4H-Chromene-based anticancer agents towards multi-drug resistant CrossMark HL60/MX2 human leukemia: SAR at the 4th and 6th positions

作者：Puppala, Manohar; Zhao, Xinghua; Casemore, Denise; Zhou, Bo; Aridoss, Gopalakrishnan; Narayanapillai, Sreekanth; Xing, Chengguo^*

来源：Bioorganic & Medicinal Chemistry, 2016, 24(6): 1292-1297.

DOI：10.1016/j.bmc.2016.01.056

• 4H-Chromene
• Anticancer
• Cytotoxicity
• Multi-drug resistant
• Structure-activity relationship

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.

• 出版日期2016-3-15
• 单位河北农业大学