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Article

Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.

European journal of medicinal chemistry - 1 Jan 2016

Punganuru Surendra R, Madala Hanumantha Rao, Venugopal Sanjay N, Samala Ramakrishna, Mikelis Constantinos, Srivenugopal Kalkunte S

Abstract excerpt

Small molecules that can restore biological function to the p53 mutants found in human cancers have been highly sought to increase the anticancer efficacy. In efforts to generate hybrid anticancer drugs that can impact two or more targets simultaneously, we designed and developed piperlongumine (PL) derivatives with an aryl group inserted at the C-7 position. This insertion bestowed a combretastatin A4 (CA4, an...

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PMID: 26599530
DOI: 10.1016/j.ejmech.2015.10.052

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MDM2

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