Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents.

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Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents.

Bioorg Med Chem Lett. 2017 Feb 13;:

Authors: Yang J, Tu Z, Xu X, Luo J, Yan X, Ran C, Mao X, Ding K, Qiao C

Abstract
In the present study, endoperoxide and 4-anilinoqnazoline were conjugated to obtain a series of compounds. These conjugates exhibited high antiproliferative potency against a number of cancer cell lines, including the epidermal growth factor receptor (EGFR) L858R/T790M mutant cell. Compound 5 was selected as a representative for mechanistic study. Further experiments revealed the conjugate's reactive oxygen species (ROS) generating ability, apoptosis inducing activity and involvement in EGFR downstream signaling pathways.

PMID: 28236592 [PubMed - as supplied by publisher]

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