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Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

FTase

Action

inhibitors

Mechanism

Ftase inhibitors(Protein farnesyltransferase inhibitors)

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neoplasms

Originator Organization

Bristol Myers Squibb Co.

Active Organization-

Inactive Organization

Bristol Myers Squibb Co.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC25H24N6O2S2

InChIKeyFPEPZFNRGIPRRN-UHFFFAOYSA-N

CAS Registry660843-57-2

Author: Krista Fager ; Rajeev S. Bhide ; Louis J. Lombardo ; Kelly McGlinchey ; Laurence I. Wu ; Amy Camuso ; Veeraswamy Manne ; David Kan ; Johnni Gullo-Brown ; David K. Williams ; Carolyn Ricca ; Ivan Inigo ; John T. Hunt ; Francis Lee ; John Tokarski ; Ligang Qian ; Barry Koplowitz ; George Rovnyak ; Yufen Zhao ; Sarah Traeger ; John Clark

Tetrahydroquinoline-based small molecule inhibitors of farnesyltransferase (FT) have been identified. Lead compounds were shown to have nanomolar to sub-nanomolar activity in biochemical assays with excellent potency in a Ras-mutated cellular reversion assay. BMS-316810 (9e), a 0.7 nM FT inhibitor, was orally-active in a nude mouse tumor allograft efficacy study.

Oxidation Communications

Quantitative structure activity relationship studies on a series of tetrahydroquinoline-based farnesyltransferase inhibitors

Author: Nath, A. ; Srivastava, A. K. ; Chaurasia, Sh. ; Srivastava, M. K. ; Pandey, A.

QSAR anal. on a series of 28 derivatives of tetrahydroquinoline based on farnesyltransferase (FTase) inhibitory activity was performed.The inhibitory activities of these compounds were found to increase with electronegativity, polarizability, hydrophobicity and bulkiness.Excellent results were obtained from multiparametric regression upon introduction of indictor parameters.It was found that the presence of imidazolyl group at X-position and 2-Me propene group at Y-position was conductive for FTase inhibitory activity, and the presence of parazolyl group at X-position and Me cyclohexane at Y-position was found to be detrimental to FTase inhibitory activity.The results are critically discussed on the basis of regression data and crossvalidation technique.

100 Deals associated with BMS-316810

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