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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
A potent series of substituted 2-phenyl-2H-indazole-7-carboxamides were synthesized and evaluated as inhibitors of poly (ADP-ribose) polymerase (PARP). This extensive SAR exploration culminated with the identification of substituted 5-fluoro-2-phenyl-2H-indazole-7-carboxamide analog 48 which displayed excellent PARP enzyme inhibition with IC(50)=4nM, inhibited proliferation of cancer cell lines deficient in BRCA-1 with CC(50)=42nM and showed encouraging pharmacokinetic properties in rats compared to the lead 6.
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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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
488-92
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pubmed:meshHeading |
pubmed-meshheading:20007017-Amides,
pubmed-meshheading:20007017-Animals,
pubmed-meshheading:20007017-Antineoplastic Agents,
pubmed-meshheading:20007017-Azetidines,
pubmed-meshheading:20007017-Enzyme Inhibitors,
pubmed-meshheading:20007017-HeLa Cells,
pubmed-meshheading:20007017-Humans,
pubmed-meshheading:20007017-Indazoles,
pubmed-meshheading:20007017-Poly(ADP-ribose) Polymerases,
pubmed-meshheading:20007017-Rats,
pubmed-meshheading:20007017-Structure-Activity Relationship,
pubmed-meshheading:20007017-Ubiquitin-Protein Ligases
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pubmed:year |
2010
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pubmed:articleTitle |
Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors.
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pubmed:affiliation |
IRBM-Merck Research Laboratories Rome, Via Pontina km 30,600, Pomezia 00040, Rome, Italy. rita.scarpelli@iit.it
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pubmed:publicationType |
Journal Article
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