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- Volume 21, Issue 16, 2021
Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 21, Issue 16, 2021
Volume 21, Issue 16, 2021
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Sanguinarine: A Double-Edged Sword of Anticancer and Carcinogenesis and Its Future Application Prospect
Authors: Guanhua Lou, Jin Wang, Ju Hu, Qingxia Gan, Chengyi Peng, Haijun Xiong and Qinwan HuangBackground: Sanguinarine, a kind of benzophenanthridine alkaloid, is a natural compound with potential development value for its anticancer activity. Hundreds of studies have been carried out in vivo or in vitro, trying to make it feasible for the anticancer clinic medication of sanguinarine. However, sanguinarine was branded as a toxicant or even a carcinogen according to some toxicological experiments and cancer investi Read More
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Cell Arrest and Apoptosis Induced by the Next Generation of Vanadium Based Drugs: Action Mechanism to Structure Relation and Future Perspectives
Authors: Manos C. Vlasiou and Kyriaki S. PafitiBackground: Every year, we encounter more projects indicating the promising anticancer activity of vanadium molecules against different types of cancer cells. The new generation of metal-based drugs, targets the energy supplies of the cell through ROS generation leading them to cell arrest and apoptosis. The relatively low toxicity of vanadium metal, the different oxidation states that it can occur and in general, the lipophilici Read More
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Therapeutic Potential of Polyphenols and their Nanoformulations in the Treatment of Colorectal Cancer
Authors: Shaheer H. Khan, Fahad A. Alhumaydhi, Masood A. Khan and Hina YounusBackground: Colorectal Cancer (CRC) ranks third among all cancer-related deaths around the globe. Chemotherapy may prolong the survival of CRC patients to some extent, but its clinical use is associated with grave side effects on overall health. Contrary to chemotherapy, the use of plant-derived therapeutic molecules offered advantages because of their reduced toxicity. Polyphenol is a group of phytochemicals that impar Read More
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Mitophagy in Carcinogenesis and Tumour Progression- A New Paradigm with Emerging Importance
Authors: Suman K. Ray and Sukhes MukherjeeThe term Mitophagy has been newly concerned in reforming the metabolic landscape inside cancerous cells in addition to the interface between malignant cells as well as other major constituents of tumour microenvironment. Several profoundly interrelated systems, comprising mitochondrial dynamics and mitophagy, function in mammalian cells as vital mitochondrial regulator processes, and their consequence i Read More
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COVID-19: Our Current Knowledge of Epidemiology, Pathology, Therapeutic Approaches, and Diagnostic Methods
Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) firstly emerged in Wuhan, China at the end of 2019. After going through the experimental process, the virus was named the novel coronavirus (2019-nCoV) by the World Health Organization (WHO) in February 2020 which has created a global pandemic. The coronavirus disease 2019 (COVID-19) infection is challenging the people who are especially suffering fro Read More
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Dual Human Carbonic Anhydrase/Cyclooxygenase-2 Inhibitors: A Promising Approach for Cancer Treatment
Authors: Mohammad Mahboubi-Rabbani and Afshin ZarghiHuman Carbonic Anhydrase (hCA) and Cyclooxygenase-2 (COX-2) have been known for a long to be chiefly involved in both the pathogenesis and progression of cancer and cancer chemoresistance. Interestingly, there is considerable evidence that the sulfonamide-type COX-2 selective inhibitors (coxibs) demonstrate inhibitory action against the cancer-related hCA isoforms, confirmed by X-ray crystal structures for celec Read More
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Antiproliferative and Pro-Apoptotic Effects of Thiazolo[3,2–b][1,2,4]triazoles in Breast and Cervical Cancer Cells
Authors: Imtiaz Khan, Sumera Zaib, Mohsin Javed, Faisal Rashid, Jamshed Iqbal and Aliya IbrarBackground and Objectives: Cancer is one of the leading causes of death in the world affecting millions of people. The commercially available anticancer drugs lack the selectivity and show several undue side effects during the biologically targeted therapy, thus calling for the exploration of wider chemical space to furnish new structural leads with promising anticancer potential. In this endeavor, we synthesized a series of co Read More
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Neurokinin-1 Receptor Antagonist Can Prevent the Delayed Phase in Patients: A Single Center Retrospect Study
Authors: Jing Xu, Shuhui Tang, Jie Li, Wei Wang, Meihong Wu and Xianbao ZhanBackground: Neurokinin-1 receptor antagonists are playing a major advance in Chemotherapy-Induced Nausea and Vomiting (CINV) as powerful prophylactic agents. Therefore, it is significant to find the association between risk factors of patients and CINV so as to adjust the anti-emetic regimens. Objective: To evaluate the role of Neurokinin-1 Receptor (NK-1R) antagonist in preventing chemotherapy-induced vomiting in t Read More
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Hepatitis B Virus X Protein Modulates Chemokine CCL15 Upregulation in Hepatocellular Carcinoma
Authors: Ying Li, Chaomin Wang, Ting Zhao, Ranliang Cui, Linfei Hu, Luchen Chang, Xi Wei, Jin Zhang and Yueguo LiBackground: Hepatitis B virus X protein (HBx) is an indispensable progression factor in Hepatocellular Carcinoma (HCC). CCL15 could be a peculiar proteomic biomarker of HCC with tumorigenesis and tumor invasion. Objective: The aim of the study was to explore the relationship between HBx and CCL15 expression in HCC. Methods: HBV-positive HCC pathological tissue samples and corresponding adjacent non-tumor liver tissu Read More
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Synergistic Interactions between GW8510 and Gemcitabine in an In Vitro Model of Pancreatic Cancer
Authors: Duygu G. Rüstem, Sevcan Atay, Hikmet Hakan Aydin and Handan AkBackground: One of the main reasons for the poor survival rates of pancreatic cancer patients is the development of gemcitabine resistance, indicating that novel treatment strategies that have the ability to improve gemcitabine sensitivity are in need to combat this devastating disease. Methods: TCGA PAAD data was used to determine the clinicopathological significance of high RRM2 (Ribonucleotide reductase subunit M Read More
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Synthesis, Characterization and Biological Evaluation of Indole-Pyrazole Amalgamated α-Cyano Substituted Chalcones
Authors: Pravin S. Bhale, Sadanand N. Shringare, Amol B. Khade and Hemant V. ChavanBackground: Indole and pyrazole constitute a major class of biologically active scaffolds. The amalgamation of two or more pharmacophores would generate novel molecular templates that are likely to unveil remarkable biological properties. Objective: An efficient and high yielding synthesis of indole-pyrazole integrated α-cyano substituted chalcones and their in vitro anti-breast cancer and antioxidant evaluation. Methods: The Read More
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Carvacrol Exhibits Chemopreventive Potential against Cervical Cancer Cells via Caspase-Dependent Apoptosis and Abrogation of Cell Cycle Progression
Authors: Afza Ahmad and Irfan A. AnsariBackground: The carcinogenesis of the uterine cervix is predominantly initiated with the consistent infection of the Human Papilloma Virus (HPV). Owing to the side effects of standard chemotherapeutics in the treatment of recurrent and metastatic cervical cancer, there is a need for a better and effective treatment modality. In this lieu of concern, natural compounds have proven their worthwhile potential against the treatme Read More
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Platelet-Rich and Platelet-Poor Plasma Might Play Supportive Roles in Cancer Cell Culture: A Replacement for Fetal Bovine Serum?
Background: Platelet-Rich (PRP) and Platelet-Poor plasma (PPP) are widely used in research and clinical platforms mainly due to their capacities to enhance cell growth. Although the short half-life (5 days) and the high price of platelet products pose challenges regarding their usage, they maintain the growth regulatory functions for weeks. Thus, we aimed to assess the supplementary values of these products in human CC Read More
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The Synergistic Cytotoxic and Apoptotic Effect of Resveratrol and Naringenin on Y79 Retinoblastoma Cell Line
Background: Resveratrol is a phenolic natural product, which is found in red grapes and in Japanese knotweed root (Polygonum cuspidatum). Naringenin is one of the flavonoid compounds found in landing grape and other citrus fruits. Both agents exert antioxidant and anti-inflammatory properties. Objective: In this study, the effect of Resveratrol and Naringenin in an in vitro model of retinoblastoma of the eye has been in Read More
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Antimutagenic, Antiproliferative and Antioxidant Properties of Sea Grape Leaf Extract Fractions (Coccoloba uvifera L.)
Background: Cancer is a disease characterized by the invasion and uncontrolled growth of cells. One of the best ways to minimize the harmful effects of mutagens is through the use of natural antimutagens. In this regard, the search for new antimutagens that act in the chemoprevention could represent a promising field in this area. Objective: In this study biological potential of 11 fractions from Coccoloba uvifera L. leaf h Read More
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The Uses of Dimedone for the Synthesis of Thiophene, Thiazole and Annulated Derivatives with Antitumor, Pim-1 Kinase Inhibitions, PAINS Evaluations and Molecular Docking
Authors: Wagnat W. Wardakhan, Amira M. Elmetwally, Abeer A. Mohamed and Rafat M. MoharebBackground: Dimedone is considered as one of the most important classes of compounds belonging to cyclohexan-1,3-dione. Such groups of compounds were considered as precursors for many pharmaceutically active heterocyclic compounds. Objective: The target molecules in this work were synthesized from arylhydrazones of dimedone with different substituents enhancing the study of their structure-activity relationshi Read More
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Discovery of Potent Natural-Product-Derived SIRT2 Inhibitors Using Structure- Based Exploration of SIRT2 Pharmacophoric Space Coupled With QSAR Analyses
Authors: Mohammad A. Khanfar and Saja AlqtaishatBackground: SIRT2 belongs to a class III of Histone Deacetylase (HDAC) and has crucial roles in neurodegeneration and malignancy. Objective: The objective of this study is to discover structurally novel natural-product-derived SIRT2 inhibitors. Methods: Structure-based pharmacophore modeling integrated with validated QSAR analysis was implemented to discover structurally novel SIRT2 inhibitors from the natural products datab 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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