4H-Chromene-based compounds, for example, CXL017, CXL035, and CXL055, have a unique anticancer potential that they selectively kill multi-drug resistant cancer cells. Reported herein is the extended structure-activity relationship (SAR) study, focusing on the ester functional group at the 4th position and the conformation at the 6th position. Sharp SARs were observed at both positions with respect to cellular cytotoxic potency and selectivity between the parental HL60 and the multi-drug resistant HL60/MX2 cells. These results provide critical guidance for future medicinal optimization.
Bibliographical noteFunding Information:
This research was supported by grants from the National Cancer Institute ( R01CA163864 , C.X.) and the Program of Study Abroad for Young Teachers by Agricultural University of Hebei (X.Z.) – China.
© 2016 Published by Elsevier Ltd.
- Multi-drug resistant
- Structure-activity relationship