1,582 results match your criteria Anti-Cancer Agents in Medicinal Chemistry[Journal]


Verbascoside attenuates Rac-1 and HIF-1α signaling cascade in colorectal cancer cells.

Anticancer Agents Med Chem 2018 Jun 10. Epub 2018 Jun 10.

Department of Cellular & Molecular Biology, Kharazmi University . Iran.

Objective: Metastasis phenotype is considered as a main challenge in colon cancer therapeutic methods. Furthermore, the side effects of conventional colorectal cancer treatment methods, has attracted a lot of attention into natural ingredients. The aim of the study was to assess the molecular mechanism of verbascoside as natural bio-compound in human HT29 colon cancer cells. Read More

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June 2018
2 Reads

Cytotoxic and apoptotic effects of novel pyrrolo[2,3-d]pyrimidine derivatives containing urea moieties on cancer cell lines.

Anticancer Agents Med Chem 2018 Jun 4. Epub 2018 Jun 4.

Baskent University, School of Medicine, Department of Medical Genetics, Yuregir, Adana. Turkey.

A series of new pyrrolo[2,3-d]pyrimidines containing urea moieties have been synthesized and evaluated for their anticancer activity against cancer cell lines including A549, PC3, SW480 and MCF-7. Among the synthesized compounds, 9e, 10a and 10b exhibited the most potent cytotoxic activities against different cancer cell lines. Compound 10a (IC50 = 0. Read More

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June 2018
3 Reads

Bursal hexapeptide , a potential immunomodulator, inhibits tumor cells proliferation via p53 signaling pathway.

Anticancer Agents Med Chem 2018 Jun 3. Epub 2018 Jun 3.

College of Animal Science and Technology, Henan University of Science and Technology. No.263 kaiyuan Road, Luoyang 471023, Henan Province. China.

The bursa of Fabricius (BF) is acknowledged as central humoral immune organ unique to birds. Bursal hexapeptide (BHP, AGCCNG) is a recently reported bursal-derived bioactive peptide. However, there are few reports of the molecular basis of the mechanism on immune induction and potential antitumor activity of BHP. Read More

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June 2018
2 Reads

Curcumin Modulates Glycolytic Metabolism and Inflammatory Cytokines via Nrf2 in Dalton's Lymphoma Ascites Cells in vivo.

Anticancer Agents Med Chem 2018 Jun 3. Epub 2018 Jun 3.

Biochemistry and Molecular Biology Laboratory, Department of Zoology, Institute of Science, Banaras Hindu University, Varanasi-221005. India.

Background: Warburg effect is characterized by upregulation of HIF-1 and c-Myc regulated LDH-A, even aerobically owing to hypoxic environment and alterations in oncogenes or tumor suppressor genes in cancer. Reduced antioxidant defence system in transformed cells favors higher ROS production, which plays a significant role in carcinogenesis and acts as an important regulator of NF-κB. In addition, various proinflammatory cytokines play active roles in maintenance and progression of cancer. Read More

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June 2018
6 Reads

Artepillin C induces selective oxidative stress and inhibits migration and invasion in a comprehensive panel of human cervical cancer cell lines.

Anticancer Agents Med Chem 2018 Jun 3. Epub 2018 Jun 3.

Programa de Pos Graduacao em Biociencias e Fisiopatologia, Departamento de Analises Clinicas e Biomedicina, Universidade Estadual de Maringa (UEM), Maringa, Parana. Brazil.

Artepillin C (3,5-diprenyl-4-hydroxycinnamic acid) is the main bioactive component of Brazilian green propolis, and possesses, among other things, anticancer properties. However, to the best of our knowledge, there are no studies of artepillin C in cervical cancer. To explore a new therapeutic candidate for cervical cancer, we have evaluated the effects of artepillin C on cellular viability in a comprehensive panel of human cervical cancer-derived cell lines including HeLa (human papillomavirus/HPV 18-positive), SiHa (HPV 16-positive), CaSki (HPV 16- and 18-positive) and C33A (HPV-negative) cells compared to a spontaneously immortalized human epithelial cell line (HaCaT). Read More

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June 2018
2 Reads

New approaches for the uses cyclohexan-1,4-dione for the synthesis of 5,6,7,8-tetrahydro-benzo[4,5]thieno[2,3-b]pyridine derivatives used as potential anti-prostate cancer agents and Pim-1 kinase inhibitors.

Anticancer Agents Med Chem 2018 Jun 3. Epub 2018 Jun 3.

Department of Pharmaceutical Chemistry, College of pharmacy, Jazan University, P.O. Box 114, Jazan 45142. Saudi Arabia.

Background: Among wide range of heterocyclic steroidal derivatives acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Many pharmacological drugs containing the thiophene nucleus were known in the market.

Method: A series of tetrahydrobenzothienopyridine derivatives were synthesized from the reaction 2-amino-3-benzoyl-4,5-dihydrobenzo[b]thiophen-6(7H)-one were synthesized and used for further heterocyclization reactions through the reaction with different reagent. Read More

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June 2018
2 Reads

Peniciketal A, A Novel Spiroketal Compound, Exerts Anticancer Effects by Inhibiting Cell Proliferation, Migration and Invasion of A549 Lung Cancer Cells.

Anticancer Agents Med Chem 2018 Jun 3. Epub 2018 Jun 3.

Department of Pharmaceutical Sciences, Binzhou Medical University, Yantai 264003. China.

Peniciketal A (Pe-A) is a spiroketal compound isolated from saline soil-derived fungus Penicillium raistrickii. However, its role for biological processes has not been clarified. In this study, we for the first time investigated the anticancer effects and the underlying mechanisms of Pe-A in A549 lung cancer cells. Read More

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June 2018
2 Reads

An Overview of Natural Plant Products in the Treatment of Hepatocellular Carcinoma.

Anticancer Agents Med Chem 2018 Jun 3. Epub 2018 Jun 3.

Biochemistry Laboratory, Department of Zoology, School of Biological Sciences, Dr. Harisingh Gour Central University, Sagar-470003, Madhya Pradesh. India.

Liver cancer is the fifth most commonly diagnosed cancer and the second leading cause of cancer related deaths worldwide. Among the liver cancers, hepatocellular carcinoma has been reported to be responsible for 85-90% of primary liver cancer and it is the second most common cause of cancer mortality with 700,000 deaths documented annually. The major risk factors of HCC include chronic infections with the hepatitis B (HBV) or hepatitis C (HCV) virus, chronic liver diseases, alcoholism as well as dietary carcinogens, such as aflatoxins. Read More

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June 2018
3 Reads

Lichen acids may be used as a potential drug for cancer therapy; by inhibiting mitochondrial thioredoxin reductase purified from rat lung.

Anticancer Agents Med Chem 2018 May 24. Epub 2018 May 24.

Department of Molecular Biology and Genetics, Science Faculty, Ataturk University, Erzurum. Turkey.

Background: Thioredoxin reductase (E.C 1.6. Read More

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May 2018
7 Reads

Oxaliplatin regulates chemotherapy induced peripheral neuropathic pain in the dorsal horn and dorsal root ganglion via the Calcineurin/NFAT pathway.

Anticancer Agents Med Chem 2018 May 24. Epub 2018 May 24.

Sun Yat-sen University Cancer Center, State Key Laboratory of Oncology in South China,Collaborative Innovation Center for Cancer Medicine, Guangzhou 510060. China.

Objective: The aim of this study was to investigate the mechanism of oxaliplatin in the induction of neuropathic pain as a symptom of chemotherapy-induced peripheral neuropathy (CIPN).

Methods: The CIPN rat model was induced with a one-time injection of oxaliplatin, and the paw withdrawal response was determined using von Frey filaments. The paw withdrawal threshold (PWT) value was recorded and the dorsal horn (DH) and dorsal root ganglion (DRG) tissues were collected. Read More

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May 2018
3 Reads

Synthesis and Cyototoxicities of New Azafluorenones with Apoptotic Mechanism of Action and Cell Cycle Analysis.

Anticancer Agents Med Chem 2018 May 24. Epub 2018 May 24.

Department of Chemistry, Faculty of Science, Ataturk University, Erzurum. Turkey.

In this study, new azafluorenones, 4-(4-fluorophenyl)-2-(4-substitutedphenyl)-5H-indeno[1,2-b]pyridin-5-one, I1-I8 were synthesized and chemical structures were elucidated by spectral analysis. All compounds were reported for the first time here. Compounds were tested in terms of cytotoxicity. Read More

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May 2018
1 Read

Anti-glioma effects of Caffeic acid phenethyl ester and Dasatinib combination therapy in an in vivo rat glioma model.

Anticancer Agents Med Chem 2018 05 15. Epub 2018 May 15.

Women Scientist Fellow Centre of Research for Development University of Kashmir - 190006, Jammu & Kashmir. India.

Background: Caffeic acid phenethyl ester and Dasatinib in combination, when used in congruous proportions and durations, present an antitumor potential for glioma in vitro, suggesting a high therapeutic potential for glioma treatment.

Objective: In the present study, we addressed the question whether CAPE and Dasatinib target multiple pathways involved in tumor growth, proliferation and development on an in vivo rat model of glioma.

Methods: Expression analysis of proteins thought to be mediating proliferation, cell motility, angiogenesis, and invasion was carried out to delineate the antineoplastic action of CAPE and Dasatinib. Read More

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Selection of G1-PABA as a GPER1 ligand compared to phenol red via a ligand-based virtual screening coupled to molecular dynamics simulations and its anti-proliferative effects on breast cancer cells.

Anticancer Agents Med Chem 2018 May 10. Epub 2018 May 10.

Laboratorio de Modelado Molecular y Diseno de farmacos, Laboratorio de Bioquimica, Seccion de Estudios de Posgrado e Investigacion, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Miron, 11340 Ciudad de Mexico. Mexico.

Recent reports have demonstrated the role of the G protein-coupled estrogen receptor (GPER1) on the growth and proliferation of breast cancer cells. The coupling of GPER1 to estrogen, tamoxifen or fulvestrant triggers cellular signaling pathways (PI3K and ERK) related to cell proliferation. In an effort to develop new therapeutic strategies against breast cancer, we performed an in silico study to explore the binding pose of a set of designed G15 and G1 analogue compounds, including phenol red. Read More

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May 2018
5 Reads

Indazoles derivatives: promising anti-tumor agents.

Anticancer Agents Med Chem 2018 May 9. Epub 2018 May 9.

Key Laboratory of Theoretical Organic Chemistry and Functional Molecule (Ministry of Education), Hunan Provincial Key Laboratory of Controllable Preparation and Functional Application of Fine Polymers, School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, Hunan 411201. China.

Currently, cancer continues being a dramatically increasing and serious threat to public health. Although many anti-tumor agents have been developed in recent years, the survival rate of patients is not satisfactory. The poor prognosis of cancer patients is closely related to the occurrence of drug resistance. Read More

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Novel Nicotinonitrile Derivatives Bearing Imino Moieties Enhance Apoptosis and Inhibit Tyrosine Kinase.

Anticancer Agents Med Chem 2018 May 9. Epub 2018 May 9.

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

Background: Fused heterocyclic containing pyrazolopyridine systems have several medicinal activities including cytotoxic and carcinostatic activities.

Objective: To investigate the antiproliferative activity and associated mechanism(s) of a novel series of nicotinonitrile derivatives.

Method: The series has been synthesized by reaction of hydrazonoyl chlorides with each of 4-(4-methoxyphenyl)-3-methyl-6-oxo-6,7-dihydro-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile and 2-amino-4-(4-methoxyphenyl)-6,7-dihydro-5H-cyclopenta[b]pyridine-3-carbonitrile in dioxane in basic medium. Read More

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May 2018
3 Reads

Synthesis and Evaluation of A Series of 1,3,4-Thiadiazole Derivatives as Potential Anticancer Agents.

Anticancer Agents Med Chem 2018 May 8. Epub 2018 May 8.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskisehir. Turkey.

In an effort to develop potent anticancer agents, the synthesis of a series of benzothiazole-based 1,3,4-thiadiazole derivatives (1-14) was described and their cytotoxic effects on A549 human lung adenocarcinoma, MCF-7 human breast adenocarcinoma, HepG2 human hepatocellular carcinoma and NIH/3T3 mouse embryonic fibroblast cell lines were investigated using MTT assay. Phenyl-substituted compounds (8-14) were found to be more effective than naphthyl-substituted compounds (1-7) on cancer cells. Compounds 8, 9, 10, 12, 13 and 14 were identified as the most potent anticancer agents on MCF-7 and HepG2 cell lines and therefore their effects on DNA synthesis and apoptotic/necrotic cell death in MCF-7 cell line were evaluated. Read More

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May 2018
1 Read

Zinc Finger Nuclease Combines with Cisplatin and Trichostatin A Enhances the Antitumor Potency in Cervical Cancer Cells.

Anticancer Agents Med Chem 2018 May 9. Epub 2018 May 9.

Department of Obstetrics and Gynecology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan. China.

Cervical cancer is the third-most common malignant tumor among women worldwide, which seriously endangers the life and health of Chinese women. The primary etiological factor of cervical cancer is persistent infection with high-risk human papillomavirus (HR-HPV), particularly HPV16 and HPV18. HR-HPV express oncoproteins E6 and E7, both of which play key roles in the progression of cervical carcinogenesis. Read More

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Heterocyclization of Thiophenes derived from Estrone followed by cytotoxic, HTRF kinase and Pim-1 kinase evaluations.

Anticancer Agents Med Chem 2018 May 7. Epub 2018 May 7.

Department of Chemistry, Faculty of Science, University of Tabuk, Tabuk 71491, P. O. Box 741. Saudi Arabia.

Background: Among wide range of heterocyclic steroidal derivatives acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Many pharmacological drugs containing the steroid nucleus were known in the market.

Objective: Our main aim of this work was to synthesis a seies of heterocyclic compounds especially thiophene and thienopyridine derivatives containing the estrone nucleuous. Read More

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May 2018
3 Reads

HCC Specific Protein Network Involving Interactions of EGFR with A-Raf and Transthyretin: Experimental Analysis and Computational Biology Correlates.

Anticancer Agents Med Chem 2018 May 7. Epub 2018 May 7.

Jamia Hamdard - Biochemistry, HIMSR New Delhi. India.

The network interactions link human disease proteins to regulatory cellular pathways leading to better understanding of protein functions and cellular processes. Revealing the network of signaling pathways in cancer through protein-protein interactions at molecular level enhances our understanding of hepatocellular carcinoma (HCC). A rodent model for study of HCC was developed by administrating N-Nitrosodiethylamine (DEN) and 2-aminoacetylfluorine (2-AAF) to male Wistar rats. Read More

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May 2018
2 Reads

Cold physical plasma treated buffered saline solution as effective agent against pancreatic cancer cells.

Anticancer Agents Med Chem 2018 May 7. Epub 2018 May 7.

Department of General, Visceral, Thoracic and Vascular Surgery, University Medicine Greifswald, Ferdinand-Sauerbruch-Straße, 17475 Greifswald. Germany.

Cold physical plasma has been suggested as a new anticancer tool recently. However, direct use of plasma is limited to visible tumors and in some clinical situations not feasible. This includes repetitive treatment of peritoneal metastases which commonly occur in advanced gastrointestinal cancer and in pancreatic cancer in particular. Read More

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May 2018
2 Reads

Synthesis, 17α--hydroxylase-C17,20-lyase inhibitory and 5AR reductase activity of novel pregnenolone derivatives.

Anticancer Agents Med Chem 2018 Apr 25. Epub 2018 Apr 25.

Centre of research and development, University of Kashmir, Hazratbal, India-190002. India.

A series of 1,5-diaryl pyrazoline pregnenolones were synthesized and screened for 5α-reductase inhibitory activities. Synthesis of the analogs is multistep and proceeds in good overall yields. The key step in the synthesis of 1,5-disubstituted pyrazolinyl pregnenolones (5a-l) is the heterocyclization of bezylidine derivatives (3) in presence of phenylhydrazines (4) through the initial formation of the phenylhydrazones, which undergo concomitant cyclization to generate the stable pyrazoline derivatives. Read More

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April 2018
3 Reads

TPEN exerts antitumor efficacy in murine mammary adenocarcinoma through an H2O2 signaling mechanism dependent on caspase-3.

Anticancer Agents Med Chem 2018 Apr 25. Epub 2018 Apr 25.

Neuroscience Research Group, Medical Research Institute, Faculty of Medicine, University of Antioquia (UdeA), Calle 70 No. 52-21, and Calle 62 # 52-59, Building 1, Room 412; SIU Medellin. Colombia.

Background: Breast cancer is the second most common cancer worldwide. N, N, N', N'-Tetrakis (2-pyridylmethyl)-ethylenediamine (TPEN) is a lipid-soluble zinc metal chelator that induces apoptosis in cancer cells through oxidative stress (OS). However, the effectiveness and the mechanisms involved in TPEN-induced cell death in mammary adenocarcinoma cells in vitro and in vivo are still unclear. Read More

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April 2018
3 Reads

Guide for Selection of Relevant Cell Lines During the Evaluation of New Anti-Cancer Compounds.

Anticancer Agents Med Chem 2018 Feb 20. Epub 2018 Feb 20.

Departamento de Farmacologia, Facultad de Medicina, Universidad Nacional Autonoma de Mexico (UNAM). Ciudad de Mexico. Mexico.

Human cancer cell lines are valuable models for anti-cancer drug development. Although all cancer cells share common biological features, each cancer cell line has unique genotypic/ phenotypic characteristics that affect drug response. Thus, the information obtained with a specific cancer cell line cannot be easily extrapolated to other cancer cells. Read More

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February 2018
2 Reads

Insights into the Biological Evaluation of Pterocarpanquinones and Carbapterocarpans with Anti-Tumor Activity against MDR Leukemias.

Anticancer Agents Med Chem 2018 Apr 20. Epub 2018 Apr 20.

Universidade Federal do Rio de Janeiro - Laboratorio de Quimica Bio-organica (LQB), Instituto de Pesquisas de Produtos Naturais Rio de Janeiro, Rio de Janeiro. Brazil.

In an attempt to find anticancer agents that could overcome multidrug resistance (MDR), two new classes of modified isoflavonoids were designed and synthesized, and their effectiveness evaluated against a vast array of tumor cell lines. Pterocarpanquinone (LQB-118) and 11a-aza-5-carbapterocarpan (LQB-223) were the most promising. LQB-118 induced cell death, in vitro, in the mM range, to a number of human cancer cell lines as well as to fresh tumor cells obtained from patients with acute or chronic myeloid leukemia, independent on whether they exhibit or not the MDR phenotype. Read More

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April 2018
4 Reads

Glioma And Neurokinin-1 Receptor Antagonists: A New Therapeutic Approach.

Anticancer Agents Med Chem 2018 Apr 20. Epub 2018 Apr 20.

Institute of Neurosciences of Castilla y Leon (INCYL) Salamanca. Spain.

Background: In children/adults, the most lethal and frequent primary brain tumor is glioblastoma. Despite multimodal aggressive therapies, the median survival time after diagnosis is around 15 months. In part, this is due to the blood-brain barrier that restricts common treatments (e. Read More

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April 2018
1 Read

Metal complexes of natural product like-compounds with antitumoral activity.

Anticancer Agents Med Chem 2018 Apr 20. Epub 2018 Apr 20.

Instituto de Investigacion de Enfermedades Raras (IIER), Instituto de Salud Carlos III, Madrid. Spain.

Cancer continues to be one of the major causes of death worldwide. Despite many advances in the understanding of this complex disease, new approaches are needed to improve the efficacy of current therapeutic treatments against aggressive tumors. Natural products are one of the most consistently successful source of drug leads. Read More

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April 2018
1 Read

Liposomes co-encapsulating anticancer drugs in synergistic ratios as an approach to promote increased efficacy and greater safety.

Anticancer Agents Med Chem 2018 Apr 20. Epub 2018 Apr 20.

Universidade Federal de Minas Gerais - Department of Pharmaceutical Products, Faculty of Pharmacy Belo Horizonte. Brazil.

The era of chemotherapy began in the 1940s, but it was in the 1960s that it was seen as really promising, when the first patients with childhood acute lymphoblastic leukemia were cured with combination chemotherapy. Today, it is known that due to resistance to single agents, combination therapy is essential for tumor eradication and cure. In the last decade, studies have shown that anticancer drug combinations can act synergistically or antagonistically against tumor cells in vitro, depending on the ratios of the individual drugs forming the combination. Read More

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April 2018
1 Read

Active surveillance for low-risk prostate cancer: are all criteria similar?

Anticancer Agents Med Chem 2018 Apr 25. Epub 2018 Apr 25.

Department Of Surgery, Urology Section, University Of Catania. Italy.

Active surveillance (AS) is a therapeutic strategy for early-stage prostate cancer (PCa) conceived to balance early detection of aggressive disease and overtreatment of indolent tumor. Several active surveillance protocol have been published over the years, however the risk of misclassification still exist. In this review, we revised the current criteria of AS and evaluated the characteristics of potential risk factors of misclassification or deferred treatment. Read More

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Natural macromolecules with protective and antitumor activity.

Anticancer Agents Med Chem 2018 Apr 24. Epub 2018 Apr 24.

Grigore T. Popa University of Medicine and Pharmacy, Iasi. Romania.

This review summarizes the literature data regarding plant lectins and as novel drug sources in prevention or treatment of cancer. Moreover, such compounds have been described as natural toxins that possess different biological activities (cytotoxic, antitumor, antimutagenic and anticarcinogenic properties). This activity depends greatly on their structure and affinity. Read More

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April 2018
8 Reads

DTCM-glutarimide delays growth and radiosensitizes glioblastoma.

Anticancer Agents Med Chem 2018 Apr 22. Epub 2018 Apr 22.

Department of Biology, Faculty of Philosophy, Sciences and Letters at Ribeirao Preto, University of Sao Paulo. Brazil.

Background And Purpose: Glioblastoma (GBM) is the most aggressive brain tumor. Even with the advent of temozolomide, patient survival remains poor, with expected median survival around 1 year from diagnosis. Consequently, the relentless search for new therapeutic strategies able to increase patient outcome persists. Read More

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April 2018
1 Read

Novel Anthraquinone Derivatives as Dual Inhibitors of Topoisomerase 2 and Casein Kinase 2: In silico Studies, Synthesis and Biological Evaluation on Leukemic Cell Lines.

Anticancer Agents Med Chem 2018 Apr 22. Epub 2018 Apr 22.

Bharati Vidyapeeth`s College of Pharmacy, Department of Pharmaceutical Chemistry, Sector 8, C. B. D. Belapur, Navi Mumbai 400614, Maharashtra. India.

Background - Cancer being a complex disease, single targeting agents remains unsuccessful. This calls for "multiple targeting", wherein a single drug is so designed that it will modulate the activity of multiple protein targets. Topoisomerase 2 (Top2) helps in removing DNA tangles and super-coiling during cellular replication, Casein Kinase 2 (CK2) is involved in the phosphorylation of multitude of protein targets. Read More

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April 2018
2 Reads

Ultrasound Promoted Green Synthesis, Docking study of Indole Spliced Thiadiazole, α-amino phosphonates as Anticancer Agents and Anti-tyrosinase Agents.

Anticancer Agents Med Chem 2018 Apr 17. Epub 2018 Apr 17.

Shreeyash Institute of Pharmacy - Department of Pharmaceutical Chemistry Aurangabad. India.

In this work, a new series of diethyl ((1H-indole-3-yl)((5-phenyl-1,3,4-thiadiazole-2- yl)amino)methyl)phosphonate derivatives 6(a-j) were designed and synthesized in Ultrasound by green protocol using Kabachnik-Fields reaction. The structures of the synthesized compounds were confirmed by spectral analysis such as elemental analyses, IR, 1H NMR, 13C NMR, 31P NMR and mass spectra. The synthesized compounds 6(a-j) were appraised for their in vitro anticancer activity against human cancer cell lines such as SK-MEL-2 (melanoma), IMR-32 (Neuroblastoma), HT-29(Colon) and also on normal murine embryonic fibroblast NIH/3T3 by Sulforhodamine B (SRB) assay, using Adriamycin as a standard drug. Read More

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April 2018
2 Reads

Synthesis, Cytotoxicity And Antioxidant Activity Of New Analogues Of Rc-121 Synthetic Derivatives Of Somatostatin.

Anticancer Agents Med Chem 2018 Apr 17. Epub 2018 Apr 17.

University of Chemical Technology and Metallurgy, Department of Organic Chemistry Blvd. 8 Kl. Ohridski, 1756 Sofia. Bulgaria.

Background: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity.

Objectives: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine).

Methods: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (human colorectal cancer cell line), MDA-MB-23 (human breast cancer cell line), Hep G-2 (human hepatocellular carcinoma cell line) and HeLa (cervical cancer cell line). Read More

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April 2018
2 Reads

Design, synthesis, in vitro anti-cancer activity, ADMET profile and molecular docking of novel triazolo[3,4-a]phthalazine derivatives targeting VEGFR-2 enzyme.

Anticancer Agents Med Chem 2018 04 12. Epub 2018 Apr 12.

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

In view of their expected anticancer activity, novel triazolo[3,4-a]phthalazine derivatives 5-6a-o and 3-substituted-bis([1,2,4]triazolo)[3,4-a:4',3'-c]phthalazines 9a-b were designed, synthesized and evaluated for their anti-proliferative activity against two human tumor cell lines HCT-116 human colon adenocarcinoma and MCF-7 breast cancer. It was found that, compound 6o the most potent derivative against both HCT116 and MCF-7 cancer cell lines. Compounds 6o, 6m, 6d and 9b showed the highest anticancer activities against HCT116 human colon adenocarcinoma with IC50 of 7±0. Read More

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April 2018
4 Reads

Specific cytostatic and cytotoxic effect of dihydrochelerythrine in glioblastoma cells: role of NF-kB/b-catenin and STAT3/IL-6 pathways.

Anticancer Agents Med Chem 2018 Apr 12. Epub 2018 Apr 12.

Universidade Federal da Bahia - Health Sciences Institute Salvador, Bahia. Brazil.

A glioblastoma is a primary CNS tumor that is more aggressive and lethal than other brain tumors. Its location, rapid proliferation, invasive growth, angiogenesis and immunosuppression are the main factors that limit its treatment, making it a major challenge to neuro-oncology.

Objective: This study investigated the in vitro effects of the alkaloid dihydrochelerythrine (DHC), which is extracted from Zanthoxylum stelligerum, on the viability, proliferation, cell death and b-catenin, NFkB, STAT3/pSTAT3 and interleukins roles. Read More

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April 2018
9 Reads

Antitumor Effect Of Pomolic Acid In Acute Myeloid Leukemia Cells Involves Cell Death, Decreased Cell Growth And Topoisomerases Inhibition.

Anticancer Agents Med Chem 2018 04 12. Epub 2018 Apr 12.

Instituto Nacional de Cancer Rio de Janeiro, RJ. Brazil.

Background: Acute myeloid leukemia (AML) represent the largest number of annual deaths from hematologic malignancy. In the United-States, it is estimated that 21.380 individuals will be diagnosed with AML and 49. Read More

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April 2018
3 Reads

Poly-L-arginine: Enhancing Cytotoxicity and Cellular Uptake of Doxorubicin and Necrotic Cell Death.

Anticancer Agents Med Chem 2018 04 11. Epub 2018 Apr 11.

Ferdowsi University of Mashhad - Department of Chemistry Mashhad. Iran.

Objective: Cell resistance to doxorubicin and its toxicity to healthy tissue reduce its efficiency. The use of cell penetrating peptides as drug delivery system along with doxorubicin is a strategy to reduce its side effects. In this study, the influence of poly-L-arginine on doxorubicin cytotoxicity, its cellular uptake and doxorubicin-induced apoptosis on human prostate cancer DU145 cells are assessed. Read More

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April 2018
6 Reads

Physicochemical characterization of curcumin loaded chitosan nanoparticles: Implications in cervical cancer.

Anticancer Agents Med Chem 2018 Apr 11. Epub 2018 Apr 11.

Department of Biosciences, Jamia Millia Islamia, New Delhi. India.

Curcumin is a potent anticancer agent and has great potential efficacy against different types of cancers. A major disadvantage of curcumin, however, is its poor solubility and bioavailability. The aim of the present work is to synthesize chitosan and curcumin-loaded chitosan nanoparticles and their characterization through various physicochemical methods and cellular uptake in cervical cancer cell line SiHa. Read More

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April 2018
2 Reads

2-Methoxy-6-Acetyl-7-Methyljuglone (MAM) Induces iNOS/NO-mediated DNA Damage Response through Activation of MAPKs Pathways.

Anticancer Agents Med Chem 2018 Apr 10. Epub 2018 Apr 10.

University of Macau, Macau. China.

There are inconsistent reports about the role of nitric oxide (NO) in cancer progression and prevention. Quinones demonstrate significant anti-cancer activities both in vitro and in vivo. Here, we reported that 2-methoxy-6-acetyl-7-methyljuglone (MAM), a natural naphthoquinone isolated from Polygonum cuspidatum Sieb. Read More

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April 2018
3 Reads

Translational research: a future strategy for managing Squamous Cell Carcinoma of the Head and Neck?

Anticancer Agents Med Chem 2018 Apr 10. Epub 2018 Apr 10.

National Tumor Institute of Naples Foundation G. Pascale - Head and Neck and Soft Tissue Sarcoma Oncology Unit Naples. Italy.

Background: Squamous cell carcinoma of the head and neck (SCCHN) are neoplasms arising from the epithelium of the first aero-digestive tract. They are very heterogeneous both clinically and biologically. Classic and well acknowledged risk factors are alcohol and tobacco consumption and other forms of smokeless tobacco assumption, although lately the incidence of human papilloma virus (HPV)-related SCCHN is rapidly increasing. Read More

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April 2018
3 Reads

ACP5: its structure, distribution, regulation and novel functions.

Anticancer Agents Med Chem 2018 Apr 11. Epub 2018 Apr 11.

Department of Pathology, Xuzhou Medical University, Xuzhou 221002. China.

Background: Tartrate-resistant acid phosphatase 5 (ACP5) is an evolutionarily conserved and multifunctional protein that is involved in generations of reactive oxygen species, normal bone development, osteoblast regulation and macrophage function, affecting a series of pathways, as well as reflecting bone resorption and osteoclast activity.

Methods: Literature searches, systematic reviews and assessments about the structure, distribution, regulation and novel functions of ACP5 were performed in this review from PubMed and Medline databases.

Results: Studies demonstrate that RANKL can increase the expression of ACP5 through NFATc1 and c-Fos to accelerate osteoclastogenesis, which also can be regulated by many regulators. Read More

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April 2018
2 Reads

Anticancer Pyrrolizines: Design, Synthesis, Caspase-3 activation and Micronucleus (MN) Induction.

Authors:
Amany Belal

Anticancer Agents Med Chem 2018 Apr 9. Epub 2018 Apr 9.

Medicinal Chemistry Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514. Egypt.

For further exploration of the promising pyrrolizine scaffold and in continuation of our previous work, that proved the potential anticancer activity of the hit compound I, a new series of pyrrolizines 2-5 and 7-9 were designed and synthesized. Structures of the new compounds were confirmed by IR, 1H-NMR, 13C-NMR and elemental analysis. Antitumor activity for the prepared compounds against human breast adenocarcinoma (MCF-7), liver (HEPG2) and colon (HCT116) cancer cell lines was evaluated using SRB assay method. Read More

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April 2018
2 Reads

Investigation of the roles of non-neuronal acetylcholine in chronic myeloid leukemic cells and their erythroid or megakaryocytic differentiated lines.

Anticancer Agents Med Chem 2018 Apr 6. Epub 2018 Apr 6.

Marmara University School of medicine - Department of Medical Pharmacology İstanbul. Turkey.

Many studies suggested that acetylcholine (ACh) might serve as an autocrine/ paracrine growth factor in several types of tumors or tumor cell lines. Therefore, cholinergic signaling seems to be functionally important in cancer. High levels of acetylcholinesterase (AChE) activity have been reported in primary brain tumors, ovarian, colon and lung tumors. Read More

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April 2018
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How Does Plasma Activated Media Treatment Differ From Direct Cold Plasma Treatment.

Anticancer Agents Med Chem 2018 Apr 6. Epub 2018 Apr 6.

Plasma Bioscience Research Center/Department of Electrical and Biological Physics, Kwangwoon University, Seoul 01897. Korea.

Objective: The aim of the paper is to investigate the optimum condition for generation of plasma activated media (PAM), where it can deactivate the cancer cells while minimum damage for normal cells.

Background: Over past few years, cold atmospheric plasma-activated media (PAM) have shown its promising application in plasma medicine for treatment of cancer. PAM has a tremendous ability for selective anti-cancer capacity in vitro and in vivo. Read More

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April 2018
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Cytotoxic effect of 5-Fluorouracil-loaded polymer-coated magnetite nanographene oxide combined with radiofrequency.

Anticancer Agents Med Chem 2018 Apr 4. Epub 2018 Apr 4.

Iran University of Medical Sciences - Medical Physics Tehran. Iran.

Despite the development of conventional therapies, include surgery, radiotherapy, chemotherapy and hyperthermia, the prognosis remains very poor. Recently, integration of conventional therapy and multifunctional nanoparticles have attracted a lot of attention because it produces a synergistic effect and better diagnostic and therapeutic efficiency.

Objective: This study aimed to investigate the uptake and cytotoxic effects of polycaprolactone (PCL)/chitosan (CHI)-coated superparamagnetic iron oxide nano-graphene oxide (SPION-NGO) as a carrier of 5-fluorouracil (5-Fu) and radiofrequency (RF) hyperthermia using an alternate magnetic field (AMF) with 13. Read More

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April 2018
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Repositioning of difluorinated propanediones as inhibitors of histone methyltransferases and their biological evaluation in human leukemic cell lines.

Anticancer Agents Med Chem 2018 Apr 4. Epub 2018 Apr 4.

Advanced Centre for Treatment, Research and Education in Cancer, Tata Memorial Centre - Epigenetics and Chromatin Biology Group, Gupta Laboratory, Cancer Research Institute Navi Mumbai, Maharashtra. India.

Cancer chemotherapy is associated with limitations like dose dependent host-tissue toxicity, multiple drug resistance and tumor heterogeneity. Hence, it is imperative to unearth novel targets to cure cancer. At present, 'pharmaco-epigenomics' constitutes the hope in cancer treatment owing to epigenetic deregulation- a reversible process, suspected of playing a role in malignancy. Read More

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April 2018
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Potential future of new glutamate agonists and antagonists development.

Authors:
Dariusz Matosiuk

Anticancer Agents Med Chem 2018 Apr 4. Epub 2018 Apr 4.

Department of Synthesis and Chemical Technology of Pharmaceutical Substances, Faculty of Pharmacy, Medical University of Lublin. Russian Federation.

Receptors of glutamic acid are known for over 30 years for their action and for about 20 years for their structure. Presence of at least three classes of ionotropic receptors was confirmed at the beginning of 80' [1]. Recognition of the sequence [2,3] and first cloning were done at the beginning of 90' [4-6]. Read More

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April 2018
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7-O-aminoalkyl-2,3-dehydrosilibinins: synthesis and in vitro anti-cancer efficacy.

Anticancer Agents Med Chem 2018 Apr 2. Epub 2018 Apr 2.

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

A series of 7-O-aminoalkyl-2,3-dehydrosilibinin derivatives were synthesized and evaluated for their antiproliferative activities against several cancer cell lines. A number of them exhibited greatly enhanced potency with 50% growth inhibition at low micromolar concentrations. Structure activity study indicated that the distance between N and 7-O on the side chain has a limited influence on the antiproliferative activity, while the presence of a morpholino group decreases the antiproliferative activities dramatically. Read More

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April 2018
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Inhibitory Effect of Filipendula ulmaria on Mammary Carcinogenesis Induced by Local Administration of Methylnitrosourea to Target Organ in Rats.

Anticancer Agents Med Chem 2018 Apr 2. Epub 2018 Apr 2.

International Research Centre "Biotechnologies of the Third Millennium", ITMO University, St. Petersburg. Russian Federation.

Background: The meadowsweet (Filipendula ulmaria (L.) Maxim.) may have a cancer prophylactic activity, since its extracts exhibits antioxidant, antiinflammatory and other effects. Read More

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April 2018
3 Reads