450840-98-9Relevant academic research and scientific papers
Diversity-oriented synthesis of 1-substituted 4-aryl-6-oxo-1,6- dihydropyridine-3-carboxamides.
Baskovc, Jernej,Dahmann, Georg,Golobic, Amalija,Groselj, Uros,Kocar, Drago,Stanovnik, Branko,Svete, Jurij
, p. 513 - 519 (2012/10/29)
A simple five-step diversity-oriented synthesis of 1-substituted 4-aryl-6-oxo-1,6-dihydropyridine-3-carboxamides was developed. Treatment of dimethyl 2-((dimethylamino)methylidene)-3-oxopentanedioate with twenty primary amines gave 1-substituted methyl 4-hydroxy-6-oxo-1,6-dihydropyridine-3- carboxylates. Transformation into the corresponding 4-tosyloxy and 4-chloro derivatives, followed by Suzuki-Miyaura arylations gave a series of eleven N-substituted methyl 4-aryl-6-oxo-1,6-dihydropyridine-3-carboxylates. Combinatorial screening was employed to establish suitable reaction conditions for Suzuki-Miyaura arylation of N-alkylpyridones. Hydrolysis of the esters followed by parallel solution-phase amidation of the corresponding carboxylic acids with primary and secondary amines furnished a library of seventeen final products.
Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors
Li, Qun,Claiborne, Akiyo,Li, Tongmei,Hasvold, Lisa,Stoll, Vincent S.,Muchmore, Steven,Jakob, Clarissa G.,Gu, Wendy,Cohen, Jerry,Hutchins, Charles,Frost, David,Rosenberg, Saul H.,Sham, Hing L.
, p. 5367 - 5370 (2007/10/03)
As a part of our efforts to identify potent inhibitors of farnesyltransferase (FTase), modification of the structure of tipifarnib through structure-based design was undertaken by replacing the 2-quinolones with 4-quinolones and pyridones, and subsequent
Farnesyltransferase inhibitors
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, (2008/06/13)
Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient.
Farnesyltransferase inhibitors
-
, (2008/06/13)
Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient.
