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Issue 13, 2004
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Synthesis and biological evaluation of synthetic viridins derived from C(20)-heteroalkylation of the steroidal PI-3-kinase inhibitorwortmannin

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Abstract

A series of viridin analogs was prepared from wortmannin by nucleophilic ring opening at C(20) and evaluated against the signaling kinases PI-3-kinase and mTOR. Several subnanomolar enzyme inhibitors with orders of magnitude selectivity for PI-3-kinase and strong cytotoxic activity against four cancer cell lines were identified. Among the ten most promising derivatives, six demonstrated lower liver toxicity and greater promise for inhibition of tumor cell growth than the lead structure wortmannin.

Graphical abstract: Synthesis and biological evaluation of synthetic viridins derived from C(20)-heteroalkylation of the steroidal PI-3-kinase inhibitor wortmannin

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Article information


Submitted
14 Apr 2004
Accepted
11 May 2004
First published
14 Jun 2004

Org. Biomol. Chem., 2004,2, 1911-1920
Article type
Paper

Synthesis and biological evaluation of synthetic viridins derived from C(20)-heteroalkylation of the steroidal PI-3-kinase inhibitor wortmannin

P. Wipf, D. J. Minion, R. J. Halter, M. I. Berggren, C. B. Ho, G. G. Chiang, L. Kirkpatrick, R. Abraham and G. Powis, Org. Biomol. Chem., 2004, 2, 1911
DOI: 10.1039/B405431H

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