Design, Synthesis and Evaluation of Novel 1-(Substituted Acetyl)-4-(10-Bromo-8-Chloro-5,6-Dihydro-11H-Benzo[5,6]Cyclohepta[1,2-B]Pyridine-11-Ylidene)piperidines as Antitumor Agents and Farnesyl Protein Transferase Inhibitors

Autor:	PS Gatne, Premlata K. Ambre, Aarti Juvekar, C.L. Viswanathan
Jazyk:	angličtina
Rok vydání:	2010
Předmět:	Antitumor activity Farnesyl Protein Transferase Zinc binding Chemistry Stereochemistry farnesyl protein transferase inhibitors Short Communication Pharmaceutical Science In vitro chemistry.chemical_compound Design synthesis Cell culture Anticancer agents Pyridine benzocycloheptapyridines Molecule
Zdroj:	Indian Journal of Pharmaceutical Sciences
ISSN:	1998-3743 0250-474X
Popis:	Eight novel 1-(substituted acetyl)-4-(10-bromo-8-chloro-5,6-dihydro-11H-benzo[5,6] cyclohepta [1,2-b] pyridine-11-ylidene)piperidines were designed by incorporating zinc binding groups to enhance activity. The designed molecules were synthesized and were evaluated for antitumor activity in vitro in five cell lines and for farnesyl protein transferase inhibition. Test compounds (6a-h) exhibited antitumor activity in most of the cell lines but were less potent than adriamycin. Compound 6e was most active with IC 50 values of
Databáze:	OpenAIRE
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