Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10586524 | Bioorganic & Medicinal Chemistry Letters | 2014 | 10 Pages |
Abstract
The rational structural modification of new substituted indolizin-3-yl(phenyl)methanones 1a-i, 2a-i and 3a-i has greatly improved human farnesyltransferase inhibition. The para-bromophenyl analog 2f bearing an ester unit on the indolizine ring demonstrates the highest inhibition potential, with IC50 value of 1.3 ± 0.2 μM. The amidic series 1a-i proves to be the most promising for future modulations, particularly at the triple bond level.71
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Authors
Carmen Dumea, Dalila Belei, Alina Ghinet, Joëlle Dubois, Amaury Farce, Elena Bîcu,