Source:http://linkedlifedata.com/resource/pubmed/id/20557981
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
2010-8-9
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pubmed:abstractText |
A series of 3,5-diaryl-isoxazoline/isoxazole linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates were prepared. These conjugates showed potent anticancer activity with GI(50) values in the range of <0.1-3.6 microM. Some of these PBD conjugates (6a-c) with promising anticancer activity were further investigated on the cell cycle distribution. Moreover, these PBD conjugates exhibited G0/G1 arrest, enhancement in the levels of p53 protein as well as mitochondrial-mediated intrinsic pathway, leading to release of cytochrome c, activation of caspase-3, cleavage of PARP and subsequent apoptotic cell death. Hence these PBD conjugates with 6a being the most potent one could be be taken up for preclinical studies either alone or in combination with existing therapies.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
1768-3254
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pubmed:author |
pubmed-author:AzharM AmeruddinMA,
pubmed-author:BharathiE VijayaEV,
pubmed-author:DastagiriDD,
pubmed-author:JuvekarAartiA,
pubmed-author:KamalAhmedA,
pubmed-author:Pal-BhadraManikaM,
pubmed-author:PushpavalliS N C V LSN,
pubmed-author:RamaiahM JanakiMJ,
pubmed-author:ReddyJ SurendranadhaJS,
pubmed-author:SenSubrataS,
pubmed-author:SultanaFarheenF,
pubmed-author:ZingdeSurekhaS
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pubmed:copyrightInfo |
2010 Elsevier Masson SAS. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3924-37
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pubmed:meshHeading |
pubmed-meshheading:20557981-Antineoplastic Agents,
pubmed-meshheading:20557981-Apoptosis,
pubmed-meshheading:20557981-Benzodiazepines,
pubmed-meshheading:20557981-Cell Cycle Proteins,
pubmed-meshheading:20557981-Cell Line, Tumor,
pubmed-meshheading:20557981-Cell Proliferation,
pubmed-meshheading:20557981-Drug Design,
pubmed-meshheading:20557981-Gene Expression Regulation, Neoplastic,
pubmed-meshheading:20557981-Humans,
pubmed-meshheading:20557981-Inhibitory Concentration 50,
pubmed-meshheading:20557981-Isoxazoles
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pubmed:year |
2010
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pubmed:articleTitle |
Design, synthesis and biological evaluation of 3,5-diaryl-isoxazoline/isoxazole-pyrrolobenzodiazepine conjugates as potential anticancer agents.
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pubmed:affiliation |
Division of Organic Chemistry, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 607, India. ahmedkamal@iict.res.in
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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