183500-36-9Relevant articles and documents
Design and synthesis of piperidine farnesyltransferase inhibitors with reduced glucuronidation potential
Tanaka, Rieko,Rubio, Almudena,Harn, Nancy K.,Gernert, Douglas,Grese, Timothy A.,Eishima, Jun,Hara, Mitsunobu,Yoda, Nobuyuki,Ohashi, Rui,Kuwabara, Takashi,Soga, Shiro,Akinaga, Shiro,Nara, Shinji,Kanda, Yutaka
, p. 1363 - 1382 (2008/02/13)
The design and synthesis of a novel piperidine series of farnesyltransferase (FTase) inhibitors with reduced potential for metabolic glucuronidation are described. The various substitution and exchange of the phenyl group at the C-2 position of the previously described 2-(4-hydroxy)phenyl-3-nitropiperidine 1a (FTase IC50 = 5.4 nM) resulted in metabolically stable compounds with potent FTase inhibition (14a IC50 = 4.3 nM, 20a IC50 = 3.0 nM, and 50a IC50 = 16 nM). Molecular modeling studies of these compounds complexed with FTase and farnesyl pyrophosphate are also described.
Method of treating cancer
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Page/Page column 93, (2010/02/12)
The present invention relates to methods of treating cancer using a combination of a compound which is an antineoplastic agent and a compound which is a inhibitor of prenyl-protein transferase, which methods comprise administering to said mammal, either s
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.
