Vogel, Susanne and Kaufmann, Doris and Pojarova, Michaela and Mueller, Christine and Pfaller, Tobias and Kuehne, Sybille and Bednarski, Patrick J. and von Angerer, Erwin (2008) Aroyl hydrazones of 2-phenylindole-3-carbaldehydes as novel antimitotic agents. BIOORGANIC & MEDICINAL CHEMISTRY, 16 (12). pp. 6436-6447. ISSN 0968-0896,
Full text not available from this repository. (Request a copy)Abstract
Cell cycle arrest of malignant cells is an important option for cancer treatment. In this study, we modified the structure of antimitotic 2-phenylindole-3-carbaldehydes by condensation with hydrazides of various benzoic and pyridine carboxylic acids. The resulting hydrazones inhibited the growth of MDA-MB 231 and MCF-7 breast cancer cells with IC(50) values of 20-30 nM for the most potent derivatives. These 2-phenylindole derivatives also exerted an inhibitory effect on the growth of both proliferating and resting U-373 MG glioblastoma cells. Though the hydrazones exhibited similar structure-activity relationships as the aldehydes, they did not inhibit tubulin polymerization as the aldehydes but were capable of blocking the cell cycle in G(2)/M phase. The cell cycle arrest was accompanied by apoptosis as demonstrated by the activation of caspase-3. Since these 2-phenylindole-based hydrazones display no structural similarity with other antitumor drugs they are interesting candidates for further development. (c) 2008 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | BREAST-CANCER CELLS; HISTONE-DEACETYLASE INHIBITOR; CYCLE ARREST; ANTITUMOR-ACTIVITY; STEROID SULFATASE; TRICHOSTATIN-A; APOPTOSIS; PROLIFERATION; 2-PHENYLINDOLES; ELLIPTICINE; phenylindoles; aroyl hydrazones; breast cancer cells; glioblastoma cells; cell cycle arrest; apoptosis |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 29 Oct 2020 06:49 |
| Last Modified: | 29 Oct 2020 06:49 |
| URI: | https://pred.uni-regensburg.de/id/eprint/30728 |
Actions (login required)
 |
View Item |
