Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 24, Issue 15, 2024

Background: Globally, colorectal cancer (CRC) is categorized as the third type of cancer associated with mortalities. Chemotherapeutic drugs such as cisplatin can be used to treat cancer-affected patients. However, several adverse effects are associated with its application. This motivated the researchers to search for alternatives that are more efficient and have fewer undesirable effects. Kolaviron is a bioflavonoid that has be Read More

Aims: Validating the docking procedure and maintaining the structural water molecules at HDAC8 catalytic site. Background: Molecular docking simulations play a significant role in Computer-Aided Drug Design, contributing to the development of new molecules. To ensure the reliability of these simulations, a validation process called "self-docking or re-docking" is employed, focusing on the binding mode of a ligand co-cryst Read More

Background: Drug resistance has been a problem in cancer chemotherapy, which often causes shortterm effectiveness. Further, the literature indicates that telomere G-quadruplex could be a promising anti-cancer target. Objective: We synthesized and characterized two new pyrimidine derivatives as ligands for G-quadruplex DNA. Methods: The interaction of novel non-cationic and cationic pyrimidine derivatives (3a, b) w Read More

Background: Non-Small Cell Lung Cancer (NSCLC) ranks as a leading cause of cancer-related mortality, necessitating the urgent search for cost-effective and efficient anti-NSCLC drugs. Our preliminary research has demonstrated that arsenic trioxide (ATO) significantly inhibits NSCLC angiogenesis, exerting anti-tumor effects. In conjunction with existing literature reports, the Nrf2-IL-33 pathway is emerging as a novel Read More

Background: Chronic myelogenous leukemia (CML) is an uncommon type of cancer of the bone marrow associated with high mortality. Although several effective therapies have been developed to reduce symptoms in patients with CML, many of these methods are associated with side effects. Coreopsis tinctoria Nutt. (C. tinctoria) is a natural medicinal material that possesses antioxidant and anticancer activities. Yet, its Read More

Background: The Fibroblast Growth Factor Receptor-1 (FGFR-1) is a tyrosine kinase and a validated target for the treatment of different cancer types. Objective: Design and synthesis of novel thiazole-based analogues of anticancer agents. Methods: Series of 2-aryl-5-methylthiazole analogues linked to structurally variable basic heads were synthesized as novel anticancer agents. Developed compounds were tested f Read More