Structural interrogation of benzosuberene-based inhibitors of tubulin polymerization
نویسندگان
چکیده
منابع مشابه
Novel indole-bearing combretastatin analogues as tubulin polymerization inhibitors
BACKGROUND The combretastatins are a class of natural stilbenoids. These molecules generally share three common structural features: a trimethoxy "A"-ring, a "B"-ring containing substituent often at C3' and C4', and an ethene bridge between the two rings, which provides necessary structural rigidity. Members of the combretastatin family possess varying ability to cause vascular disruption in tu...
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15 صفحه اولSynthesis of phenstatin/isocombretastatin-chalcone conjugates as potent tubulin polymerization inhibitors and mitochondrial apoptotic inducers.
A series of phenstatin/isocombretastatin–chalcones were synthesized and screened for their cytotoxic activity against various human cancer cell lines. Some representative compounds exhibited significant antiproliferative activity against a panel of sixty human cancer cell lines of the NCI, with GI50 values in the range of 0.11 to 19.0 μM. Three compounds (3b, 3c and 3e) showed a broad spectrum ...
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A series of 1,4-disubstituted-3,4-dihydroisoquinoline derivatives designed as tubulin polymerization inhibitors were synthesized. Their cytotoxic activities against the CEM leukemia cell line were evaluated. Most of them displayed moderate cytotoxic activities, and compounds 21 and 32 showed good activities with IC50 of 4.10 and 0.64 μM, respectively. The most potent compound 32 was further con...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2015
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2015.10.012