Antimitotic activities of 2-phenylindole-3-carbaldehydes in human breast cancer cells

Kaufmann, Doris and Pojarova, Michaela and Vogel, Susanne and Liebl, Renate and Gastpar, Robert and Gross, Dietmar and Nishino, Tsuyuki and Pfaller, Tobias and von Angerer, Erwin (2007) Antimitotic activities of 2-phenylindole-3-carbaldehydes in human breast cancer cells. BIOORGANIC & MEDICINAL CHEMISTRY, 15 (15). pp. 5122-5136. ISSN 0968-0896, 1464-3391

Full text not available from this repository. (Request a copy)

Abstract

Small molecules such as indoles are attractive as inhibitors of tubulin polymerization. Thus a number of 2-phenylindole-3-carbaldehydes with lipophilic substituents in both aromatic rings was synthesized and evaluated for antitumor activity in MDA-MB 231 and MCF-7 breast cancer cells. Some 5-alkylindole derivatives with a 4-methoxy group in the 2-phenyl ring strongly inhibit the growth of breast cancer cells with IC50 values of 5-20 nM. Their action can be rationalized by the cell cycle arrest in G(2)/M phase due to the inhibition of tubulin polymerization. (c) 2007 Elsevier Ltd. All rights reserved.

Item Type: Article
Uncontrolled Keywords: COMBRETASTATIN A-4 ANALOGS; POTENT ANTITUBULIN AGENTS; TUBULIN POLYMERIZATION; BIOLOGICAL EVALUATION; IN-VIVO; INHIBITORS; INDOLE; ARYLTHIOINDOLES; 3-AROYLINDOLES; DERIVATIVES; phenylindoles; breast cancer; tubulin polymerization; cell cycle arrest
Subjects: 600 Technology > 615 Pharmacy
Divisions: Chemistry and Pharmacy > Institute of Pharmacy
Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Depositing User: Dr. Gernot Deinzer
Date Deposited: 02 Dec 2020 13:44
Last Modified: 02 Dec 2020 13:44
URI: https://pred.uni-regensburg.de/id/eprint/32415

Actions (login required)

View Item View Item