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4H-Chromene-based Anticancer Agents Towards Multi-drug Resistant HL60/MX2 Human Leukemia: SAR at the 4th and 6th Positions

Overview
Journal Bioorg Med Chem
Specialties Biochemistry
Chemistry
Date 2016 Feb 13
PMID 26867486
Citations 8
Authors
Manohar Puppala
Xinghua Zhao
Denise Casemore
Bo Zhou
Gopalakrishnan Aridoss
Sreekanth Narayanapillai
Chengguo Xing
Affiliations
Soon will be listed here.
Abstract

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.

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