405548-67-6Relevant articles and documents
Synthesis Routes Towards the Farnesyl Protein Transferase Inhibitor ZARNESTRA
Angibaud, Patrick R.,Venet, Marc G.,Filliers, Walter,Broeckx, Rudy,Ligny, Yannick A.,Muller, Philippe,Poncelet, Virginie S.,End, Dave W.
, p. 479 - 486 (2007/10/03)
The discovery that post-translational farnesylation of Ras oncoprotein was an essential step in exercising its biological effect led to the design of farnesyl protein transferase inhibitors (FTIs) in order to control growth of tumors bearing Ras mutations. Pre-clinical studies on murine models have confirmed their inhibitory effect on tumor growth and enabled clinical development. R115777 (ZARNESTRA) is currently undergoing clinical evaluation and recent studies have confirmed its antitumor potential and low toxicity. We wish to describe here the chemical synthesis routes that our group have developed to access ZARNESTRA. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
Farnesyl transferase inhibiting 2-quinolone derivatives
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, (2008/06/13)
The present invention is concerned with compounds of formula (I), STR1 the stereoisomeric forms thereof and the pharmaceutically acceptable acid or base addition salts thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R