Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 24, Pages 5777-5781Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.10.044
Keywords
Indolizine; Farnesyltransferase inhibitor; Activated ester; Propargyl ester; Butynyl ester; Propargyl amide
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Funding
- Project Doctoral and Postdoctoral programs support for increased competitiveness in Exact Sciences research [POSDRU/159/1.5/S/137750]
- European Social Found within the Sectorial Operational Program Human Resources Development
- Romanian Ministry of Education
- CNCS-UEFISCDI [PN-II-RU-PD-2012-3-0426]
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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 mu M. The amidic series 1a-i proves to be the most promising for future modulations, particularly at the triple bond level. (C) 2014 Elsevier Ltd. All rights reserved.
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