Antimitotic activities of 2-phenylindole-3-carbaldehydes in human breast cancer cells.
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 IC(50) values of 5-20nM. Their action can be rationalized by the cell cycle arrest in G(2)/M phase due to the inhibition of tubulin polymerization.
Kaufmann
Doris
D
Institut für Pharmazie, Universität Regensburg, Regensburg, Germany.
Pojarová
Michaela
M
Vogel
Susanne
S
Liebl
Renate
R
Gastpar
Robert
R
Gross
Dietmar
D
Nishino
Tsuyuki
T
Pfaller
Tobias
T
von Angerer
Erwin
E
D000447:Aldehydes / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D048430:Cell Shape / Q000187:drug effects; D002477:Cells / Q000187:drug effects; D006801:Humans; D008938:Mitosis / Q000187:drug effects*; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013997:Time Factors; D014404:Tubulin / Q000378:metabolism
D000447:Aldehydes; D000970:Antineoplastic Agents; D014404:Tubulin