A novel class of highly potent, selective, and non-peptidic inhibitor of Ras farnesyltransferase (FTase)

  • Bioorg Med Chem Lett. 2001 Dec 3;11(23):3069-72. doi: 10.1016/s0960-894x(01)00624-2.
H Lee  1 ,  J Lee ,  S Lee ,  Y Shin ,  W Jung ,  J H Kim ,  K Park ,  K Kim ,  H S Cho ,  S Ro ,  S Lee ,  S W Jeong ,  T Choi ,  H H Chung ,  J S Koh
Affiliations
  • 1. Life Science R&D, LGCI, Science Town, Taejon 305-380, Republic of Korea.
PMID: 11714612 DOI: 10.1016/s0960-894x(01)00624-2
Abstract

Design, synthesis and structure-activity relationship of a class of aryl pyrroles as farnesyltransferase inhibitors are described. In vitro and in vivo evaluation of a panel of these inhibitors led to identification of 2 (LB42908) as a highly potent (IC(50)=0.9 nM against H-Ras and 2.4 nM against K-Ras) antitumor agent that is currently undergoing preclinical studies.

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