Synthesis, biological activity, and three-dimensional quantitative structure-activity relationship model for a series of benzo [c] quinolizin-3-ones, nonsteroidal inhibitors …

…, A Ferrali, G Menchi, A Guarna, G Danza…

Index: Occhiato, Ernesto G.; Ferrali, Alessandro; Menchi, Gloria; Guarna, Antonio; Danza, Giovanna; Comerci, Alessandra; Mancina, Rosa; Serio, Mario; Garotta, Gianni; Cavalli, Andrea; De Vivo, Marco; Recanatini, Maurizio Journal of Medicinal Chemistry, 2004 , vol. 47, # 14 p. 3546 - 3560

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Citation Number: 30

Abstract

New 5α-reductase 1 (5αR-1) inhibitors were designed to complete a consistent set of analogues suitable for a 3D QSAR study. These compounds were synthesized by a modification of the aza-Robinson annulation, further functionalized by Pd-catalyzed cross- coupling processes, and were tested with human 5αR-1 expressed in Chinese hamster ovary 1827 cells. It turned out that the potency of the resulting inhibitors was strongly ...