Literature DB >> 11294379

2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase.

B W Trotter1, A G Quigley, W C Lumma, J T Sisko, E S Walsh, C S Hamann, R G Robinson, H Bhimnathwala, D G Kolodin, W Zheng, C A Buser, H E Huber, R B Lobell, N E Kohl, T M Williams, S L Graham, C J Dinsmore.   

Abstract

A series of 2-arylindole-3-acetamide farnesyl protein transferase inhibitors has been identified. The compounds inhibit the enzyme in a farnesyl pyrophosphate-competitive manner and are selective for farnesyl protein transferase over the related enzyme geranylgeranyltransferase-I. A representative member of this series of inhibitors demonstrates equal effectiveness against HDJ-2 and K-Ras farnesylation in a cell-based assay when geranylgeranylation is suppressed.

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Year:  2001        PMID: 11294379     DOI: 10.1016/s0960-894x(01)00061-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Single-flask synthesis of N-acylated indoles by catalytic dehydrogenative coupling with primary alcohols.

Authors:  Brooks E Maki; Karl A Scheidt
Journal:  Org Lett       Date:  2009-04-02       Impact factor: 6.005

2.  Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen.

Authors:  Marina Bukhtiyarova; Erica M Cook; Paula J Hancock; Alan W Hruza; Anthony W Shaw; Gregory C Adam; Richard J O Barnard; Philip M McKenna; M Katharine Holloway; Ian M Bell; Steve Carroll; Ivan Cornella-Taracido; Christopher D Cox; Peter S Kutchukian; David A Powell; Corey Strickland; B Wesley Trotter; Matthew Tudor; Scott Wolkenberg; Jing Li; David M Tellers
Journal:  ACS Med Chem Lett       Date:  2020-12-23       Impact factor: 4.345

  2 in total

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