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Updated: Aug 22, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and structure-activity relationships of andrographolide analogues as novel cytotoxic agents
Srinivas Nanduri1, Vijay Kumar Nyavanandi, Siva Sanjeeva Rao Thunuguntla
1Discovery Chemistry, Dr. Reddy's Laboratories Ltd, Discovery Research, Bollaram Road, Miyapur, Hyderabad 500 049, India. nandurisrinivas@drreddys.com
Abstract:
Andrographolide 1, the cytotoxic agent of the plant Andrographis paniculata was subjected to semi-synthetic studies leading to the preparation of a number of potent and novel analogues. Of the analogues synthesized, while 8,17-epoxy andrographolide 6 retained the cytotoxic activity of 1, ester derivatives of 6 exhibited considerable improvement in activity. Lower activity was observed when the epoxy moiety in the triacetate 9, derived from 6 was modified. Synthesis and structure-activity relationships are discussed.
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