Title : Molecular hybridization design and synthesis of novel spirooxindole-based MDM2 inhibitors endowed with BCL2 signaling attenuation; a step towards the next generation p53 activators.

Pub. Date : 2021 Dec

PMID : 34794098






1 Functional Relationships(s)
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1 The most balanced potent and safe derivatives; 5i and 5q were more active than 5-fluorouracil, exhibited low mumrange MDM2 binding (KD=1.32and 1.72 mum, respectively), induced apoptosis-dependent anticancer activities up to 50%, activated p53 by 47-63%, downregulated the BCL2 gene to 59.8%, and reduced its protein level (13.75%) in the treated cancer cells. Fluorouracil tumor protein p53 Homo sapiens