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

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

  • Bioorg Med Chem Lett. 2016 Apr 1;26(7):1726-31. doi: 10.1016/j.bmcl.2016.02.053.
Tara Man Kadayat 1,  Seojeong Park 2,  Kyu-Yeon Jun 2,  Til Bahadur Thapa Magar 1,  Ganesh Bist 1,  Aarajana Shrestha 1,  Younghwa Na 3,  Youngjoo Kwon 4,  Eung-Seok Lee 5
Affiliations

Affiliations

  • 1 College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
  • 2 College of Pharmacy, Graduate School of Pharmaceutical Sciences, Ewha Global Top 5 Program, Ewha Womans University, Seoul 120-750, Republic of Korea.
  • 3 College of Pharmacy, Cha University, Pochon 487-010, Republic of Korea.
  • 4 College of Pharmacy, Graduate School of Pharmaceutical Sciences, Ewha Global Top 5 Program, Ewha Womans University, Seoul 120-750, Republic of Korea. Electronic address: ykwon@ewha.ac.kr.
  • 5 College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea. Electronic address: eslee@yu.ac.kr.
PMID: 26927425 DOI: 10.1016/j.bmcl.2016.02.053
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.

Keywords

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

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