Natural and Synthetic Molecules with Anticancer Activity: Pharmacological Basis and Mechanistic Insight

Dear Colleagues,

Cancer is one of the most challenging health problems encountered humanity and ranks among the top leading causes of death worldwide according to statistics from the World Health Organization (WHO). While substantial advancements have been achieved towards the early detection of the disease along with the creation of targeted/selective therapies, cancer is still claiming more victims. The deleterious side-effects and development of resistance to the current clinically used chemotherapeutics necessitate continuing research to better understand the pathology of the disease and design more effective therapeutics. Natural products with defined molecular compounds or their semisynthetic derivatives have been well-documented for their potent antitumor activity, as exemplified in multiple FDA-approved drugs such as paclitaxel, vincristine, doxorubicin, and bleomycin. They are defined as having novel chemical scaffolds, 3D pharmacophores, and unique mechanistic modes of action. In some cases, total synthesis of natural products with defined molecular compounds or inspired scaffolds has provided biomolecules for drug development. On the other hand, another approach is ligand-based anticancer drug discovery, which relies on the screening of mega libraries of chemically diverse synthetic molecules against relevant targets, while the structure-based approach involves the rational design and synthesis of biomolecules to optimize their binding to a validated macromolecular target of a known 3D molecular architecture. In this context, this Special Issue is aimed at encouraging scientists in the field of anticancer drug development to publish their recent finding on the mechanistic mode of action of defined natural, semisynthetic, and synthetic biomolecules with emphasis on their anticancer molecular pharmacology.

Dr. Hassan Ebrahim
Dr. Angela Patricia Hernandez
Guest Editors

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• anticancer
• molecular pharmacology
• mechanistic mode of action
• signal transduction
• in vitro
• preclinical
• natural products
• synthesis