Analogues of 1-(3, 10-Dibromo-8-chloro-6, 11-dihydro-5H-benzo [5, 6]-cyclohepta [1, 2-b] pyridin-11-yl) piperidine as inhibitors of farnesyl protein transferase

…, J Weinstein, J Kelly, R Wolin, SB Rosenblum…

Index: Afonso, Adriano; Weinstein, Jay; Kelly, Joseph; Wolin, Ronald; Rosenblum, Stuart B.; Connolly, Michael; Guzi, Timothy; James, Linda; Carr, Donna; Patton, Robert; Bishop, W.Robert; Kirshmeier, Paul; Liu; Heimark; Chen; Nomeir Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 9 p. 1845 - 1855

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Citation Number: 10

Abstract

The synthesis of several 4-pyridylacetyl N-oxide derivatives of 4-(3-bromo-6, 11-dihydro-5H- benzo [5, 6]-cyclohepta [1, 2-b] pyridin-11-yl) piperazine/piperidine 3 is described. This study was aimed at identifying fomesyl protein transferase (FPT) inhibitors in these two series of tricycles containing different phenyl ring substituents. The in vitro activity profile of the initial group of compounds 7a–7g led to the synthesis of the 8-methyl-10-methoxy and 8-methyl- ...