183500-94-9Relevant articles and documents
Synthesis and cytotoxicity evaluation of some novel 1-(3-Chlorophenyl) piperazin-2-one derivatives bearing imidazole bioisosteres
Ghasemi, Saeed,Sharifi, Simin,Davaran, Soodabeh,Danafar, Hosein,Asgari, Davoud,Mojarrad, Javid Shahbazi
, p. 655 - 660 (2013/07/26)
A series of substituted 3-chlorophenylpiperazinone derivatives were synthesised using L-778123 (an imidazole-containing FTase inhibitor) as a model by bioisosteric replacement of the imidazole ring. The final compounds were evaluated against two human cancer cell lines including A549 (lung cancer) and HT-29 (colon cancer) by MTT assay. The results showed that substitution of imidazole ring with 1-amidinourea, semicarbazide, and thiobiuret led to improvement of cytotoxic activity against both cell lines.
Preparation of a clinically investigated ras farnesyl transferase inhibitor
Maligres, Peter E.,Waters, Marjorie S.,Weissman, Steven A.,McWilliams, J. Christopher,Lewis, Stephanie,Cowen, Jennifer,Reamer, Robert A.,Volante,Reider, Paul J.,Askin, David
, p. 229 - 241 (2007/10/03)
The synthesis of ras farnesyl-protein transferase inhibitor 1 is described on a multi-kilogram scale. Retrosynthetic analysis reveals chloromethylimidazole 2 and a piperazinone 3 as viable precursors. The 1,5-disubstituted imidazole system was regioselectively assembled via an improved Marckwald imidazole synthesis. A new imidazole dethionation procedure has been developed to convert the Marckwald mercaptoimidazole product to the desired imidazole. This methodology was found to be tolerant of a variety of functional groups providing good to excellent yields of 1,5-disubstituted imidazoles. A new Mitsunobu cyclization strategy was developed to prepare the arylpiperazinone fragment 3.
Sustained release drug dispersion delivery device
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, (2008/06/13)
The present invention is related to a drug delivery device, that is pH insensitive, for the sustained in situ production and release of a dispersion, in an environment of use, which comprises a) a compressed core prepared from an admixture comprising i) a