- METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
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Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.
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Paragraph 01152
(2021/11/20)
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- O-Iodoxybenzoic acid (IBX): A versatile reagent for the synthesis of N-substituted pyrroles mediated by β-cyclodextrin in water
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O-Iodoxybenzoic acid (IBX), a very mild and efficient hypervalent iodine(V) reagent, aromatizes diversely substituted 1-benzylpyrrolidines and N-substituted l-proline analogues to the corresponding substituted pyrroles in good to excellent yields under mild conditions mediated by β-cyclodextrin in water at room temperature. To the best of our knowledge, this is the first report on IBX, promoting complete aromatization leading to N-benzylpyrroles from the corresponding saturated five membered heterocyclic derivatives in water medium.
- Narayana Murthy,Nageswar
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supporting information; experimental part
p. 4481 - 4484
(2011/09/19)
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- Structure-activity relationship and liver microsome stability studies of pyrrole necroptosis inhibitors
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Necroptosis is a regulated caspase-independent cell death pathway resulting in morphology reminiscent of passive non-regulated necrosis. Several diverse structure classes of necroptosis inhibitors have been reported to date, including a series of [1,2,3]thiadiazole benzylamide derivatives. However, initial evaluation of mouse liver microsome stability indicated that this series of compounds was rapidly degraded. A structure-activity relationship (SAR) study of the [1,2,3]thiadiazole benzylamide series revealed that increased mouse liver microsome stability and increased necroptosis inhibitory activity could be accomplished by replacement of the 4-cyclopropyl-[1,2,3]thiadiazole with a 5-cyano-1-methylpyrrole. In addition, the SAR and the cellular activity profiles, utilizing different cell types and necroptosis-inducing stimuli, of representative [1,2,3]thiadiazole and pyrrole derivatives were very similar suggesting that the two compound series inhibit necroptosis in the same manner.
- Teng, Xin,Keys, Heather,Yuan, Junying,Degterev, Alexei,Cuny, Gregory D.
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body text
p. 3219 - 3223
(2009/04/06)
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- Studies on antihypertensive agents with antithrombotic activity. 2.(1)) syntheses and pharmacological evaluation of pyrrolo[2,3-c]azepine derivatives
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As an extension of our previous investigation,(1)) a series of 7-aminoalkylpyrrolo[2,3-c]azepine derivatives was synthesized and evaluated as α1-adrenergic- and serotonin 2 (5-HT2)-receptor antagonists, with the aim of finding a nove
- Mizuno,Miya,Kamei,Shibata,Tatsuoka,Nakanishi,Takiguchi,Hidaka,Yamaki,Inomata
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p. 1129 - 1137
(2007/10/03)
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- Alphacarbamoyl-pyrrolpropionitriles
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1-Substituted-β-oxo-α-phenylcarbamoyl-pyrrolpropionitriles, e.g. those of the formula STR1 their alkylenol ethers or alkanoylenol esters and salts thereof are antiinflammatory and antiarthritic agents.
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