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- Volume 17, Issue 1, 2017
Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 17, Issue 1, 2017
Volume 17, Issue 1, 2017
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Thiol-Activated Anticancer Agents: The State of the Art
The thiol or sulfhydryl group, as part of low molecular weight non-peptide biomolecules, as well as part of the cysteine residues in peptides and proteins, is known to play extremely important roles in several aspects of cellular function. Glutathione (γ-Glu-Cys-Gly; GSH) is the most abundant thiol-containing peptide in mammals, being present intracellularly in the low millimolar concentration range, but only in the low micromo Read More
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Anticancer Drug Combinations, How Far We can Go Through?
Authors: Da-Yong Lu, En-Hong Chen, Hong-Ying Wu, Ting-Ren Lu, Bin Xu and Jian DingMany clinical cancer therapies are less effective by using one anticancer drug only due to refractory properties of cancer pathogenesis and drug resistance property in advanced cancer patients. A general consensus among clinicians is that anticancer drug cocktail might better control cancer progresses and metastasis than single drug therapeutics in clinical trials. Despite great popularity, the anticancer drug combination dog Read More
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Ruthenium(II) Complexes as Potential Apoptosis Inducers in Chemotherapy
Authors: Kangdi Zheng, Qiong Wu, Chengxi Wang, Weijun Tan and Wenjie MeiHerein, the development of ruthenium complexes as potential apoptosis inducers, as well as their underlying mechanism has been reviewed. In recent years, various ruthenium complexes have been designed and their in vitro and in vivo inhibitory activities against various types of tumor cells have been evaluated extensively. It’s demonstrated that ruthenium complexes can induce apoptosis of tumor cells through the sign Read More
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Killing Glioma ‘Stem-like’ Cells via Drug-Induced Relocation of Endosomal Urokinase Proteins
Authors: Fredric A. Gorin, Nagarekha Pasupuleti, Dinesh Mahajan and Sundeep DugarHigh grade gliomas (HGGs) are primary CNS cancers with more than 95% of patients experiencing tumor recurrence following radiation therapy, chemotherapy, and/or an anti-angiogenic therapy. Populations of glioma ‘stem-like’ cells (GSCs) exist in both proliferative and non-proliferative states and are capable of tumor regrowth. These GSCs survive within hypoxic tumor regions and avascular tumor margins, while retaini Read More
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Rapamycin-loaded Immunoliposomes Functionalized with Trastuzumab: A Strategy to Enhance Cytotoxicity to HER2-positive Breast Cancer Cells
Background: Liposomes have been employed to improve pharmacokinetics and reduce side effects of drugs. They can be functionalized with antibodies for targeted delivery. While the monoclonal antibody trastuzumab has been employed in the therapy of HER2-positive breast cancer, the resistance developed during treatment has been reported. Rapamycin could be used in combination with trastuzumab for improved the Read More
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Novel 2-Thienyl- and 2-Benzothienyl-Substituted 6-(2-Imidazolinyl)Benzothiazoles: Synthesis; in vitro Evaluation of Antitumor Effects and Assessment of Mitochondrial Toxicity
Background: Differently substituted thiophenes are largely studied due to their diverse pharmacological properties, especially anticancer activity. Recent studies have reported on interesting benzothiophene compounds antitumor properties and we also recently reported on the synthesis, strong antitumor activities and DNA binding features of substituted thieno[3',2':4,5]thieno- and benzo[b]thieno[2,3-c]quinolones, containi Read More
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Design, Synthesis and Evaluation of 5-pyridin-4-yl-2-thioxo-[1,3,4]oxadiazol-3-yl Derivatives as Anti-angiogenic Agents Targeting VEGFR-2
Background: Angiogenesis is physiological process in embryogenesis, organ development, endometrial vasculature in menstrual cycle and wound healing. Angiogenesis has also been associated with several pathological conditions such as cancer, arthritis, atherosclerosis, etc. Out of the many growth factor responsible for angiogenesis, vascular endothelial growth factor (VEGF) is one of the most important and positive regulato Read More
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Synthesis, in vitro Antiproliferative and Antiinflammatory Activities, and Kinase Inhibitory effects of New 1,3,4-triarylpyrazole Derivatives
Background: Pyrazole derivatives have been reported as both anticancer and antiinflammatory agents. Objective: This study was conducted to develop new pyrazole derivatives as potential anticancer and/or antiinflammatory agents. Their molecular mechanisms of action have been investigated. Method: a series of new triarylpyrazole derivatives were synthesized. Their in vitro anticancer activity was tested against N Read More
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New 2-Imino-2H-Chromene-3(N-aryl)carboxamides as Potential Cytotoxic Agents
Authors: Rupinder Kaur Gill, Jyoti Kumari and Jitender BariwalSynthesis and structure activity relationships of four series of novel 2-imino-2H-chromene-3(N-aryl) carboxamides (V-VIII) have been described by bioisosteric replacement of usually present ketone at 2nd position of coumarin with imine. Various substitutents are introduced on aryl and chromene ring of iminocoumarin to investigate the effect of lipophilicity and electronic properties of substituents on cytotoxic activity ag Read More
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Effect of PUFAs Oral Administration on the Amount of Apoptotic Caspases Enzymes in Gastric Cancer Patients Undergoing Chemotherapy
Objective: Gastric cancer is the fourth most common cancer and the second cause of death in the world. According to the studies, the gastric cancer is relatively sensitive to chemotherapy. The aim of this study was to investigate the association of oral administer PUFAs with Caspase enzymes in patients with gastric cancer under chemotherapy. Methods: This study was a Clinical Trial in which the target group consisted Read More
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Glycodendrimer PPI as a Potential Drug in Chronic Lymphocytic Leukaemia. The Influence of Glycodendrimer on Apoptosis in In Vitro B-CLL Cells Defined by Microarrays
Background: Chronic lymphocytic leukaemia (CLL) cells are characterized by failures in the apoptosis pathway and increased proliferation, resulting in the progressive accumulation of B-lymphocytes in blood. Despite the wide range of antileukaemic drugs, CLL remains an incurable disease. However, a breakthrough is expected which will allow more effective treatment. Objective: The study investigates the influence of poly(p Read More
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Induction of Autophagic Cell Death in Apoptosis-resistant Pancreatic Cancer Cells using Benzo[α]phenoxazines Derivatives, 10-methyl-benzo[α]phenoxazine-5-one and benzo[α]phenoxazine-5-one
Authors: Sanjima Pal, Sunita Salunke-Gawalib and V. Badireenath KonkimallaaBackground: Intrinsic resistance to apoptotic cell death due to co-occurrence of mutated KRAS and p53 is frequently reported in pancreatic cancer that renders them aggressive, highly proliferative and metastatic. In addition, these cancer types are less sensitive to apoptosis inducing drugs where promotion of autophagic cell death could be a viable option for treatment under such circumstances. Objective: In this study we Read More
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In Vivo Performance of a Ruthenium-cyclopentadienyl Compound in an Orthotopic Triple Negative Breast Cancer Model
Background: Ruthenium-based anti-cancer compounds are proposed as viable alternatives that might circumvent the disadvantages of platinum-based drugs, the only metallodrugs in clinical use for chemotherapy. Organometallic complexes in particular hold great potential as alternative therapeutic agents since their cytotoxicity involves different modes of action and present reduced toxicity profiles. Objective: During the Read More
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Synthesis of Icaritin and β-anhydroicaritin Mannich Base Derivatives and Their Cytotoxic Activities on Three Human Cancer Cell Lines
Authors: Van-Son Nguyen, Ling Shi, Sheng-Chun Wang and Qiu-An WangBackground: Prenyl flavonoid icaritin (1) and β-anhydroicaritin (2) are two natural products with important biological and pharmacological effects. such as antiosteoporosis, estrogen regulation and antitumor properties. Objective: The present study investigates the synthesis and cytotoxic activities on three Human cancer cell lines (Hela, HCC1954 and SK-OV-3) of icaritin and β-anhydroicaritin Mannich base derivatives in vitr Read More
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Cordycepin Affects Multiple Apoptotic Pathways to Mediate Hepatocellular Carcinoma Cell Death
Authors: Yulin Zhou, Zhihua Guo, Qingfan Meng, Jiahui Lu, Ning Wang, Hui Liu, Qiming Liang, Yutong Quan, Di Wang and Jing XieBackground: Cordycepin possesses anti-inflammatory, anti-metastatic and anti-tumor properties. Objective: The present study investigates the anti-hepatocellular carcinoma activities of cordycepin in in vitro and in vivo models. Method: Cell viability, apoptosis rate, intracellular reactive oxygen species (ROS) level and mitochondrial membrane potential (MMP) were determined by 3-(4,5)-dimethylthiahiazo(-z-y1)-3,5-di-phenytetr 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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