Mahboobi, Siavosh and Sellmer, Andreas and Hoecher, Heymo and Eichhorn, Emerich and Baer, Thomas and Schmidt, Mathias and Maier, Thomas and Stadlwieser, Josef F. and Beckers, Thomas L. (2006) [4-(imidazol-1-yl)thiazol-2-yl]phenylamines. A novel class of highly potent colchicine site binding tubulin inhibitors: Synthesis and cytotoxic activity on selected human cancer cell lines. JOURNAL OF MEDICINAL CHEMISTRY, 49 (19). pp. 5769-5776. ISSN 0022-2623,
Full text not available from this repository. (Request a copy)Abstract
Synthesis and cytotoxic activity in the submicromolar range of a series of [4-(imidazol-l-yl)thiazol-2-yl]-phenylamines are described. Cell cycle dependent cytotoxicity on RKO human colon carcinoma cells with inducible expression of p27(kip1) and the influence on microtubule formation were investigated. Considering the significant correlation between the IC50 values of tubulin polymerization inhibition, [H-3]colchicine competition, and cytotoxicity of the investigated compounds, tubulin is the main cellular target. The inhibition of microtubule formation was shown to be mediated by interference with the colchicine binding site of tubulin. In depth analysis of the investigated compounds allowed the identification of modifications that altered the pharmacological profile of the compounds from a mitosis-inducing phenotype to a G1 cell cycle arresting phenotype.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | DEPENDENT KINASE INHIBITORS; DERIVATIVES; P21(WAF1); P27(KIP1); THERAPY; CYCLE; DRUG; |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 27 Jan 2021 11:00 |
| Last Modified: | 27 Jan 2021 11:00 |
| URI: | https://pred.uni-regensburg.de/id/eprint/34017 |
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