Effect of chlorine substituent on cytotoxic activities: Design and synthesis of systematically modified 2,4-diphenyl-5H-indeno[1,2-b]pyridines

Tara Man Kadayat, Seojeong Park, Kyu Yeon Jun, Til Bahadur Thapa Magar, Ganesh Bist, Aarajana Shrestha, Younghwa Na, Youngjoo Kwon, Eung Seok Lee

Research output: Contribution to journalArticlepeer-review

11 Scopus citations

Abstract

In continuation of our previous work, six hydroxylated 2,4-diphenyl-5H-indeno[1,2-b]pyridine analogs were modified by introducing one chlorine functionality at ortho, meta or para position of the 2- or 4-phenyl ring. Eighteen new chlorinated compounds were thus prepared and assessed for topoisomerase inhibitory activity and cytotoxicity against HCT15, T47D, and HeLa cancer cell lines. All of the chlorinated compounds displayed significant cytotoxic effect, revealing potent anticancer activity against T47D breast cancer cells. This functional group modification allowed us to explore the importance of chlorine group substitution for the cytotoxic properties. The information reported here provides valuable insight for further study to develop new anticancer agents using related scaffolds.

Original languageEnglish
Pages (from-to)1726-1731
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number7
DOIs
StatePublished - 1 Apr 2016

Keywords

  • 2,4-Diphenyl-5H-indeno[1,2-b]pyridine analog
  • Anticancer agents
  • Breast cancer
  • Cytotoxicity

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