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Synthesis and biological evaluations of novel indenoisoquinolines as topoisomerase I inhibitors.
Bioorg Med Chem Lett. 2012 Jan 15; 22(2):1276-81.BM

Abstract

A series of novel indenoisoquinoline derivatives were synthesized. The anticancer activities of these molecules were tested in human cancer cell lines A549, HepG2, and HCT-116. These compounds were also tested for their activity of topoisomerase I (top1) inhibition. Among them, compound 25 was found to be 10-times more potent in cell-killing activity for both cell lines HepG2 and HCT-116 than reported compound 11, with IC(50) of 0.019 and 0.093μM, respectively. Compound 25 was also found to have stronger top1 inhibition activity than 11 in our inhibition assay. Further in vivo evaluations of compound 25 are in progress and will be reported in due course.

Authors+Show Affiliations

Department of Medicinal Chemistry, Jiangsu Key Laboratory of Carcinogenesis and Intervention, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, People's Republic of China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Evaluation Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22079759

Citation

Zhang, Xiaoyun, et al. "Synthesis and Biological Evaluations of Novel Indenoisoquinolines as Topoisomerase I Inhibitors." Bioorganic & Medicinal Chemistry Letters, vol. 22, no. 2, 2012, pp. 1276-81.
Zhang X, Wang R, Zhao L, et al. Synthesis and biological evaluations of novel indenoisoquinolines as topoisomerase I inhibitors. Bioorg Med Chem Lett. 2012;22(2):1276-81.
Zhang, X., Wang, R., Zhao, L., Lu, N., Wang, J., You, Q., Li, Z., & Guo, Q. (2012). Synthesis and biological evaluations of novel indenoisoquinolines as topoisomerase I inhibitors. Bioorganic & Medicinal Chemistry Letters, 22(2), 1276-81. https://doi.org/10.1016/j.bmcl.2011.10.019
Zhang X, et al. Synthesis and Biological Evaluations of Novel Indenoisoquinolines as Topoisomerase I Inhibitors. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1276-81. PubMed PMID: 22079759.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and biological evaluations of novel indenoisoquinolines as topoisomerase I inhibitors. AU - Zhang,Xiaoyun, AU - Wang,Rubing, AU - Zhao,Li, AU - Lu,Na, AU - Wang,Jubo, AU - You,Qidong, AU - Li,Zhiyu, AU - Guo,Qinglong, Y1 - 2011/10/24/ PY - 2011/08/11/received PY - 2011/10/04/revised PY - 2011/10/07/accepted PY - 2011/11/15/entrez PY - 2011/11/15/pubmed PY - 2012/8/25/medline SP - 1276 EP - 81 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 22 IS - 2 N2 - A series of novel indenoisoquinoline derivatives were synthesized. The anticancer activities of these molecules were tested in human cancer cell lines A549, HepG2, and HCT-116. These compounds were also tested for their activity of topoisomerase I (top1) inhibition. Among them, compound 25 was found to be 10-times more potent in cell-killing activity for both cell lines HepG2 and HCT-116 than reported compound 11, with IC(50) of 0.019 and 0.093μM, respectively. Compound 25 was also found to have stronger top1 inhibition activity than 11 in our inhibition assay. Further in vivo evaluations of compound 25 are in progress and will be reported in due course. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/22079759/Synthesis_and_biological_evaluations_of_novel_indenoisoquinolines_as_topoisomerase_I_inhibitors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(11)01407-7 DB - PRIME DP - Unbound Medicine ER -