Structural Perspective of Benzophenones Targeting Tubulin as Anticancer Agents

Abstract

Abstract: Cancer is the main cause of death and the most significant determinant of life expectancy in every country in the twenty-first century. According to the World Health Organization (WHO) cancer is responsible for major cause of death globally. Benzophenone derivatives are found in a variety of naturally occurring compounds which are known to be pharmacologically efficacious against a variety of diseases, including cancer. Microtubules are thought to be a good target for cancer chemotherapies. Microtubule polymerization and depolymerization are induced by a variety of natural, synthetic, and semisynthetic chemicals having a benzophenone nucleus, affecting tubulin dynamics. Several medications that affect microtubule dynamics are in various stages of clinical trials, including Combretastatins (phase II), Vincristine (clinically approved), Paclitaxel (in clinical usage), and epothilone (phase III), and only a few have been patented. Benzophenone derivatives act by targeting the colchicine binding site of microtubules damage them and cause cell cycle arrest in the G2-M phase. Belonging to this class of molecules, phenstatin, a potent inhibitor of tubulin polymerization, shown strongly inhibited cancer cell growth and arrest the G2/M phase of the cell cycle by targeting the colchicine binding site of microtubules. In the present manuscript we described the benzophenone as tubulin polymerization inhibitors their structure activity relationships (SARs) and molecular docking studies that reveal its binding affinity with the colchicine binding site.