Romagnoli, Romeo and Baraldi, Pier Giovanni and Carrion, Maria Dora and Cruz-Lopez, Olga and Cara, Carlota Lopez and Basso, Giuseppe and Viola, Giampietro and Khedr, Mohammed and Balzarini, Jan and Mahboobi, Siavosh and Sellmer, Andreas and Brancale, Andrea and Hamel, Ernest (2009) 2-Arylamino-4-Amino-5-Aroylthiazoles. "One-Pot" Synthesis and Biological Evaluation of a New Class of Inhibitors of Tubulin Polymerization. JOURNAL OF MEDICINAL CHEMISTRY, 52 (17). pp. 5551-5555. ISSN 0022-2623, 1520-4804
Full text not available from this repository. (Request a copy)Abstract
The essential role of microtubules in mitosis makes them a major target of compounds useful for cancer therapy. In our search for potent antitumor agents, a novel series of 2-anilino-4-amino-5-aroylthiazoles was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. SAR was elucidated with various substitutions on the phenylamino and aroyl moiety at the 2- and 5-positions, respectively, of the 4-aminothiazole skeleton. Tumor cell exposure to several of these compounds led to the arrest of HeLa cells in the G2/M phase of the cell cycle and induction of apoptosis.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | ANTINEOPLASTIC AGENTS; COLCHICINE; CANCER; COMBRETASTATIN-A-4; BINDING; |
| 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: | 07 Sep 2020 08:21 |
| Last Modified: | 07 Sep 2020 08:21 |
| URI: | https://pred.uni-regensburg.de/id/eprint/28412 |
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