2. Academic Validation
  3. Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase I inhibitors

Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase I inhibitors

  • Bioorg Med Chem. 2011 Mar 15;19(6):1924-9. doi: 10.1016/j.bmc.2011.01.064.
Daulat Bikram Khadka 1,  Quynh Manh Le,  Su Hui Yang,  Hue Thi My Van,  Thanh Nguyen Le,  Suk Hee Cho,  Youngjoo Kwon,  Kyung-Tae Lee,  Eung-Seok Lee,  Won-Jea Cho
Affiliations

Affiliation

  • 1 College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 500-757, Republic of Korea.
PMID: 21353568 DOI: 10.1016/j.bmc.2011.01.064
Abstract

Various 5-amino group-substituted indeno[1,2-c]isoquinolines 7a-f were synthesized based on the previous QSAR study as rigid structures of 3-arylisoquinolines. Amino group-substituted compounds, especially 5-piperazinyl indeno[1,2-c]isoquinoline 7f, displayed potent Topoisomerase I inhibitory activity as well as cytotoxicities against five different tumor cell lines. A Surflex-Dock docking model of 7f was also studied.

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