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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
13
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pubmed:dateCreated |
2004-6-30
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pubmed:abstractText |
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.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1477-0520
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
7
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pubmed:volume |
2
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1911-20
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:15227545-Alkylation,
pubmed-meshheading:15227545-Androstadienes,
pubmed-meshheading:15227545-Androstenes,
pubmed-meshheading:15227545-Bacteriocins,
pubmed-meshheading:15227545-Cell Line, Tumor,
pubmed-meshheading:15227545-Cell Proliferation,
pubmed-meshheading:15227545-Humans,
pubmed-meshheading:15227545-Inhibitory Concentration 50,
pubmed-meshheading:15227545-Molecular Structure,
pubmed-meshheading:15227545-Phosphatidylinositol 3-Kinases,
pubmed-meshheading:15227545-Phosphatidylinositols,
pubmed-meshheading:15227545-Protein Kinase Inhibitors,
pubmed-meshheading:15227545-Substrate Specificity
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pubmed:year |
2004
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pubmed:articleTitle |
Synthesis and biological evaluation of synthetic viridins derived from C(20)-heteroalkylation of the steroidal PI-3-kinase inhibitor wortmannin.
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pubmed:affiliation |
Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, N.I.H., Extramural
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