| Literature DB >> 20006519 |
Yali Kong1, Kan Wang, Michael C Edler, Ernest Hamel, Susan L Mooberry, Mikell A Paige, Milton L Brown.
Abstract
Chalcones represent a class of natural products that inhibits tubulin assembly. In this study we designed and synthesized boronic acid analogs of chalcones in an effort to compare biological activities with combretastatin A-4, a potent inhibitor of tubulin polymerization. Systematic evaluation of the positional effects of the carbonyl moiety towards inhibition of tubulin polymerization, cancer cell proliferation and angiogenesis revealed that placement of the carbonyl adjacent to the trimethoxybenzene A-ring resulted in more active compounds than when the carbonyl group was placed adjacent to the C-ring. Our study identified a boronic acid chalcone with inhibition towards 16 human cancer cell lines in the 10-200nM range, and another three cell lines with GI(50)-values below 10nM. Furthermore, this drug has significant anti-angiogenesis effects demonstrated by HUVEC tube formation and aortic ring assay. Copyright 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 20006519 PMCID： PMC2819108 DOI： 10.1016/j.bmc.2009.11.003
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641