Synthesis, cytotoxicity, and structure-activity relationship (SAR) studies of andrographolide analogues as anti-cancer agent

Bimolendu Das, Chinmay Chowdhury, Deepak Kumar, Rupashree Sen, Rajneeta Roy, Padma Das, Mitali Chatterjee

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish (US)
Pages (from-to)6947-6950
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number23
DOIs
StatePublished - Dec 1 2010
Externally publishedYes

Keywords

  • Analogue
  • Andrographolide
  • Anti-cancer
  • Apoptosis
  • C14-ester

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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