Identification of novel and improved antimitotic agents derived from noscapine
| Autor: | Jianmin Wang, Laurel Faga, Joel Danzig, John J. Harrington, James T. Anderson, Anthony E. Ting, Alain Stricker-Krongrad, Kurt R. Brunden, William F. Hodnick, Youssef L. Bennani, Sherry Boozer, Robert Perry, Chris Crumrine, Stephen Rundlett, Gary Pawlowski, Amy Raber, Steven M. Murphy, Tom Dent |
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| Rok vydání: | 2005 |
| Předmět: |
G2 Phase
Noscapine Antineoplastic Agents Chemical synthesis Microtubules Cell Line chemistry.chemical_compound Mice Biopolymers Tubulin Drug Discovery medicine Animals Humans Natural product Cell growth Biological activity Stereoisomerism Cell cycle Tubulin Modulators chemistry Biochemistry Cell culture Molecular Medicine Antimitotic Agent Drug Screening Assays Antitumor medicine.drug HeLa Cells |
| Zdroj: | Journal of medicinal chemistry. 48(23) |
| ISSN: | 0022-2623 |
| Popis: | Analogues of the natural product noscapine were synthesized and their potential as antitumor agents evaluated. The discovery of a novel regioselective O-demethylation facilitated the synthesis of the potent aniline 6, which arrests mammalian cells in the G2/M phase of the cell cycle at 0.1 microM and also affects tubulin polymerization. Aniline 6 is orally bioavailable and is 250-fold more potent than noscapine in reducing cell proliferation in rapidly dividing cells. |
| Databáze: | OpenAIRE |
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