220364-27-2Relevant articles and documents
Synthesis and activity of 1-aryl-1′-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors
Li, Qun,Wang, Gary T.,Li, Tongmei,Gwaltney II, Stephen L.,Woods, Keith W.,Claiborne, Akiyo,Wang, Xilu,Gu, Wendy,Cohen, Jerry,Stoll, Vincent S.,Hutchins, Charles,Frost, David,Rosenberg, Saul H.,Sham, Hing L.
, p. 5371 - 5376 (2007/10/03)
A series of imidazole-containing methyl ethers (4-5) have been designed and synthesized as potent and selective farnesyltransferase inhibitors (FTIs) by transposition of the D-ring to the methyl group on the imidazole of the previously reported FTIs 3. Several compounds such as 4h and 5b demonstrate superior enzymatic activity to the current benchmark compound tipifarnib (1) with IC50 values in the lower subnanomolar range, while maintaining excellent cellular activity comparable to tipifarnib. The compounds are characterized as being simple, easier to make, and possess no chiral center involved.
Pyrrole derivatives useful for farnesyl transferase inhibitors and their preparations
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, (2008/06/13)
The present invention relates to a novel pyrrole derivative which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof; to a process for preparation of said compound; and to a pharmaceutical composition such as anti-cancer composition, etc. comprising said compound as an active ingredient together with pharmaceutically acceptable carrier.
Imidazole derivatives having an inhibitory activity for farnesyl transferase and process for preparation thereof
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, (2008/06/13)
The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1); and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.