New semi-synthetic scaffolds of isoalantolactone and their cytotoxic activity

In this study, a series of sixteen new isoalantolactone (IAL 1) amino derivatives (IAL 2 - IAL 17) had been synthesized. IAL 1 and synthesized analogs were evaluated for in vitro cytotoxicity against three human cancer cell lines including cervical cancer (SiHa), epidermoid carcinoma (KB) and colorectal carcinoma (HCT116). The compounds IAL 2, 8, 9, 10, 12 and 17 were found to be nearly active as IAL 1 against all the three tested cell lines, whereas IAL 4 and 16 against HCT116 cells. Findings of the cytotoxicity had provided a correlation on the structure activity relationship of IAL 1 and derivatized analogs against tested cells. The retention of cytotoxicity with enhanced water solubility in derivatized amino adducts including IAL 2, 4, 8, 9,10,12,16 and 17 suggest that these adducts can further be tested for the detailed in vivo safety and anticancer studies with the aim to develop them as a drug. (C) 2016 Phytochemical Society of Europe. Published by Elsevier Ltd. All rights reserved.