Synthesis, molecular modeling, and structure-activity relationship of benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitors

J Sakowski, M Böhm, I Sattler, HM Dahse…

Index: Sakowski; Boehm; Sattler; Dahse; Schlitzer Journal of Medicinal Chemistry, 2001 , vol. 44, # 18 p. 2886 - 2899

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Citation Number: 46

Abstract

Because of the involvement of farnesylated proteins in oncogenesis, inhibition of the protein- modifying enzyme farnesyltransferase is considered a major emerging strategy in cancer therapy. Here, we describe the structure-activity relationship of a novel class of CAAX- peptidomimetic farnesyltransferase inhibitors based on the benzophenone scaffold. 4'- Methyl, 4'-chloro, 4'-bromo, and 4'-nitrophenylacetic acid as substituents at the 2-amino ...