882280-82-2Relevant academic research and scientific papers
New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: Diversification of the aryl moiety by solid-phase synthesis
Lethu, Sébastien,Bosc, Damien,Mouray, Elisabeth,Grellier, Philippe,Dubois, Jo?lle
, p. 163 - 171 (2013/04/23)
A new synthetic pathway was devised to reach tetrasubstituted 3-arylthiophene 2-carboxylic acids in a three-step solid-phase synthesis. This very efficient methodology provided more than 20 new compounds that were evaluated for their ability to inhibit protein farnesyltransferase from different species as well as Trypanosoma brucei and Plasmodium falciparum proliferation.
Discovery of a new class of protein farnesyltransferase inhibitors in the arylthiophene series
Lethu, Sébastien,Ginisty, Maryon,Bosc, Damien,Dubois, Jo?lle
supporting information; experimental part, p. 6205 - 6208 (2010/03/24)
Screening of the ICSN chemical library led to the discovery of 3-(4-chlorophenyl)-4-cyano-5-thioalkylthiophene 2-carboxylic acids as potent farnesyltransferase inhibitors. Enzymatic kinetic studies showed that this original FTI series belongs to the CaaX
