3-Aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrrole, a novel class of farnesyltransferase inhibitors

H Lee; J Lee; Y Shin; W Jung; J H Kim; K Park; S Ro; H H Chung; J S Koh

doi:10.1016/s0960-894x(01)00593-5

3-Aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrrole, a novel class of farnesyltransferase inhibitors

Bioorg Med Chem Lett. 2001 Nov 19;11(22):2963-5. doi: 10.1016/s0960-894x(01)00593-5.

Authors

H Lee¹, J Lee, Y Shin, W Jung, J H Kim, K Park, S Ro, H H Chung, J S Koh

Affiliation

¹ Life Science R & D, LGCI, Science Town, Taejon 305-380, South Korea.

PMID: 11677136
DOI: 10.1016/s0960-894x(01)00593-5

Abstract

Design, synthesis and structure-activity relationship of a class of 3-aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrroles as farnesyltransferase inhibitors are described. Compound 7 inhibits farnesyltransferase with an IC(50) value of 4.6 nM.

MeSH terms

Alkyl and Aryl Transferases / antagonists & inhibitors*
Drug Design
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Farnesyltranstransferase
Imidazoles / chemical synthesis*
Imidazoles / pharmacology
Inhibitory Concentration 50
Pyrroles / chemical synthesis*
Pyrroles / pharmacology
Structure-Activity Relationship

Substances

3-aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrrole
Enzyme Inhibitors
Imidazoles
Pyrroles
Alkyl and Aryl Transferases
Farnesyltranstransferase