1,731 results match your criteria Anti-Cancer Agents in Medicinal Chemistry[Journal]


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

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
2 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
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

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

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

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

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
1 Read

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
2 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

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
3 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

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
1 Read
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

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

CORRIGENDUM A Promising Anti-Cancer and Anti-Oxidant Agents Based on the Pyrrole and Fused Pyrrole: Synthesis, Docking Studies and Biological Evaluation.

Authors:

Anticancer Agents Med Chem 2018 ;18(10):1505

Due to an oversight, one of the author's name was published wrong in the article entitled "A Promising Anti-Cancer and Anti-Oxidant Agents Based on the Pyrrole and Fused Pyrrole: Synthesis, Docking Studies and Biological Evaluation" in "Anti-Cancer Agents in Medicinal Chemistry, 2015, Vol. 15, No. 4, pp. Read More

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http://dx.doi.org/10.2174/187152061810181211124824DOI Listing
January 2018

Synthesis, Spectroscopic Properties, Crystal Structure And Biological Evaluation of New Platinum Complexes with 5-methyl-5- (2-thiomethyl)ethyl Hydantoin.

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

Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University of Sofia, Dunav -2 Street, 1000 Sofia. Bulgaria.

Background: The accidental discovery of cisplatin's growth-inhibiting properties a few decades ago led to resurgence of interest in metal-based chemotherapeutics. A number of well-discussed factors such as severe systemic toxicity and unfavourable physicochemical properties further limit the clinical application of the platinating agents. Great efforts have been placed in the development of alternative platinum derivatives with an extended antitumor spectrum and amended toxicity profile as compared to the reference drug cisplatin. Read More

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http://dx.doi.org/10.2174/1871520619666190214103345DOI Listing
February 2019
2 Reads

Erratum to Algerian Propolis Potentiates Doxorubicin Mediated Anticancer Effect Against Human Pancreatic PANC-1 Cancer Cell Line through Cell Cycle Arrest, Apoptosis Induction and P-Glycoprotein Inhibition.

Authors:

Anticancer Agents Med Chem 2018 ;18(9):1364

Due to an oversight one of the author's name was published wrong in the article entitled "Algerian Propolis Potentiates Doxorubicin Mediated Anticancer Effect Against Human Pancreatic PANC-1 Cancer Cell Line through Cell Cycle Arrest, Apoptosis Induction and P-Glycoprotein Inhibition" in "Anti-Cancer Agents in Medicinal Chemistry, 2018, Vol. 18, No. 3, pp. Read More

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http://dx.doi.org/10.2174/187152061809181207144153DOI Listing
January 2018

Two Novel tri-aryl Derivatives Attenuate the Invasion- Promoting Effects of Stromal Mesenchymal Stem Cells on Breast Cancer.

Anticancer Agents Med Chem 2019 02 12. Epub 2019 Feb 12.

Physiology and Pharmacology Department, Pasteur Institute of Iran, Tehran. Iran.

Background: The concept of Epithelial-Mesenchymal Transition (EMT) to promote carcinoma progression has been recognized as a venue for research on novel anticancer drugs. Triaryl template-based structures are one of the pivotal structural features found in a number of compounds with a wide variety of biological properties including anti-breast cancer. Among the various factors triggering EMT program, cyclooxygenase-2 (COX-2), NF-κB as well as the transforming growth factor-beta (TGF-β) have been widely investigated. Read More

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http://dx.doi.org/10.2174/1871520619666190212123912DOI Listing
February 2019
4 Reads

Cancer Therapy Based on Smart Drug Delivery with Advanced Nanoparticles.

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

Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, 410013. China.

Background: Cancer, as one of the most dangerous disease, had caused millions of deaths every year. The main reason is the vacancy of an effective and thorough treatment. The avocations of drug delivery systems had significantly reduced the side-effect of chemotherapy. Read More

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http://dx.doi.org/10.2174/1871520619666190212124944DOI Listing
February 2019
1 Read

Analysis of Comparative Proteomic and Potent Targets of Peniciketal A in Human Acute Monocytic Leukemia.

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

Department of Pharmaceutical Sciences, Binzhou Medical University, Yantai. China.

Background: Peniciketal A (Pe-A), a spiroketal compound, shows potent anticancer activities in human acute monocytic leukemia. However, the detailed mechanisms and potent targets of Pe-A remain largely unexplored. Here, we investigated the differentially expressed proteins between the Pe-A-treated group and the control group on human acute monocytic leukemia cell line THP-1. Read More

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http://dx.doi.org/10.2174/1871520619666190212124339DOI Listing
February 2019
3 Reads

Biological and toxicological evaluation of N-(4methyl-phenyl)-4-methylphthalimide on bone cancer in mice.

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

Postgraduate Program in Pharmaceutical Science, Universidade do Vale do Itajaí, Rua Uruguai, 458, Itajaí/SC, CEP 88302-202. Brazil.

Background: It was recently demonstrated that the phthalimide N-(4-methyl-phenyl)-4-methylphthalimide (MPMPH-1) has important effects against acute and chronic pain in mice, with mechanism of action correlated to adenylyl cyclase inhibition. Furthermore, it was also demonstrated that phthalimide derivatives presented antiproliferative and anti-tumor effects. Considering the literature data, the present study evaluated the effects of MPMPH-1 on breast cancer bone metastasis and correlated painful symptom, and provided additional toxicological information about the compound and its possible metabolites. Read More

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http://dx.doi.org/10.2174/1871520619666190207130732DOI Listing
February 2019
1 Read
2.469 Impact Factor

Synthesis and Biological Evaluation of Novel Heterocyclic Imines Linked Coumarin-Thiazole Hybrids as Anticancer Agents.

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

Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037. India.

Background: Human Galectin-1, protein of lectin family showing affinity towards β-galactosides has emerged as critical regulator of tumor progression and metastasis, by modulating diverse biological events including homotypic cell aggregation, migration, apoptosis, angiogenesis and immune escape. Therefore, galectin-1 inhibitors might represent novel therapeutic agents for cancer.

Methods: A new series of heterocyclic imines linked coumarin-thiazole hybrids (6a-6r) has been synthesized and evaluated for their cytotoxic potential against a panel of six human cancer cell lines namely, lung (A549), prostate (DU-145), breast (MCF-7 & MDA-MB-231), colon (HCT-15 & HT-29) using MTT assay. Read More

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http://dx.doi.org/10.2174/1871520619666190207140120DOI Listing
February 2019

Novel 1,3,4-Triaryl Pyrazoles: Synthesis, QSAR Studies and Cytotoxicity against Breast Cancer.

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

Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo. Egypt.

Background: The existence of drug-resistance and lack of selectivity encourage scientists to search for novel and more selective cytotoxic agents.

Objectives: In this work, novel 1,3,4-triarylpyrazole derivatives were synthesized to study their cytotoxicity on MCF7 (human breast Cell Line). In addition, QSAR studies were done to show the relation between the cytotoxic activity and the structural features of our new synthesized pyrazole derivatives. Read More

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http://dx.doi.org/10.2174/1871520619666190207094610DOI Listing
February 2019
1 Read

Thymoquinone Effects on Cell Viability, Apoptosis and VEGF-A Gene Expression Level in AGS(CRL-1739) Cell Line.

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

Department of Molecular Medicine, National institute of Genetic Engineering and Biotechnology, Tehran. Iran.

Background: Cancer is one of the most fatal diseases across the world and it was reported that 90% of a cancer's fatality depends on its angiogenesis potential. Black seed or Nigella sativa L. is a medicinal plant native to southwest Asia. Read More

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http://dx.doi.org/10.2174/1871520619666190206163504DOI Listing
February 2019
11 Reads

NF-κB-Induced Upregulation of miR-548as-3p Increases Invasion of NSCLC by Targeting PTEN.

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

Department of Medical Genetics, Faculty of Medicine, cILTAM Cancer Biology Laboratory, Pamukkale University, Kinikli, Denizli. Turkey.

Background: Non-Small Cell Lung Cancer (NSCLC) is an aggressive cancer type due to high metastatic capacity. Nuclear Factor Kappa B (NF-κB) is a consistently active transcription factor in malignant lung cancer cells and has crucial significance in NSCLC progression. It is also implicated in the transcriptional regulation of many genes including microRNAs (miRNAs) that function as tumor suppressor or oncogene. Read More

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http://dx.doi.org/10.2174/1871520619666190206165215DOI Listing
February 2019
8 Reads

Interactome Analysis Of The Differentially Expressed Proteins In Uterine Leiomyoma.

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

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

Background: Recent advances in proteomics present enormous opportunities to discover proteome related disparities and thus understanding the molecular mechanisms related to a disease. Uterine leiomyoma is a benign monoclonal tumor, located in the pelvic region, and affecting 40% of reproductive aged female.

Objective: Identification and characterization of the differentially expressed proteins associated with leiomyogenesis by comparing uterine leiomyoma and normal myometrium. Read More

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http://dx.doi.org/10.2174/1871520619666190206143523DOI Listing
February 2019
5 Reads
2.469 Impact Factor

Bis (Isothiocyanatomethyl) Benzene, A Plant Derived Anti-Neoplastic Compound: Purified from Moringa Oleifera Leaf Extract.

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

Department of Biotechnology, Heritage Institute of Technology, Chowbaga Road, Anandapur, P.O East Kolkata Township, Kolkata, West Bengal 700107. India.

Background: Moringa oleifera lam, which is commonly known as "Sajina" is the indigenous species to the India. In our folk medicine it is used for treatment of Canker (cancer). The Moringa oleifera leaf extract contain many phytocompound, among them some are anti-neoplastic in nature. Read More

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http://dx.doi.org/10.2174/1871520619666190206164137DOI Listing
February 2019

GPER Overexpression in Cervical Cancer Versus Premalignant Lesions: Its Activation Induces Different forms of Cell Death.

Anticancer Agents Med Chem 2019 02 6. Epub 2019 Feb 6.

Laboratorio de Inmunología, Departamento de Fisiología, Centro Universitario de Ciencias de la Salud, Universidad de Guadalajara, Guadalajara. Mexico.

Background: The effect of estrogen has been traditionally studied through the modulation of its alpha and beta nuclear receptors; however, the G Protein-Coupled Estrogen Receptor (GPER) has been recently involved in the pathology of numerous tumors. Although the study of GPER in cervical cancer has begun, its contribution still remains to be completely evaluated.

Objective: The purpose of this work was to determine the expression of this receptor in different degrees of cervical lesions and whether the stimulation with its specific agonist (G-1) modulated mechanisms of cell survival or cell death in cervical cancer cells. Read More

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http://dx.doi.org/10.2174/1871520619666190206171509DOI Listing
February 2019
8 Reads

Detection and Analysis of RNAs Expression Profile for Methylated Candidate Tumor Suppressor Genes in Nasopharyngeal Carcinoma.

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

Key Laboratory of Cancer Proteomics of National Health Commission, Xiangya Hospital, Central South University, Changsha 410008. China.

Objective: DNA methylation that acts as a regulator of multiple tumor suppressor genes (TSGs) expression, is believed to play an important role in nasopharyngeal carcinoma (NPC) development.

Methods: We compared the effects of 5-aza-2-deoxycytidine (decitabine, DAC), on gene expression by using RNA-sequencing in NPC cells.

Results: We analyzed differentially expressed genes (DEGs) and found that 2182 genes were significantly up-regulated (≥ 2-fold change) in NPC cells with the demethylation treatment of DAC, suggesting that they may play a key role in cell growth, proliferation, death, and development. Read More

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http://dx.doi.org/10.2174/1871520619666190204094815DOI Listing
February 2019

Synthesis and Reactivity of 6,8-Dibromo-2-ethyl-4H-benzo[d][1,3]oxazin-4-one Towards Nucleophiles and Electrophiles and Their Anticancer Activity.

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

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

Background And Methods: The genetic heterogeneity of tumor cells and the development of therapy-resistant cancer cells in addition to the high cost necessitate the continuous development of novel targeted therapies. In this regard, 14 novel benzoxazinone derivatives were synthesized and examined for anticancer activity against two human epithelial cancer cell lines; breast MCF-7 and liver HepG2 cells. 6,8-Dibromo-2-ethyl-4H-benzo[d][1,3]oxazin-4-one was subjected to react with nitrogen nucleophiles to afford quinazolinone derivatives and other related moieties (3-12). Read More

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http://dx.doi.org/10.2174/1871520619666190201145221DOI Listing
February 2019
1 Read

A New Synthetic Spiroketal: Studies on Antitumor Activity on Murine Melanoma Model In Vivo and Mechanism of Action In Vitro.

Anticancer Agents Med Chem 2019 Jan 31. Epub 2019 Jan 31.

Istituto di Genetica e Biofisica A. Buzzati Traverso - Consiglio Nazionale delle Ricerche, Napoli. Italy.

Background: In a previous study we synthesised a new spiroketal derivative, inspired to natural products, that has shown high antiproliferative activity, potent telomerase inhibition and proapoptotic activity on several human cell lines.

Objective: This work focused on the study of in vivo antitumor effect of this synthetic spiroketal on a murine melanoma model. In order to shed additional light on the origin of the antitumor effect, in vitro studies were performed. Read More

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http://dx.doi.org/10.2174/1871520619666190131141400DOI Listing
January 2019
4 Reads
2.469 Impact Factor

Recent Synthetic Approaches and Biological Evaluations of Amino Hexahydroquinolines and Their Spirocyclic Structures.

Anticancer Agents Med Chem 2019 Jan 31. Epub 2019 Jan 31.

Chemistry Department, Faculty of Science, Cairo University, Giza. Egypt.

In this review, the recent synthetic approaches of amino hexahydroquinolines and their spirocyclic structures were highlighted. The bioactivity profiles and SAR studies of these compounds were also reviewed with emphasis to the utility of these substances as antimicrobial, anticancer and antitubercular agents, as well as calcium channel modulators. Read More

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http://dx.doi.org/10.2174/1871520619666190131140436DOI Listing
January 2019
1 Read

Reverse Screening Bioinformatics Approach to Identify Potential Anti Breast Cancer Targets Using Thymoquinone from Neutraceuticals Black Cumin Oil.

Anticancer Agents Med Chem 2019 Jan 24. Epub 2019 Jan 24.

Avinashilingam Institute for Home Science and Higher Education for Women, Coimbatore, TN. India.

Background: Functional foods, neutraceuticals and natural antioxidants have established their potential roles in the protection of human health and diseases. Thymoquinone (TQ), the main bioactive component of Nigella sativa seeds (black cumin seeds), a plant derived neutraceutical was used by ancient Egyptians because of their ability to cure a variety of health conditions and used as a dietary food supplement. Owing to its multi targeting nature, TQ interferes with a wide range of tumorigenic processes and counteracts carcinogenesis, malignant growth, invasion, migration, and angiogenesis. Read More

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http://dx.doi.org/10.2174/1871520619666190124155359DOI Listing
January 2019

Design, Synthesis, Cytotoxic Activity and Apoptosis-inducing Action of Novel Cinnoline Derivatives as Anticancer Agents.

Anticancer Agents Med Chem 2018 ;18(8):1208-1217

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University; Cairo 11561, Egypt.

Aims: Tyrosine kinases and topoisomerase I are common target enzymes for the majority of the anticancer agents. In contrast to quinazolines and quinolines, kinase inhibitors and topoisomerase inhibitors incorporating cinnoline scaffold are relatively infrequent. Thus the aim of this work was to replace the former scaffolds with the latter one. Read More

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http://dx.doi.org/10.2174/1871520618666180220121319DOI Listing
January 2018
4 Reads

Erratum to Design, Synthesis and Biological Evaluation of a Phenyl Butyric Acid Derivative, N-(4-chlorophenyl)-4- phenylbutanamide: A HDAC6 Inhibitor with Anti-proliferative Activity on Cervix Cancer and Leukemia Cells.

Authors:

Anticancer Agents Med Chem 2018 ;18(8):1218

Due to an oversight one of the author's name was published wrong in the article entitled "Design, Synthesis and Biological Evaluation of a Phenyl Butyric Acid Derivative, N-(4-chlorophenyl)-4- phenylbutanamide: A HDAC6 Inhibitor with Anti-proliferative Activity on Cervix Cancer and Leukemia Cells" in "Anti-Cancer Agents in Medicinal Chemistry, 2017, Vol. 17, No. 10. Read More

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http://dx.doi.org/10.2174/187152061808181112151244DOI Listing
January 2018

Synthesis of New N1Arylpiperazine Substituted Xanthine Derivatives and Evaluation of Their Antioxidant and Cytotoxic Effects.

Anticancer Agents Med Chem 2019 Jan 21. Epub 2019 Jan 21.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University-Sofia, 2 "Dunav" str., 1000,Sofia. Bulgaria.

Background: Cancer is one of the leading causes of morbidity and mortality worldwide, with approximately 14 million new cases in 2012, with most of the clinically used drugs being ineffective. The methylxanthines have emerged highest interest in researches in modifying their structure because of their diverse biological activity. In addition the piperazine nucleus is one of the most important heterocycles exhibiting remarkable pharmacological activities. Read More

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http://www.eurekaselect.com/169218/article
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http://dx.doi.org/10.2174/1871520619666190121155651DOI Listing
January 2019
5 Reads

Synthesis of Dual Target CPT-Ala-Nor Conjugates and Their Biological Activity Evaluation.

Anticancer Agents Med Chem 2019 Jan 21. Epub 2019 Jan 21.

Department of Pharmacy, Zunyi Medical University Affiliated Hospital, 149 Dalian Road, Zunyi. China.

Background: Target therapy has been one of important strategies in new drug discovery. And the resulting drug resistance has also been a serious problem for concern. At the same time, there are several cancer genes or pathways operating within a given cancer. Read More

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http://dx.doi.org/10.2174/1871520619666190121121933DOI Listing
January 2019
4 Reads

Synthesis of Oridonin Derivatives via Mizoroki-Heck Reaction and Click Chemistry for Cytotoxic Activity.

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

Shanghai Institute for Advanced Immunochemical Studies (SIAIS), ShanghaiTech University, Shanghai, 201210. China.

Background: Natural products (NPs) are evolutionarily chosen "privileged structures" that have a profound impact upon the anticancer drug discovery and development progress. However, the search for new drugs based on structure modification of NPs has often been hindered due to the tedious and complicated synthetic pathways. Fortunately, Mizoroki-Heck reaction and copper-catalyzed alkyne-azide cycloaddition (CuAAC) could provide perfect strategies for selective modification on NPs even in the presence of liable functionalities. Read More

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http://dx.doi.org/10.2174/1871520619666190118121439DOI Listing
January 2019
9 Reads

Multi-targeting Anticancer Agents: Rational Approaches, Synthetic Routes and Structure Activity Relationship.

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

Program in Chemical Biology, Sloan Kettering Institute, New York, NY 10065. United States.

We live in a world with complex diseases such as cancer which cannot be cured with one-compound one-target based therapeutic paradigm. This could be due to the involvement of multiple pathogenic mechanisms. One-compound-various-targets stratagem has become a prevailing research topic in anti-cancer drug discovery. Read More

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http://dx.doi.org/10.2174/1871520619666190118120708DOI Listing
January 2019
3 Reads
2.469 Impact Factor

Cytotoxic and genotoxic activities of alkaloids from the bulbs of Griffinia gardneriana and Habranthus itaobinus (Amaryllidaceae).

Anticancer Agents Med Chem 2019 01 18. Epub 2019 Jan 18.

Department of Chemistry, Federal University of Espírito Santo (UFES), Avenida Fernando Ferrari, 514, 29.075-910, Vitória, Espírito Santo. Brazil.

Background: Amaryllidaceae plants are known to be a great source of alkaloids, which are considered an extensive group of compounds encompassing a wide range of biological activity. The remarkable cytotoxic activity observed to the most of Amaryllidaceae alkaloids derivatives have prompt the chemical and biological investigations in unexplored species from Brazil.

Objective: Evaluate the cytoxic and genotoxic properties of alkaloids of Griffinia gardneriana and Habranthus itaobinus bulbs and study the role of caspase-3 as a molecular apoptosis mediator. Read More

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http://dx.doi.org/10.2174/1871520619666190118122523DOI Listing
January 2019
11 Reads

Anti-Diarrheal Drug Repositioning in Tumour Cell Cytotoxicity.

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

Laboratory of Molecular and Cellular Screening Processes, Centre of Biotechnology of Sfax, Sidi Mansour Road Km 6, BP 1177, 3018 Sfax. Tunisia.

Background: Drug repositioning is becoming an ideal strategy to select new anticancer drugs. In particular, drugs treating side effects of chemotherapy are the best candidates.

Objective: In this present work, we tried the evaluation of anti-tumour activity of two anti-diarrheal drugs (nifuroxazide and rifaximin). Read More

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http://dx.doi.org/10.2174/1871520619666190118120030DOI Listing
January 2019
7 Reads

Adenosine analogues as opposite modulators of the cisplatin resistance of ovarian cancer cells.

Anticancer Agents Med Chem 2019 Jan 17. Epub 2019 Jan 17.

Department of Operative Gynaecology and Gynaecological Oncology, Polish Mother's Memorial Hospital - Research Institute, 93-338 Lodz, 281/289 Rzgowska Street. Poland.

Background: Adenosine released by cancer cells in high amounts in the tumour microenvironment is one of the main immunosuppressive agents responsible for the escape of cancer cells from immunological control. Blocking adenosine receptors with adenosine analogues and restoring immune cell activity is one of the methods considered to increase the effectiveness of anticancer therapy. However, their direct effects on cancer cell biology remain unclear. Read More

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http://dx.doi.org/10.2174/1871520619666190118113201DOI Listing
January 2019
11 Reads