1,2,3-Triazole analogs of combretastatin A-4 as potential microtubule-binding agents |
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| Authors: | Kristin Odlo Jérémie Fournier-Dit-Chabert Sylvie Ducki Osman ABSM Gani Ingebrigt Sylte Trond Vidar Hansen |
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| Institution: | 1. School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, PO Box 1068, N-0316 Oslo, Norway;2. Clermont Université, ENSCCF, EA 987, LCHG, BP 10448, F-63000 Clermont-Ferrand, France;3. Medical Pharmacology and Toxicology, Department of Medical Biology, University of Tromsø, N-9037 Tromsø, Norway |
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| Abstract: | A series of cis-restricted 1,4- and 1,5-disubstituted 1,2,3-triazole analogs of combretastatin A-4 (1) have been prepared. Cytotoxicity and tubulin inhibition studies showed that 2-methoxy-5-((5-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazol-1-yl)methyl)aniline (5e) and 2-methoxy-5-(1-(3,4,5-trimethoxybenzyl)-1H-1,2,3-triazol-5-yl)aniline (6e) were two of the most active compounds. Molecular modeling studies revealed that the N-2 and N-3 atoms in the triazole rings in 5e and 6e did not form hydrogen bonds with the amino acids in the anticipated pharmacophore. |
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