Bridgehead modification of trihalocycloheptabenzopyridine lead to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability

Njoroge, F. George; Vibulbhan, Bancha; Shi, Xiongwei; Strickland, Corey; Kirschmeier, Paul T.; Bishop, Robert; Nomeir, Amin A.; Girijavallabhan, Viyyoor

doi:10.1016/j.bmcl.2004.09.020

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“…It is also reported that the incorporation of groups with zinc binding ability at 2-position of the piperidine ring can enhance activity (structure I, fig. 1)[5]. …”

mentioning

confidence: 99%

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

Gatne¹,

Viswanathan²,

Ambre³

et al. 2010

Indian J Pharm Sci

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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 IC50 values of <15 μM in two cell lines tested. Test compounds also exhibited potent FPT inhibitory activity and 6c was most potent with IC50 value of <30 μM.

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“…It is also reported that the incorporation of groups with zinc binding ability at 2-position of the piperidine ring can enhance activity (structure I, fig. 1)[5]. …”

mentioning

confidence: 99%