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- Volume 18, Issue 11, 2018
Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 18, Issue 11, 2018
Volume 18, Issue 11, 2018
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Computational Study of the Binding Modes of Diverse DPN Analogues on Estrogen Receptors (ER) and the Biological Evaluation of a New Potential Antiestrogenic Ligand
Estrogen (17β-estradiol) is essential for normal growth and differentiation in the mammary gland. In the last three decades, previous investigations have revealed that Estrogen Receptor Alpha (ERα) plays a critical role in breast cancer. More recently, observations regarding the widespread expression of ERβ-like proteins in normal and neoplastic mammary tissues have suggested that ERβ is also involved in the mentioned pa Read More
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Determination of the Apoptotic Effect and Molecular Docking of Benzamide Derivative XT5 in K562 Cells
Background: The tyrosine kinase inhibitor, imatinib, used as a first line treatment in Chronic Myeloid Leukemia (CML) patients, may lead to resistance and failure to therapy. Novel combinations of imatinib with other drugs is a strategy to improve treatment efficiency. Objective: In this study, the antileukemic and apoptotic effects of a benzamide derivative XT5 and benzoxazole derivative XT2B and their combination wit Read More
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Synthesis and Biological Evaluation of Novel Triazoles Linked 7-hydroxycoumarin as Potent Cytotoxic Agents
Authors: Saleem Farooq, Aashiq Hussain, Mushtaq A. Qurishi, Abid Hamid and S. KoulBackground: BacCancer is regarded as second leading cause of death worldwide. Therefore, there is a high demand for the discovery, development and improvement of novel anti-cancer agents which could efficiently prevent proliferative pathways and clonal expansion of cells. Objective: In view of this, a new series of bioactive scaffolds viz triazoles linked 7-hydroxycoumarin (1) were synthesized using click che Read More
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Exploring the Lapse in Druggability: Sequence Analysis, Structural Dynamics and Binding Site Characterization of K-RasG12C Variant, a Feasible Oncotherapeutics Target
Authors: Emmanuel A. Adeniji, Fisayo A. Olotu and Mahmoud E.S. SolimanBackground: The difficulty in druggability of K-Ras variant has presented a challenge in the treatment of cancer diseases associated with its dysfunctionality. Despite the identification of different binding sites, limited information exists in the literature about their characteristics. Therefore, identification, crossvalidation and characterization of its druggable sites would aid the design of chemical compounds that will arrest its Read More
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Novel Anthraquinone Derivatives as Dual Inhibitors of Topoisomerase 2 and Casein Kinase 2: In Silico Studies, Synthesis and Biological Evaluation on Leukemic Cell Lines
Authors: Abbas Kabir, Kalpana Tilekar, Neha Upadhyay and C.S. RamaaBackground: Cancer being a complex disease, single targeting agents remain 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 a multitude of protein targets. Thus, in the present Read More
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Pinocembrin-Enriched Fractions of Elytranthe parasitica (L.) Danser Modulates Apoptotic and MAPK Cellular Signaling in HepG2 Cells
Background: Hepatocellular carcinoma (HCC) is the fifth leading cause of cáncer mortality. Elytranthe parasitica (L.) Danser (EP), a hemiparasitic plant (Loranthaceae) has potent anti-cancer properties. Objective: In the study, we investigated the effect of EP fractions on the expression of apoptosis and mitogenactivated protein kinase (MAPK) markers deregulated in HCC. Bioactivity fractionation was performed to isolate th Read More
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Peniciketal A, A Novel Spiroketal Compound, Exerts Anticancer Effects by Inhibiting Cell Proliferation, Migration and Invasion of A549 Lung Cancer Cells
Authors: Xue Gao, Yuming Zhou, Xiaoqi Zheng, Hongliu Sun, Jing Zhang, Weizhong Liu and Xiaohong PanBackground: 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. Metheds: Cell proliferation was tested by MTT assay and colony formation assay. Flow cytometry was per Read More
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Bursal Hexapeptide, A Potential Immunomodulator, Inhibits Tumor Cells Proliferation via p53 Signaling Pathway
Authors: Cong Zhang, Jiangfei Zhou, Shengnan Li, Kairui Cai, Xiangling Guo, Chengshui Liao and Chen WangBackground: The Bursa of Fabricius (BF) is acknowledged as the 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. Method: In this paper, Gene microarray analyses demonstrated that BHP regu Read More
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Novel Nicotinonitrile Derivatives Bearing Imino Moieties Enhance Apoptosis and Inhibit Tyrosine Kinase
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 the reaction of hydrazonoyl chlorides with each of 4-(4- methoxyphenyl)-3-methyl-6-oxo-6,7-dihydro Read More
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Lichen Acids May Be Used as A Potential Drug For Cancer Therapy; by Inhibiting Mitochondrial Thioredoxin Reductase Purified From Rat Lung
Authors: Ilknur Ozgencli, Harun Budak, Mehmet Ciftci and Mustafa AnarBackground: Thioredoxin reductase (E.C 1.6.4.5.; TrxR) is a widely distributed flavoprotein that catalyzes the NADPH-dependent reduction of thioredoxin (Trx) in many cellular events such as DNA synthesis, DNA repair, angiogenesis, antioxidative defense, and regulating apoptosis. Although TrxR is indispensible in protecting cells against oxidative stress, the overexpression of TrxR is seen in many aggressive tumors. Read More
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Synthesis and Evaluation of a Series of 1,3,4-Thiadiazole Derivatives as Potential Anticancer Agents
Background and Methods: In an attempt to develop potent antitumor agents, the synthesis of a series of N-(6-substituted benzothiazol-2-yl)-2-[(5-(arylamino)-1,3,4-thiadiazol-2-yl)thio]acetamides (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 investi Read More
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TPEN Exerts Antitumor Efficacy in Murine Mammary Adenocarcinoma Through an H2O2 Signaling Mechanism Dependent on Caspase-3
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 TPENinduced cell death in mammary adenocarcinoma cells in vitro and in vivo are still unclear. Objective: This study aimed t Read More
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Selection of a GPER1 Ligand via Ligand-based Virtual Screening Coupled to Molecular Dynamics Simulations and Its Anti-proliferative Effects on Breast Cancer Cells
Background: Recent reports have demonstrated the role of the G Protein-Coupled Estrogen Receptor 1 (GPER1) on the proliferation of breast cancer. The coupling of GPER1 to estrogen triggers cellular signaling pathways related to cell proliferation. Objective: Develop new therapeutic strategies against breast cancer. Method: We performed in silico studies to explore the binding mechanism of a set of G15 /G1 analogue Read More
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Synthesis and Anticancer Activity of 9-O-Pyrazole Alkyl Substituted Berberine Derivatives
Authors: Daipeng Xiao, Fen He, Dongming Peng, Min Zou, Junying Peng, Pan Liu, Yanfei Liu and Zhenbao LiuBackground: Berberine (BBR), an isoquinoline plant alkaloid isolated from plants such as Coptis chinensis and Hydrastis canadensis, own multiple pharmacological activities. Objective: In this study, seven BBR derivatives were synthesized and their anticancer activity against HeLa cervical and A549 human lung cancer cell lines were evaluated in vitro. Methods: The anti-cancer activity was measured by MTT assay, and apoptosi Read More
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Volumes & issues
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Volume 25 (2025)
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Volume 24 (2024)
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Volume 23 (2023)
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Volume 22 (2022)
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Volume 21 (2021)
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Volume 20 (2020)
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Volume 19 (2019)
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Volume 18 (2018)
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Volume 17 (2017)
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Volume 16 (2016)
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Volume 15 (2015)
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Volume 14 (2014)
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Volume 13 (2013)
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Volume 12 (2012)
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Volume 11 (2011)
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Volume 10 (2010)
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Volume 9 (2009)
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Volume 8 (2008)
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Volume 7 (2007)
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Volume 6 (2006)
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