Pojarova, Michaela and Kaufmann, Doris and Gastpar, Robert and Nishino, Tsuyuki and Reszka, Przemyslaw and Bednarski, Patrick J. and von Angerer, Erwin (2007) [(2-Phenylindol-3-yl)methylene]propanedinitriles inhibit the growth of breast cancer cells by cell cycle arrest in G(2)/M phase and apoptosis. BIOORGANIC & MEDICINAL CHEMISTRY, 15 (23). pp. 7368-7379. ISSN 0968-0896, 1464-3391
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 malononitrile. The resulting methylene propanedinitriles inhibited the growth of MDA-MB 231 and MCF-7 breast cancer cells with IC50 values below 100 nM. Though they exhibited similar structure-activity relationships as the aldehydes, they did not inhibit tubulin polymerization 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 caspases 3 and 9. Since the new 2-phenylindole derivatives also inhibited the growth of transplanted MXT mouse mammary tumors, they are interesting candidates for further development. (C) 2007 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | INDIRUBIN DERIVATIVES; 3,3'-DIINDOLYLMETHANE DIM; ANTIPROLIFERATIVE AGENTS; TUBULIN POLYMERIZATION; ANTITUMOR-ACTIVITY; EXPRESSION; TYRPHOSTINS; ACTIVATION; DISCOVERY; TARGETS; phenylindoles; breast cancer; cell cycle arrest; apoptosis |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 25 Nov 2020 08:12 |
| Last Modified: | 25 Nov 2020 08:12 |
| URI: | https://pred.uni-regensburg.de/id/eprint/31821 |
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