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

Das, Bimolendu ; Chowdhury, Chinmay ; Kumar, Deepak ; Sen, Rupashree ; Roy, Rajneeta ; Das, Padma ; Chatterjee, Mitali (2010) Synthesis, cytotoxicity, and structure–activity relationship (SAR) studies of andrographolide analogues as anti-cancer agent Bioorganic & Medicinal Chemistry Letters, 20 (23). pp. 6947-6950. ISSN 0960894X

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Official URL: http://doi.org/10.1016/j.bmcl.2010.09.126

Related URL: http://dx.doi.org/10.1016/j.bmcl.2010.09.126

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

Item Type:Article
Source:Copyright of this article belongs to Elsevier Ltd.
Keywords:Andrographolide;C14-ester;Analogue;Anti-cancer;Apoptosis
ID Code:132998
Deposited On:26 Dec 2022 04:05
Last Modified:26 Dec 2022 04:05

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