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Org Biomol Chem. 2004 Jul 7;2(13):1911-20. Epub 2004 Jun 14.

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

Author information

1
Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA.

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.

PMID:
15227545
DOI:
10.1039/b405431h
[Indexed for MEDLINE]

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