Abstract

SYNTHESIS, ANTI-CANCER ACTIVITY AND MOLECULAR DOCKING STUDIES OF THIAZOLIDINE-4-CARBOXYLIC ACIDS

Tanuja Mirashi, Gayatri Chhatre, Dharti H. Modh, Sandeep S. Pathare, Vithal M. Kulkarni*

Abstract

Angiogenesis is encouraged when tumor tissues require nutrients and oxygen. VEGF is an important growth factor that regulates the process of angiogenesis. Its overexpression is observed in many cancers like breast, cervical, hepatocellular, non-small cell lung cancer, etc. Targeting the VEGFR-2 is a useful strategy for developing selective and specific anticancer agents. Thiazolidine-4-carboxylic acid (Tz4C) is a fivemembered saturated and privileged pharmacophore that has been explored as a selective anticancer agent since the 1980s. It can be derived from natural amino acid, L-cysteine and the developed molecules can be lesser toxic in the human body. The current work describes synthesis, biological evaluation and molecular docking studies of these compounds for their ability to inhibit the growth of cancer cells. From this study, 5 analogues had comparable potency to the standard drug Sorafenib.

Keywords: VEGFR-2, Thiazolidine-4-carboxylic acid, thiaproline, Cancer.