In vitro study reveals potent MDM2-p53 inhibition and selective p53 activation by spirocyclopentene oxindoles in wild-type p53 cancer cells, highlighting their potential as targeted anticancer agents.
3,3′-Spirocyclopentene oxindoles structurally related to Wang’s spiropyrrolidine oxindoles have been highlighted as a new class of antiproliferative agents against cancer cell lines with wild-type p53 status (IC 50 up to 0.96 μM on SJSA-1 and 2.9 μM in HCT116 p53-wt). Inhibition of the MDM2-p53 interactions has been demonstrated through in vitro HTRF assays (IC 50 up to 3.1 nM), while Western blot analysis showed activation of p53 selectively in HCT116 cancer cell lines with wild-type p53.
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Gicquel et al. (2018) studied this question.
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