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Synthesis and evaluation of 9-benzylideneamino derivatives of homocamptothecin as potent inhibitors of DNA topoisomerase I.
Eur J Med Chem. 2010 Jun; 45(6):2223-8.EJ

Abstract

A series of novel 9-benzylideneamino derivatives of homocamptothecin were synthesized via Friedlaender cyclization from our obtained intermediate 5. All the compounds were evaluated for in vitro cytotoxicity against three cancer cell lines (A549, LOVO and MDA-MB-435). Most of these derivatives possessed potent growth inhibitory effect on all the tested cell lines and four compounds (6d, 6f, 6i, 6k) showed higher inhibitory activities with the IC50 values of 2.3 nM-9.8 nM against breast cancer cell than topotecan. As compared to CPT, compound 6f revealed higher topoisomerase I inhibitory activity.

Authors+Show Affiliations

School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, 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 availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

20202723

Citation

Guo, Wei, et al. "Synthesis and Evaluation of 9-benzylideneamino Derivatives of Homocamptothecin as Potent Inhibitors of DNA Topoisomerase I." European Journal of Medicinal Chemistry, vol. 45, no. 6, 2010, pp. 2223-8.
Guo W, Miao Z, Sheng C, et al. Synthesis and evaluation of 9-benzylideneamino derivatives of homocamptothecin as potent inhibitors of DNA topoisomerase I. Eur J Med Chem. 2010;45(6):2223-8.
Guo, W., Miao, Z., Sheng, C., Yao, J., Feng, H., Zhang, W., Zhu, L., Liu, W., Cheng, P., Zhang, J., Che, X., Wang, W., Luo, C., & Xu, Y. (2010). Synthesis and evaluation of 9-benzylideneamino derivatives of homocamptothecin as potent inhibitors of DNA topoisomerase I. European Journal of Medicinal Chemistry, 45(6), 2223-8. https://doi.org/10.1016/j.ejmech.2010.01.063
Guo W, et al. Synthesis and Evaluation of 9-benzylideneamino Derivatives of Homocamptothecin as Potent Inhibitors of DNA Topoisomerase I. Eur J Med Chem. 2010;45(6):2223-8. PubMed PMID: 20202723.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and evaluation of 9-benzylideneamino derivatives of homocamptothecin as potent inhibitors of DNA topoisomerase I. AU - Guo,Wei, AU - Miao,Zhenyuan, AU - Sheng,Chunquan, AU - Yao,Jianzhong, AU - Feng,Hao, AU - Zhang,Wannian, AU - Zhu,Lingjian, AU - Liu,Wenfeng, AU - Cheng,Pengfei, AU - Zhang,Jing, AU - Che,Xiaoying, AU - Wang,Wenya, AU - Luo,Chuan, AU - Xu,Yulan, Y1 - 2010/02/01/ PY - 2009/10/24/received PY - 2010/01/05/revised PY - 2010/01/27/accepted PY - 2010/3/6/entrez PY - 2010/3/6/pubmed PY - 2010/7/28/medline SP - 2223 EP - 8 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 45 IS - 6 N2 - A series of novel 9-benzylideneamino derivatives of homocamptothecin were synthesized via Friedlaender cyclization from our obtained intermediate 5. All the compounds were evaluated for in vitro cytotoxicity against three cancer cell lines (A549, LOVO and MDA-MB-435). Most of these derivatives possessed potent growth inhibitory effect on all the tested cell lines and four compounds (6d, 6f, 6i, 6k) showed higher inhibitory activities with the IC50 values of 2.3 nM-9.8 nM against breast cancer cell than topotecan. As compared to CPT, compound 6f revealed higher topoisomerase I inhibitory activity. SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/20202723/Synthesis_and_evaluation_of_9_benzylideneamino_derivatives_of_homocamptothecin_as_potent_inhibitors_of_DNA_topoisomerase_I_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(10)00108-X DB - PRIME DP - Unbound Medicine ER -