Structure-activity relationship (SAR) of parthenin analogues with pro-apoptotic activity: Development of novel anti-cancer leads

A small library of semi-synthetic analogues of sesquiterpene lactone parthenin was prepared and screened for cytotoxicity. Some of the members displayed significant cytotoxicity in human cervical carcinoma (HeLa) and human myeloid leukemia (HL-60) cells. A few molecules also induced apoptosis in HL-60 cells measured in terms of sub-Go/G1 DNA fraction. Some information about SAR has also been obtained. Interestingly, one of the lead molecules has been found to be the inhibitor of both telomerase and topoisomerase-II.