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Synthesis and biological evaluation of 7-alkenyl homocamptothecins as potent topoisomerase I inhibitors.
Chem Biodivers. 2012 Jun; 9(6):1084-94.CB

Abstract

Homocamptothecin (hCPT) is a camptothecin (CPT) derivative with a seven-membered β-hydroxylactone E ring, which shows higher lactone stability and improves topoisomerase I (Topo I) inhibition activity. In an attempt to improve the antitumor activity of homocamptothecins, a series of 7-alkenyl-homocamptothecin derivatives was designed and synthesized based on a semisynthetic route starting from CPT. Most of the synthesized compounds exhibit higher cytotoxic activities on the A-549 tumor cell line than topotecan (TPT). Some compounds such as 2a and 2o show a broad in vitro antitumor spectrum and exhibit superior Topo I-inhibition activity.

Authors+Show Affiliations

School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P. R. 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 available

Pub Type(s)

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

Language

eng

PubMed ID

22700227

Citation

Zhu, Lingjian, et al. "Synthesis and Biological Evaluation of 7-alkenyl Homocamptothecins as Potent Topoisomerase I Inhibitors." Chemistry & Biodiversity, vol. 9, no. 6, 2012, pp. 1084-94.
Zhu L, Zhang X, Lei N, et al. Synthesis and biological evaluation of 7-alkenyl homocamptothecins as potent topoisomerase I inhibitors. Chem Biodivers. 2012;9(6):1084-94.
Zhu, L., Zhang, X., Lei, N., Liu, W., Miao, Z., Zhuang, C., Sheng, C., Guo, W., Dong, G., Yao, J., Cheng, P., & Zhang, W. (2012). Synthesis and biological evaluation of 7-alkenyl homocamptothecins as potent topoisomerase I inhibitors. Chemistry & Biodiversity, 9(6), 1084-94. https://doi.org/10.1002/cbdv.201100195
Zhu L, et al. Synthesis and Biological Evaluation of 7-alkenyl Homocamptothecins as Potent Topoisomerase I Inhibitors. Chem Biodivers. 2012;9(6):1084-94. PubMed PMID: 22700227.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and biological evaluation of 7-alkenyl homocamptothecins as potent topoisomerase I inhibitors. AU - Zhu,Lingjian, AU - Zhang,Xianghua, AU - Lei,Ning, AU - Liu,Wenfeng, AU - Miao,Zhenyuan, AU - Zhuang,Chunlin, AU - Sheng,Chunquan, AU - Guo,Wei, AU - Dong,Guoqiang, AU - Yao,Jianzhong, AU - Cheng,Pengfei, AU - Zhang,Wannian, PY - 2012/6/16/entrez PY - 2012/6/16/pubmed PY - 2012/10/30/medline SP - 1084 EP - 94 JF - Chemistry & biodiversity JO - Chem. Biodivers. VL - 9 IS - 6 N2 - Homocamptothecin (hCPT) is a camptothecin (CPT) derivative with a seven-membered β-hydroxylactone E ring, which shows higher lactone stability and improves topoisomerase I (Topo I) inhibition activity. In an attempt to improve the antitumor activity of homocamptothecins, a series of 7-alkenyl-homocamptothecin derivatives was designed and synthesized based on a semisynthetic route starting from CPT. Most of the synthesized compounds exhibit higher cytotoxic activities on the A-549 tumor cell line than topotecan (TPT). Some compounds such as 2a and 2o show a broad in vitro antitumor spectrum and exhibit superior Topo I-inhibition activity. SN - 1612-1880 UR - https://www.unboundmedicine.com/medline/citation/22700227/Synthesis_and_biological_evaluation_of_7_alkenyl_homocamptothecins_as_potent_topoisomerase_I_inhibitors_ L2 - https://doi.org/10.1002/cbdv.201100195 DB - PRIME DP - Unbound Medicine ER -