Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 21, Issue 4, 2021

Quinacrine (QC) is a tricyclic compound and a derivative of 9-aminoacridine. It has been widely used to treat malaria and other parasitic diseases since the last century. Interestingly, studies have revealed that it also displays anti-cancer activities. Here, we have discussed the anti-cancer mechanism of QC along with its potentiality to specifically target cancer stem cells. The anti-cancer action of this drug includes DNA inte Read More

Cancer is one of the most lethal diseases in the world. Because of the high death rate associated with cancer and the side effects of chemotherapy and radiation therapy, patients require alternative strategies for its treatment. Ginger (Zingiber officinale) has enormous medicinal properties and health benefits. In this review, we discuss the basic mechanism by which gingerol (an active component of ginger) modulates a variety o Read More

Background: The currently available anti breast cancer agents as well as conventional drug delivery methods have some limitations. Objective: In view of these limitations, researchers used phytochemicals/herbal extracts as anti-breast cancer agents together with the polymeric nanoparticles to provide an effective way of targeted drug delivery with lesser /no side effects. Methods: The literature for this review was searched d Read More

Aim: The rapid growth, morbidity and mortality of prostate cancer, and the lack of effective treatment have attracted great interest of researchers to find novel cancer therapies aiming at the effect of gossypin on cell proliferation and apoptosis of PC-3 cells. Methods: The effect of gossypin on cell viability was determined using MTT assay at 5-100μg/ml and cisplatin (50μM) in a time-dependent manner in PC-3 cell lines. The exp Read More

Background: The abnormal signaling from tyrosine kinase causes many types of cancers, including breast cancer, non-small cell lung cancer, and chronic myeloid leukemia. This research reports the in silico, synthesis, and in vitro study of novel pyrimidine derivatives as EGFR inhibitors. Objective: The objective of the research study is to discover more promising lead compounds using the drug discovery process, in which Read More

Background: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as an immunosuppressant, it also possesses anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where the carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, Read More

Background: Recentlty, pyrazoloquinazoline derivatives acquired a special attention due to their wide range of pharmacological activities, especially therapeutic. Through the market, it was found that many pharmacological drugs containing the quinazoline nucleus were known. Objective: The aim of this work is to synthesize target molecules possessing not only anti-tumor activities but also kinase inhibitors. The target molecule Read More

Background: Recently, the Notch signaling pathway has gained attention as a potential therapeutic target for chemotherapeutic intervention. However, the efficacy of previously known Notch inhibitors in colon cancer is still unclear. The purpose of this study was to investigate the effect of andrographolide on aberrantly activated Notch signaling in SW-480 cells in vitro. Methods: The cytostatic potential of andrographolide o Read More

Background and Purpose: Leukemia is considered a top-listed ailment, according to WHO, which contributes to the death of a major population of the world every year. Paris Saponin VII (PS), a saponin which was isolated from the roots of Trillium kamtschaticum, from our group, was reported to provide hemostatic, cytotoxic and antimicrobial activities. However, its molecular mechanism underlying the anti-proliferative effects Read More

Background: A Chinese folk medicine plant Pleurospermum lindleyanum possesses pharmacological activities of heat-clearing, detoxifying and preventing from hepatopathy, coronary heart disease, hypertension, and high altitude sickness. We isolated and characterized its constituents to investigate its synergistic effects against human hepatoma SMMC-7721 cells. Objective: The aim of this study was to explore the synergi Read More

Background: Compounds with biological activities had been reported in the jackfruit. These compounds are susceptible to structural changes such as isomerization and/or loss of bonds due to environmental factors. Then, the encapsulation for protecting is a necessary process. Objective: In this study, encapsulation of High-Value Biological Compounds (HVBC) was performed using High Degree of Polymerization Agave Fructans (H Read More

Aim: The aim of this study is to explore the therapeutic potential of S-allylcysteine (SAC) organosulphur compound as a potent immune checkpoint inhibitor PD-L1. Background: Natural compounds have been showing tremendous anticancerous potential via suppressing the expression of genes involved in the development and progression of several carcinomas. This has further motivated us to explore the therapeutic potential o Read More