Citation
Liu, Wenfeng, et al. "Synthesis and Biological Evaluation of Novel 7-acyl Homocamptothecins as Topoisomerase I Inhibitors." European Journal of Medicinal Chemistry, vol. 46, no. 6, 2011, pp. 2408-14.
Liu W, Zhu L, Guo W, et al. Synthesis and biological evaluation of novel 7-acyl homocamptothecins as Topoisomerase I inhibitors. Eur J Med Chem. 2011;46(6):2408-14.
Liu, W., Zhu, L., Guo, W., Zhuang, C., Zhang, Y., Sheng, C., Cheng, P., Yao, J., Wang, W., Dong, G., Wang, S., Miao, Z., & Zhang, W. (2011). Synthesis and biological evaluation of novel 7-acyl homocamptothecins as Topoisomerase I inhibitors. European Journal of Medicinal Chemistry, 46(6), 2408-14. https://doi.org/10.1016/j.ejmech.2011.03.024
Liu W, et al. Synthesis and Biological Evaluation of Novel 7-acyl Homocamptothecins as Topoisomerase I Inhibitors. Eur J Med Chem. 2011;46(6):2408-14. PubMed PMID: 21463912.
TY - JOUR
T1 - Synthesis and biological evaluation of novel 7-acyl homocamptothecins as Topoisomerase I inhibitors.
AU - Liu,Wenfeng,
AU - Zhu,Lingjian,
AU - Guo,Wei,
AU - Zhuang,Chunlin,
AU - Zhang,Yongqiang,
AU - Sheng,Chunquan,
AU - Cheng,Pengfei,
AU - Yao,Jianzhong,
AU - Wang,Wenya,
AU - Dong,Guoqiang,
AU - Wang,Shengzheng,
AU - Miao,Zhenyuan,
AU - Zhang,Wannian,
Y1 - 2011/03/23/
PY - 2011/01/11/received
PY - 2011/03/07/revised
PY - 2011/03/13/accepted
PY - 2011/4/6/entrez
PY - 2011/4/6/pubmed
PY - 2011/9/13/medline
SP - 2408
EP - 14
JF - European journal of medicinal chemistry
JO - Eur J Med Chem
VL - 46
IS - 6
N2 - A series of novel 7-acyl derivatives of homocamptothecin (hCPT) were designed and synthesized with the purpose to improve antitumor activity of hCPT, via Minisci free-radical reaction from 10-methoxyhomocamptothecin. All the compounds were evaluated for in vitro cytotoxicity against three cancer cell lines (A549, MDA-MB-435 and HCT116). For MDA-MB-435 cell line, compounds, 6a, 6b, 6k and all of 7-alkylcabonyl homocamptothecin derivatives showed higher in vitro inhibitory activities than topotecan (TPT). Furthermore, compounds 6d, 6e, and 6k showed highly potent inhibitory activities with the IC50 values from less than 1 nM to 2.2 nM. In Topoisomerase I (Topo I)-induced DNA cleavage assay, compounds 6a, 6d, and 6k, as compared to CPT, revealed higher Topo I inhibitory activity.
SN - 1768-3254
UR - https://www.unboundmedicine.com/medline/citation/21463912/Synthesis_and_biological_evaluation_of_novel_7_acyl_homocamptothecins_as_Topoisomerase_I_inhibitors_
L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(11)00238-8
DB - PRIME
DP - Unbound Medicine
ER -