| Literature DB >> 15454219 |
Ayako Yamashita1, Emily B Norton, Joshua A Kaplan, Chuan Niu, Frank Loganzo, Richard Hernandez, Carl F Beyer, Tami Annable, Sylvia Musto, Carolyn Discafani, Arie Zask, Semiramis Ayral-Kaloustian.
Abstract
Analogs of hemiasterlin (1) and HTI-286 (2), which contain various aromatic rings in the A segment, were synthesized as potential inhibitors of tubulin polymerization. The structure-activity relationships related to stereo- and regio-chemical effects of substituents on the aromatic ring in the A segment were studied. Analogs, which carry a meta-substituted phenyl ring in the A segment show comparable activity for inhibition of tubulin polymerization to 2, as well as in the cell proliferation assay using KB cells containing P-glycoprotein, compared to those of 1 and 2.Entities:
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Year: 2004 PMID： 15454219 DOI： 10.1016/j.bmcl.2004.08.024
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823