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- Volume 16, Issue 12, 2016
Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 16, Issue 12, 2016
Volume 16, Issue 12, 2016
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Statins and Alkylphospholipids as New Anticancer Agents Targeting Lipid Metabolism
More LessThe partial efficacy and high toxicity of the current anticancer chemotherapeutics as well as the development of multiple drug resistance are the major problems in cancer therapy. Therefore, there is an emergency need for the development of novel well-tolerated anticancer agents with different mode of action that could be successfully used in combination with other drugs as an adjuvant therapy. The inhibition of intrace Read More
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Brain-metastatic Breast Cancer: Clinical Considerations and Pharmacological Approaches
Authors: Ana C. Andrade, Daniel S. Ferruzzi and Carolina PanisDespite constant advances on breast cancer knowledge, the metastatic disease resulting from the spreading of this disease is still a challenge. This scenario is particularly critical in the more aggressive subtypes, as HER2-amplified and triple negative breast cancers, when often occurs the invasion of central nervous system (CNS) structures. In this situation, the survival of patients is drastically reduced, and the number of s Read More
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Circulating Tumor Cells: A New Window for Diagnosis and Evaluation of Cancer
Authors: Meihui Liu, Min Tang, Ming Li, Feng Gao, Can Shi, Jing Hou and Wenbin ZengAs the ever more critical role of individualized therapy in the cancer treatment and management, circulating tumor cells (CTCs) have caught much attention for providing a promising way in metastases establishment, disease diagnosis and prognosis. Also, their presence has been generally considered as the rationale behind the application of systemic adjuvant chemotherapy. Therefore, CTCs open a new window for the clini Read More
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Peroxisome Proliferator-Activated Receptors and their Ligands in Cancer Drug- Resistance: Opportunity or Challenge
Authors: Bahman Yousefi, Nosratollah Zarghami, Nasser Samadi and Maryam MajidiniaDevelopment of resistance in cancer cells results in a high failure rate in cancer chemotherapy in the clinic. Therefore, investigating the mechanisms by which cancer cells acquire the capability to avoid cell death upon exposure to antineoplastic agents is of great significance in cancer research. In this review article, we will provide an overview of the mechanisms and molecular machinery of drug resistance in ca Read More
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Novel Therapeutic Strategies Against Cancer: Marine-derived Drugs May Be the Answer?
More LessMarine ecosystem represents a wide and untapped reservoir of biologically active metabolites. Most of the sponges, seaweeds, crustaceans, fish species and their associated microorganisms have evolved chemical means in order to defend themselves against predation and to survive in the complex marine environment. Such chemical and biological adaptation produced many bioactive substances with beneficial effects on h Read More
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Mutant B-Raf Kinase Inhibitors as Anticancer Agents
Authors: Vivek Asati, Sanjay K. Bharti and Debarshi K. MahapatraThe Ras/Raf/MEK/ERK signaling pathway involves various kinases in which each kinase is associated with one another through signals and regulates cell proliferation, differentiation and apoptosis. This pathway is dysregulated almost in all cancers due to the amplification and genetic mutation of various components of the pathway. The genetic mutations have been reported to cause drug resistance to the current chemotherapy o Read More
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Selective Toxicity of Apigenin on Cancerous Hepatocytes by Directly Targeting their Mitochondria
Authors: Enayatollah Seydi, Hamid R. Rasekh, Ahmad Salimi, Zhaleh Mohsenifar and Jalal PourahmadBackground: hepatocellular carcinoma (HCC) is the third cause of mortality due to cancer throughout the world. Objective: The main goal of the current research was to evaluate the selective toxicity of apigenin (APG) on hepatocytes and mitochondria obtained from the liver of HCC rats). Method: In this research, HCC induced by a single dose of diethylnitrosamine (DEN); 200 mg/kg, i.p, and 2-acetylaminofluorene (2-AAF) ( Read More
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Synthesis and in vitro Evaluation of the Anticancer Potential of New Aminoalkanol Derivatives of Xanthone
A series of 15 derivatives of xanthone were synthesized and evaluated for the anticancer activity. The structure of the tested compounds was diversified to establish structureactivity relationships. The following evaluations were carried out: cytotoxicity-proliferation tests, apoptosis detection, expression of apoptosis and proliferation-related genes, expression and activity of gelatinases A and B, wound migration assa Read More
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In Vivo Inhibition of Proteasome Activity and Tumour Growth by Murraya koenigii Leaf Extract in Breast Cancer Xenografts and by Its Active Flavonoids in Breast Cancer Cells
Inhibition of the 26S proteasome is an attractive approach for anticancer therapy. Proteasome inhibitors are known to selectively target cancer cells and make them more sensitive to chemotherapeutic agents. Murraya koenigii is a medicinally important herb of Asian origin and a rich source of bioactive compounds such as flavonoids and alkaloids. In the present study, we investigated the proteasome inhibitory and apoptotic Read More
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Aryl Maleimides as Apoptosis Inducers on L5178-Y Murine Leukemia Cells (in silico, in vitro and ex vivo Study)
Thiol reagents were shown to act as potent inhibitors of L5178-Y murine leukemia cell proliferation. A series of aryl maleimides (AMI) was synthesized and evaluated theoretically for global and local reactivity, showing their selectivity for thiol groups, due to a reaction of the vinyl moiety (a soft acid) with thiols (a soft base). Two AMI that are benzoic acid derivatives (1f and 1h) were tested with an in vitro and ex vivo model Read More
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A Novel Method to Synthesize 4-Aryl-1H-1,2,3-Triazoles and its Antihepatoma Activity
Authors: Xiaolong Li, Yun He, Li Hai, Tao Zhang and Yong WuA novel synthetic method of 4-substituted aryl-1H-1,2,3-triazoles from arylglyoxaldoxime semicarbazone with sodium dithionite and O2 was found to be safer than the Huisgen azide– alkyne dipolar cycloaddition. A total of 17 new structures of 4-substituted aryl-1H-1,2,3- triazoles were characterized by 1H NMR, 13C NMR, ESI-MS. Subsequently, their in vitro antihepatoma activities were evaluated on human hepatoma Q Read More
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Trans-platinum(II)/(IV) Complexes with Acetylpyridine Ligands as Antivascular Agents in vitro: Cytotoxic and Antiangiogenic Potential
In vitro biological studies of four trans-platinum complexes of structural formulas trans-[PtCl2(n-acetylpyridine)2] (n = 3 or 4, complex 1 or 2) and [Pt(n-acetylpyridine)2Cl4] (n = 3 or 4, complex 3 or 4) were performed in human endothelial EA.hy 926 cells, in order to evaluate and compare their cytotoxic and antiangiogenic potential. MTT results revealed that trans-Pt(II) complexes exhibited significantly lower IC50 values: 4. Read More
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The cytotoxic effect of GW843682X on nasopharyngeal carcinoma
Authors: Qinyong Hu, Yuxin Chu, Weiguo Hu, Min Peng and Qibin SongBackground: GW843682X is a publicly available anti-cancer compound by inhibiting Polo-like kinase. Previous studies revealed that GW843682X inhibited the proliferation of various tumor cell lines. In this study, the cytotoxic effect of GW843682X was investigated on cell proliferation, cell cycle and apoptosis of nasopharyngeal carcinoma 5-8F cells. Methods: Cell morphological changes were observed by inverted microsco Read More
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In Vitro Anticancer Effects of Two New Potent Hydrazide Compounds on Leukemic Cells
Background: Chronic myeloid leukemia (CML), also recognized as chronic myelogenous leukemia, is initiated in some types of blood-forming cells of the bone marrow. The therapeutic approach to CML is usually chemotherapy; however, severe side effects and complications are major problems in the clinical research. Thus, recent efforts have focused on the search for compounds affecting apoptosis in this type of cancer. Object Read More
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4-Anilinoquinazoline Derivatives with Epidermal Growth Factor Receptor Inhibitor Activity
Authors: Fang Liu, Baoding Tang, Hao Liu, Leina Li, Gang Liu, Yun Cheng, Yan Xu, Wenwen Chen and Yinjiu Huang4-Anilinoquinazoline derivatives possess high anti-cancer activities. Many of them are highly selective tyrosine kinase inhibitors (TKI), particularly against epidermal growth factor receptor (EGFR). EGFRs are overexpressed or mutated in most carcinomas and are required for tumor progression. The efficacy of EGFR-targeted anti-tumor drugs is impaired by drug-induced acquired resistance. Therefore, there is urgen Read More
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Pyrrolidino Analogues of Gefitinib with Improved EGFR Inhibition, Cancer Cell Cytotoxicity, and Pharmacokinetic Properties
Authors: Jing-Kun Fang, Zhimin Xu, Yingjun Zhang, Weihong Zhang, Bing Liu, Yu Fang and Tengxiao SunThe binding mode analysis of Gefitinib revealed that 6-propylmorpholino group (sidechain) shows no interactions due to its weak electron density. In order to modify the electron density of Gefitinib’s sidechain, novel pyrrolidino analogs of Gefitinib where morpholino groups were replaced by substituted pyrrolidino groups were synthesized. Gefitinib derivatives with high electronegativity atoms or groups in the pyrrolidino moiet 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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