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Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines.

Authors
  • Ranjan Dwivedi, Ashish1
  • Kumar, Vijay1
  • Kaur, Harmeet1
  • Kumar, Naveen1
  • Prakash Yadav, Ravi2
  • Poduri, Ramarao1
  • Baranwal, Somesh3
  • Kumar, Vinod4
  • 1 Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, Punjab 151001, India. , (India)
  • 2 Department of Microbiology, School of Basic and Applied Sciences, Central University of Punjab, Bathinda, Punjab 151001, India. , (India)
  • 3 Department of Microbiology, School of Basic and Applied Sciences, Central University of Punjab, Bathinda, Punjab 151001, India. Electronic address: [email protected] , (India)
  • 4 Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, Punjab 151001, India; Laboratory of Organic and Medicinal Chemistry, Department of Chemistry, Central University of Punjab, Bathinda, Punjab 151001, India. Electronic address: [email protected] , (India)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Aug 05, 2020
Volume
30
Issue
20
Pages
127468–127468
Identifiers
DOI: 10.1016/j.bmcl.2020.127468
PMID: 32768647
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

A series of triphenyl substituted pyrimidines as analogous of colchicine and combretastatin A-4 was synthesized and evaluated for the antiproliferative potential. The compounds were screened against MDA-MB-231, HCT-116 and HT-29 cell lines using MTT assay. Most of the compounds displayed antiproliferative activity in low to sub micro molar concentration. Amongst the synthesized derivatives, compounds HK-2, HK-10 and HK-13 were found to be effective against all the three cancer cell lines. HK-2 exhibited IC50 values of 3.39 µM, 4.78 µM and 4.23 µM, HK-10 showed IC50 values of 0.81 µM, 5.89 µM, 4.96 µM and HK-13 showed IC50 values 3.24 µM, 4.93 µM and 4.73 µM against MDA-MB-231, HCT-116 and HT-29 cancer cell lines, respectively. HK-10 was found to be the most potent compound in the series with IC50 values of 0.81 µM against MDA-MB-231. In the cell cycle analysis, HK-2 and HK-10 showed cell arrest at G2/M phase of the cell cycle while HK-13 inhibited cell growth at the G1/G0 phase. All the three compounds showed cell death induced through apoptosis. In the docking studies, HK-2, HK-10 and HK-13 were found to fit well in the colchicine binding site of the tubulin. Some of the compounds in the current series were found to be promising against all the three cancer cell lines and may act as potent leads for further development. Copyright © 2020 Elsevier Ltd. All rights reserved.

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