- SMALL MOLECULE INHIBITORS OF MCL-1 AND USES THEREOF
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This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having benzoic acid structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
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Page/Page column 71-72; 76
(2016/11/14)
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- NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, METHODS OF USE FOR SAME, AND METHODS FOR PREPARING SAME
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The present invention relates to a novel class of compounds comprising formula I, wherein n is 0 or 1. A is NR1, O, or S, wherein R1 is H, hydroxyl, C1-C10 alkyl, C1-C10 alkoxy, alkenyl, aryl, alkylaryl or arylalkyl. X is a carboxylate, a phosphonate, or a phosphate residue, or a C1-C10 alkyl residue optionally substituted with a carboxylate, phosphonate or phosphate residue. Y is a C1-C20 alkyl, alkenyl, halide, hydroxyl, C1-C20 alkoxy, aryl, alkylaryl, arylalkyl, cycloalkyl, cycloalkenyl, or a heterocyclic ring and is optionally substituted with one or more halides. Z is a H, a hydroxyl group, a halide, an aryl group, an alkylaryl group, an arylalkyl group, a cycloalkyl group, a cycloalkenyl group or a heterocyclic ring and is optionally substituted with one or more C1-C10 alkyl groups, C1-C10alkoxy groups, hydroxyl groups, cyano groups, carboxylate groups, halides, aryl groups, alkylaryl groups, arylalkyl groups, cycloalkyl groups, cycloalkenyl groups or heterocyclic rings.
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Page/Page column 34
(2010/04/03)
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- Design and synthesis of small molecule glycerol 3-phosphate acyltransferase inhibitors
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The incidence of obesity and other diseases associated with an increased triacylglycerol mass is growing rapidly, particularly in the United States. Glycerol 3-phosphate acyltransferase (GPAT) catalyzes the ratelimiting step of glycerolipid biosynthesis, the acylation of glycerol 3-phosphate with saturated long-chain acyl-CoAs. In an effort to produce small molecule inhibitors of this enzyme, a series of benzoic and phosphonic acids was designed and synthesized. In vitro testing of this series has led to the identification of several compounds, in particular 2-(nonylsulfonamido)benzoic acid (15g), possessing moderate GPAT inhibitory activity in an intact mitochondrial assay.
- Wydysh, Edward A.,Medghalchi, Susan M.,Vadlamudi, Aravinda,Townsendd, Craig A.
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experimental part
p. 3317 - 3327
(2010/03/26)
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- Discovery of new chemical leads for selective EP1 receptor antagonists
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A series of 4-({2-[alkyl(phenylsulfonyl)amino]phenoxy}methyl)benzoic acids were identified as functional PGE2 antagonists with selectivity for the EP1 receptor subtype starting from a chemical lead 1, which was found while screening our in-house compound library. Discovery of the optimized analogs 21-23 is presented here and structure-activity relationships (SAR) are also discussed.
- Naganawa, Atsushi,Saito, Tetsuji,Nagao, Yuuki,Egashira, Hiromu,Iwahashi, Maki,Kambe, Tohru,Koketsu, Masatoshi,Yamamoto, Hiroshi,Kobayashi, Michiyoshi,Maruyama, Takayuki,Ohuchida, Shuichi,Nakai, Hisao,Kondo, Kigen,Toda, Masaaki
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p. 5562 - 5577
(2007/10/03)
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