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Synthesis, cytotoxicity, and structure-activity relationship (SAR) studies of andrographolide analogues as
Bimolendu Das1, Chinmay Chowdhury, Deepak Kumar
1Indian Institute of Chemical Biology (CSIR), Kolkata, India.
Abstract:
A series of analogues of andrographolide, prepared through chemo-selective functionalization at C14 hydroxy, have been evaluated for in vitro cytotoxicities against human leukemic cell lines. Two of the analogues (6a, 9b) exhibited significant potency. Preliminary studies on structure-activity relationship (SAR) revealed that the α-alkylidene-γ-butyrolactone moiety of andrographolide played a major role in the activity profile. The structures of the analogues were established through spectroscopic and analytical data.
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