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Natural Products and Bioprospecting

, Volume 2, Issue 5, pp 210–216

First Online: 04 December 2012Received: 19 August 2012Accepted: 12 September 2012

Abstract

A potential strategy for drug lead identification and in-active natural products re-discovery is elaborated. Starting from fifteen structurally diverse natural products, a focused library featured by Michael acceptors is constructed with IBX mediated oxidation. Biological assay on five tumor cell lines indicates that four Michael acceptors, 8a, 11a, 12a, 14a , are with improved cytotoxicity 3–10 folds more potent than the parent compounds, which merit further investigations. Further thiol-sensitive assay of the active hit 8a revealed that it was an irreversible Michael acceptor. The results suggest that the strategy is not only effective and relatively high discovery rate 28%, but also resource saving.

Graphical abstractOpen image in new windowKeywordsdrug leads identification in-active natural products re-discovery Michael acceptors anti-tumor activity This article is published with open access at Springerlink.com

Electronic Supplementary MaterialSupplementary material is available for this article at 10.1007-s13659-012-0071-7 and is accessible for authorized users.

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Author: Xu Deng - Ling-Mei Kong - Yu Zhao - Juan He - Li-Yan Peng - Yan Li - Qin-Shi Zhao

Source: https://link.springer.com/







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