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

Manohar Puppala, Xinghua Zhao, Denise Casemore, Bo Zhou, Gopalakrishnan Aridoss, Sreekanth Narayanapillai, Chengguo Xing

Research output: Contribution to journalArticle

14 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)1292-1297
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume24
Issue number6
DOIs
StatePublished - Mar 15 2016

Keywords

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

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