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

doi:10.1016/j.bmc.2016.01.056

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

Medicinal Chemistry

Research output: Contribution to journal › Article › peer-review

28 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 language	English (US)
Pages (from-to)	1292-1297
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry
Volume	24
Issue number	6
DOIs	https://doi.org/10.1016/j.bmc.2016.01.056
State	Published - Mar 15 2016

Bibliographical note

Funding 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.

Publisher Copyright:
© 2016 Published by Elsevier Ltd.

Keywords

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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmc.2016.01.056

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6131690

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

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.",

keywords = "4H-Chromene, Anticancer, Cytotoxicity, Multi-drug resistant, Structure-activity relationship",

author = "Manohar Puppala and Xinghua Zhao and Denise Casemore and Bo Zhou and Gopalakrishnan Aridoss and Sreekanth Narayanapillai and Chengguo Xing",

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T2 - SAR at the 4th and 6th positions

AU - Puppala, Manohar

AU - Zhao, Xinghua

AU - Casemore, Denise

AU - Zhou, Bo

AU - Aridoss, Gopalakrishnan

AU - Narayanapillai, Sreekanth

AU - Xing, Chengguo

N1 - Funding 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. Publisher Copyright: © 2016 Published by Elsevier Ltd.

PY - 2016/3/15

Y1 - 2016/3/15

N2 - 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.

AB - 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.

KW - 4H-Chromene

KW - Anticancer

KW - Cytotoxicity

KW - Multi-drug resistant

KW - Structure-activity relationship

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

Abstract

Bibliographical note

Keywords

UN SDGs

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