2-Substituted paullones : CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity

9-Trifluoromethyl-paullones with a carbon chain in the 2-position were synthesized by palladium-catalyzed coupling reactions of a 2-iodoprecursor with terminal alkenes or alkynes, respectively. The introduction of a 2-cyanoethyl substituent led to a significant enhancement of CDK1/cyclin B inhibitin...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-03, Vol.10 (6), p.567-569
Hauptverfasser:	KUNICK, C, SCHULTZ, C, LEMCKE, T, ZAHAREVITZ, D. W, GUSSIO, R, JALLURI, R. K, SAUSVILLE, E. A, LEOST, M, MEIJER, L
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Benzazepines - chemical synthesis Benzazepines - pharmacology Biological and medical sciences CDC2 Protein Kinase - antagonists & inhibitors Cell Division - drug effects Drug Screening Assays, Antitumor Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology General aspects Histones - metabolism Humans Indoles - chemical synthesis Indoles - pharmacology Medical sciences Oocytes - drug effects Oocytes - enzymology Pharmacology. Drug treatments Starfish Tumor Cells, Cultured
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Zusammenfassung:	9-Trifluoromethyl-paullones with a carbon chain in the 2-position were synthesized by palladium-catalyzed coupling reactions of a 2-iodoprecursor with terminal alkenes or alkynes, respectively. The introduction of a 2-cyanoethyl substituent led to a significant enhancement of CDK1/cyclin B inhibiting property and in vitro antiproliferative activity.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00048-2