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Structure optimization of new tumor-selective Passerini α-acyloxy carboxamides as Caspase-3/7 activators.


ABSTRACT: Selective elimination of tumors has always been the mainstay of oncology research. The on-going research underlying the cellular apoptotic mechanisms reveal caspases activation, especially the key effector caspase-3, as a personalized tumor-selective therapeutic strategy. Our continued research protocol has exploited new optimized Passerini α-acyloxy carboxamides as efficient apoptotic inducers via caspase-3/7 dependent mechanism with highly selective anticancer profiles. The adopted design rationale relied on excluding structural alerts of previous leads, while merging various pharmacophoric motifs of natural and synthetic caspase activators via optimized one-pot Passerini reaction conditions. The prepared compounds resulting from Passerini reaction were screened for their cytotoxic activ

SUBMITTER: Ayoup MS 

PROVIDER: S-EPMC9794698 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature