Potency and Selectivity Optimization of Tryptophanol‐Derived Oxazoloisoindolinones: Novel p53 Activators in Human Colorectal Cancer
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DOI: 10.1002/cmdc.202000522
Abstract: To search for novel p53 activators, four series of novel (S)‐ and (R)‐tryptophanol‐derived oxazoloisoindolinones were synthesized in a straightforward manner and their antiproliferative activity was evaluated in the human colorectal cancer HCT116 cell line. Structural optimization… read more here.
Keywords: derived oxazoloisoindolinones; novel p53; tryptophanol derived; p53 ... See more keywords
Molecular hybridization design and synthesis of novel spirooxindole-based MDM2 inhibitors endowed with BCL2 signaling attenuation; a step towards the next generation p53 activators.
Sign Up to like & getrecommendations! Published in 2021 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2021.105427
Abstract: Despite the achieved progress in developing efficient MDM2-p53 protein-protein interaction inhibitors (MDM2 inhibitors), the acquired resistance of tumor cells to such p53 activators posed an argument about the druggability of the pathway. Combination studies disclosed… read more here.
Keywords: mdm2 inhibitors; based mdm2; p53; spirooxindole based ... See more keywords
Metabolism-Guided Optimization of Tryptophanol-Derived Isoindolinone p53 Activators
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DOI: 10.3390/ph16020146
Abstract: For the first time, the pharmacokinetic (PK) profile of tryptophanol-derived isoindolinones, previously reported as p53 activators, was investigated. From the metabolites’ identification, performed by liquid chromatography coupled to high resolution tandem mass spectrometry (LC-HRMS/MS), followed… read more here.
Keywords: metabolism; p53 activators; tryptophanol; tryptophanol derived ... See more keywords