Abstract
A series of aroylnaphthalene derivatives were prepared as bioisosteres of combrestatin A-4 and evaluated for anticancer activity. 2-Amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalene, 9 and 8, respectively, showed strong antiproliferative activity with IC50 values of 2.1-26.3 nM against a panel of human cancer cell lines including multiple-drug resistant cell line. Compound 9 demonstrated better antiproliferative activity and has a comparable tubulin binding efficacy as that of colchicine.
Original language | English |
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Pages (from-to) | 8163-8167 |
Number of pages | 5 |
Journal | Journal of Medicinal Chemistry |
Volume | 51 |
Issue number | 24 |
DOIs | |
Publication status | Published - 2008 Dec 25 |
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Drug Discovery