73058-14-7Relevant academic research and scientific papers
METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
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Paragraph 01152, (2021/11/20)
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.
O-Iodoxybenzoic acid (IBX): A versatile reagent for the synthesis of N-substituted pyrroles mediated by β-cyclodextrin in water
Narayana Murthy,Nageswar
supporting information; experimental part, p. 4481 - 4484 (2011/09/19)
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.
Structure-activity relationship and liver microsome stability studies of pyrrole necroptosis inhibitors
Teng, Xin,Keys, Heather,Yuan, Junying,Degterev, Alexei,Cuny, Gregory D.
body text, p. 3219 - 3223 (2009/04/06)
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.
Studies on antihypertensive agents with antithrombotic activity. 2.(1)) syntheses and pharmacological evaluation of pyrrolo[2,3-c]azepine derivatives
Mizuno,Miya,Kamei,Shibata,Tatsuoka,Nakanishi,Takiguchi,Hidaka,Yamaki,Inomata
, p. 1129 - 1137 (2007/10/03)
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
Alphacarbamoyl-pyrrolpropionitriles
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, (2008/06/13)
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.
