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Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase I inhibitors.
Khadka, Daulat Bikram; Le, Quynh Manh; Yang, Su Hui; Van, Hue Thi My; Le, Thanh Nguyen; Cho, Suk Hee; Kwon, Youngjoo; Lee, Kyung-Tae; Lee, Eung-Seok; Cho, Won-Jea.
Afiliación
  • Khadka DB; College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 500-757, Republic of Korea.
Bioorg Med Chem ; 19(6): 1924-9, 2011 Mar 15.
Article en En | MEDLINE | ID: mdl-21353568
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.
Asunto(s)

Texto completo: 1 Base de datos: MEDLINE Asunto principal: Piperazinas / ADN-Topoisomerasas de Tipo I / Inhibidores de Topoisomerasa I / Isoquinolinas Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2011 Tipo del documento: Article

Texto completo: 1 Base de datos: MEDLINE Asunto principal: Piperazinas / ADN-Topoisomerasas de Tipo I / Inhibidores de Topoisomerasa I / Isoquinolinas Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2011 Tipo del documento: Article