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Particularly, 32 containing a naphthyl group and (d)-Phe moiety has higher effectiveness with a fantastic reversal fold than verapamil at a concentration of 5 μM, which induces conformational change of P-gp and prevents its function in the place of modifying P-gp expression. Also, 23 and 32 were identified to be appealing prospects, which have good pharmacokinetic profile and antitumor activity in a KBV200 xenograft mouse model.Despite the large prevalence of