Structure-activity relationship (SAR)of parthenin analogues with pro-apoptotic activity: Development of novel anti-cancer leads - Bioorganic & Medicinal Chemistry Letters, 19(15), p.4394-4398, 2009 .

Analogues of parthenin were synthesized by substitutions at different reaction centres to establish a structure-activity relationship (SAR). Some of the molecules have displayed significant cytotoxicity in human cervical carcinoma (HeLa)and human myeloid leukemia (HL-60)cells. A few of the compounds also induced apoptosis in HL-60 cells measured in terms of sub-Go/G1 DNA fraction. Also one of the lead molecules has been shown to be the inhibitor of both telomerase and topoisomerase-II.


CYTOTOXICITY
APOPTOSIS
TOPOISOMERASE-II
TELOMERASE
SAR
PARTHENIN