Down-regulation of RNF8.

Anticancer Agents Med Chem 2019 Mar 7. Epub 2019 Mar 7.

Department of General Practice Center, Nanhai Hospital of Southern Medical University, Foshan 528244. China.

Background: Esophageal squamous cell carcinoma (ESCC), the most prevalent histologic subtype of esophageal cancer, is an aggressive malignancy with poor prognosis and a high incidence in the East. Corilagin, an active component present in Phyllanthus niruri L., has been shown to suppress tumor growth in various cancers. Read More

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http://dx.doi.org/10.2174/1871520619666190307120811DOI Listing

Establishment and Characterization of Pemetrexed-Resistant NCI-H460/PMT Cells.

Anticancer Agents Med Chem 2019 Mar 7. Epub 2019 Mar 7.

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao. China.

Background: Pemetrexed (PMT) is a multitargeted antifolate agent that is used for treating patients with non-small cell lung cancer (NSCLC). However, patients have presented clinical responses of drug resistance to PMT.

Objective: This study aimed to explore the underlying mechanisms of PMT resistance in NSCLC cells. Read More

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http://dx.doi.org/10.2174/1871520619666190307120441DOI Listing
March 2019
1 Read

Synthesis, Biological Investigation and Docking Study of Novel Chromen Derivatives as Anti-Cancer Agents.

Anticancer Agents Med Chem 2019 Mar 7. Epub 2019 Mar 7.

Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad-431001, Maharashtra. India.

A series of novel 6-methyl-3-(3-oxo-1-phenyl-3-(4-(2-(piperidin-1-yl)ethoxy)phenyl)propyl)-2H-chromen-2-one was designed, synthesized and screened for their Anti-Breast Cancer activity against estrogen receptor-positive MCF-7, ZR-75-1 and negative MDA-MB-435 human breast cancer cell lines. Among the synthesized compounds C-3, C-5 and C-15 were showing potent cytotoxicity against estrogen receptor-positive MCF-7. The potent cytotoxic compounds C-3, C-5 and C-15 were further evaluated for in vivo anti-cancer activity by MNU (N-methyl-N-nitrosourea) induced mammary carcinoma in female Sprague-Dawley rats. Read More

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http://dx.doi.org/10.2174/1871520619666190307121145DOI Listing
March 2019
1 Read

Synthesis, Characterization, Quantum-Chemical Calculations and Cytotoxic Activity of 1,8-Naphthalimide Derivatives with non-Protein Amino Acids.

Anticancer Agents Med Chem 2019 Mar 6. Epub 2019 Mar 6.

Department of Chemistry and Chemical Technologies, "Angel Kanchev" University of Ruse, Razgrad Branch, Razgrad 7200. Bulgaria.

Background: The 1,8-Naphthalimides constitute an important class of biologically active, DNA-binding compounds. There are no available data on the synthesis of 1,8-naphthalimide derivatives with non-protein amino acids and their biological activity. The aims of this paper are to synthesis, structural characterization and cytotoxic activity of new 1-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)cycloalkane-1-carboxylic acids with 5-, 6-, 7-, 8- and 12-membered rings as well as 2-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)adamantane-2-carboxylic acid and 1-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)-1,2,3,4-tetrahydronaphthalene-1-carboxylic acid. Read More

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http://dx.doi.org/10.2174/1871520619666190307115231DOI Listing
March 2019
7 Reads

Biological activity, Apoptotic Induction and Cell Cycle Arrest of New Hydrazonoyl Halides Derivatives.

Anticancer Agents Med Chem 2019 Mar 6. Epub 2019 Mar 6.

Chemistry Department (Biotechnology-Biomolecular Chemistry Program), Faculty of Science, Cairo University, Giza. Egypt.

Background: The hydrazonoyl halides are presently an important target in the field of medicinal chemistry. The interest in the chemistry of hydrazonoyl halides is a consequence of the fact that they undergo a wide variety of reactions which provide routes to a myriad of both heterocyclic and acyclic compounds. In addition, they have diverse biological activities such as antiviral, anthelmintic, antiarthropodal,, fungicidal, herbicidal, insecticidal, pesticidal, acaricidal and miticidal Activity correlated to the presence of hydrazonoyl halides. Read More

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http://dx.doi.org/10.2174/1871520619666190306123658DOI Listing
March 2019
1 Read

Inhibition of Polo-Like Kinase 1 by BI2536 Reverses the Multidrug Resistance of Human Hepatoma Cells in Vitro and in Vivo.

Anticancer Agents Med Chem 2019 Mar 1. Epub 2019 Mar 1.

Department of General Surgery, Shanxi Dayi Hospital, Taiyuan, Shanxi, 030032, P. R. China.

Background: Multi Drug Resistance (MDR) is the phenomenon that cancers develop resistance to majority of chemotherapy drugs and is a serious obstacle to the treatment for hepatocellular carcinoma (HCC). Polo-Like Kinase 1 (PLK1) is a serine/threonine kinase associated with tumor growth and clinical prognosis in HCC and BI2536 is its potent inhibitor with IC50 of 0.83 nM. Read More

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http://dx.doi.org/10.2174/1871520619666190301145637DOI Listing
March 2019
4 Reads

Synthesis and Investigation of Therapeutic Potential of Isoform Specific HDAC8 Inhibitors for The Treatment of Cutaneous T Cell Lymphoma.

Anticancer Agents Med Chem 2019 Mar 1. Epub 2019 Mar 1.

Nuclear Magnetic Resonance Laboratory, School of Chemical & Biotechnology, SASTRA University, Thirumalaisamudram, Thanjavur, Tamilnadu. India.

In recent times, we have reported the design and in silico studies of 52 hydroxamic acid derivatives bearing multi-substituent heteroaromatic rings with chiral amine linker as isoform selective histone deacetylase 8 inhibitors (HDAC8i). Wherein, the report suggested that the presence of chiral amine is a prerequisite to occupy the second binding site of HDAC8. Based on these preliminary results, five compounds were shortlisted and synthesized by microwave assisted approach and high yielding synthetic protocol. Read More

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http://dx.doi.org/10.2174/1871520619666190301150254DOI Listing
March 2019
2 Reads

Nitrogen Mustards as Alkylating Agents: A Review on Chemistry, Mechanism of Action and Current USFDA Status of Drugs.

Anticancer Agents Med Chem 2019 Mar 5. Epub 2019 Mar 5.

Organic & Medicinal Chemistry Division, CSIR-IndianInstitute of Chemical Biology, Kolkata 700 032. India.

Background& Objective: Nitrogen mustard derivatives form one of the major class of the anti-cancer agents according to the USFDA approved drugs. These are polyfunctional alkylating agents which are distinguished by a unique mechanism of adduct formation with the DNA that involves a cross-linking between guanine N-7 of one strand of DNA with the other. The generated cross-linking is irreversible and leads to cell apoptosis. Read More

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http://dx.doi.org/10.2174/1871520619666190305141458DOI Listing
March 2019
5 Reads

Schiff Bases and Their Metal Complexes as Potential Anticancer Candidates: A Review of Recent Works.

Anticancer Agents Med Chem 2019 Feb 27. Epub 2019 Feb 27.

Chemistry Department, Natural Science College, Jimma University, Jimma. Ethiopia.

Background: Schiff bases and their metal complexes are emerging as key classes of medicinal compounds, possessing an enormous potential of biological activities like anticancer, anticonvulsant and antioxidant etc. The aim of this review is to examine the anticancer activity of different classes of Schiff bases and their metal complexes.

Methods: Anticancer activity of the already synthesized as well as the novel Schiff bases and their metal complexes was studied using different assays such as 3- [4,5-dimethyltiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT), PI staining, Sulforhodamine, Allium cepa, Sulfo- Rhodamine-B-stain(SRB), viability and potato disc against various human and animal cancer cell lines. Read More

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http://dx.doi.org/10.2174/1871520619666190227171716DOI Listing
February 2019
5 Reads

Microsomal Prostaglandin E2 Synthase-1 as a New Macromolecular Drug Target in the Prevention of İnflammation and Cancer.

Anticancer Agents Med Chem 2019 Feb 27. Epub 2019 Feb 27.

Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Marmara University. Turkey.

Background: Cancer is one of the top killing disease worldwide. Since inflammation is considered to be one of the known characteristics of cancer, the activity of PGE2 has been paired with different tumorigenetic steps such as increased tumor cell proliferation, resistance to apoptosis, increased invasiveness, angiogenesis and immunosuppression.

Objective: It has been succesfully demonstrated that inhibition of mPGES-1 prevented inflammation in preclinical studies. Read More

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http://dx.doi.org/10.2174/1871520619666190227174137DOI Listing
February 2019

Gossypetin Inhibits Solar-UV Induced Cutaneous Basal Cell Carcinoma Through Direct Inhibiting PBK/TOPK Protein Kinase.

Anticancer Agents Med Chem 2019 Mar 1. Epub 2019 Mar 1.

Department of Dermatology, The First Affiliated Hospital of Xi'an Jiaotong University, Xi'an, Shaanxi 710061. China.

Skin photoaging, skin inflammation and skin cancer are related with excessive exposure to solar ultraviolet light (solar-UV). PDZ-binding kinase/T-LAK cell-originated protein kinase (PBK/TOPK), a member of the serine/threonine protein kinase, which regulates the signaling cascades of p38 mitogen-activated protein kinase (p38 MAPK) and extracellular signal regulated kinase 1/2 (ERK1/2). PBK/TOPK plays a significant role in solar-UV-induced cutaneous basal cell carcinoma (cutaneous-BCC), and targeting PBK/TOPK can be supposed to treat and prevent cutaneous-BCC. Read More

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http://dx.doi.org/10.2174/1871520619666190301123131DOI Listing
March 2019
2 Reads
2.469 Impact Factor

Synergistic Effect of Novel EGFR Inhibitor AZD8931 and p38α siRNA in Lung Adenocarcinoma Cancer Cells.

Anticancer Agents Med Chem 2019 Mar 1. Epub 2019 Mar 1.

Immunology Research Center, Tabriz University of Medical Sciences, Tabriz. Iran.

Background: Lung cancer is the leading cause of cancer-related death with less than 5-year survival rate for both men and women worldwide. EGFR and MAPK signaling pathways have a critical role in proliferation and progression of various cancers, including lung cancer. P38 map kinase plays the different role in various tissue hence show a tissue-dependent behavior. Read More

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http://dx.doi.org/10.2174/1871520619666190301125203DOI Listing
March 2019
1 Read
2.469 Impact Factor

Astaxanthin Combine With Human Serum Albumin To Abrogate Cell Proliferation, Migration, And Drug-Resistant In Human Ovarian Carcinoma SKOV3 Cells.

Anticancer Agents Med Chem 2019 Feb 25. Epub 2019 Feb 25.

Youjiang Medical University for Nationalities, 98 Chengxiang Road, Baise 533000. China.

Background: Astaxanthin (AST) shows a large range of beneficial effects together with anti-cancer and antioxidation properties. Human serum albumin (HSA) is the most abundant protein in blood plasma which plays the role of depot and transport protein for many exogenous compounds. However, whether HSA could enhance AST-induced cytotoxic effects in human ovarian cancer cells has not been examined to date. Read More

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http://dx.doi.org/10.2174/1871520619666190225123003DOI Listing
February 2019
1 Read

Substitution at Phenyl Rings of Chalcone and Schiff Base Moieties Accounts for their Antiproliferative Activity.

Anticancer Agents Med Chem 2019 Feb 25. Epub 2019 Feb 25.

University of Ain Shams, Faculty of Science, Department of Zoology, Abbassia 11566, Cairo. Egypt.

Background And Methods: In a continuous combat against cancer which is one of the leading causes of mortality now, chalcone and Schiff bases moieties have been incorporated and their antiproliferative activities and associated mechanisms against liver (HepG2) and breast (MCF-7) cell lines in addition to normal fibroblasts (WI-38) have been examined.

Results: Derivatives 4 and 5 of Schiff bases only and chalcone derivatives of Schiff bases 1 and 2 were devoid of any antiproliferative activity. All three compounds (3, 6, and 7) with significant antiproliferative activity were selective and caused no growth inhibition in normal fibroblasts. Read More

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http://dx.doi.org/10.2174/1871520619666190225122338DOI Listing
February 2019
2 Reads