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Synthesis of 9-(heteroarylmethylidene)amino derivatives of homocamptothecin with biological activities.
Chem Biodivers. 2011 Jul; 8(7):1266-73.CB

Abstract

Six 9-(heteroarylmethylidene)amino derivatives, 2a-2f, of homocamptothecin were synthesized for the first time by total synthesis in 22 steps and biologically evaluated as inhibitors of topoisomerase I. Moreover, the antitumor activities of 2a-2f against three human tumor cell lines, i.e., A-549, MDA-MB-435, and HCT-116, were determined and the results showed that compound 2c was the most active homocamptothecin derivative against the A-549 (IC(50) =0.046 μM) and HTC-116 tumor cells (IC(50) =3.67 μM), with a ca. 50 times higher activity than the reference drug topotecan (TPT) against the lung cancer cell line A-549.

Authors+Show Affiliations

School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR 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 available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

21766447

Citation

Guo, Wei, et al. "Synthesis of 9-(heteroarylmethylidene)amino Derivatives of Homocamptothecin With Biological Activities." Chemistry & Biodiversity, vol. 8, no. 7, 2011, pp. 1266-73.
Guo W, Miao Z, Sheng C, et al. Synthesis of 9-(heteroarylmethylidene)amino derivatives of homocamptothecin with biological activities. Chem Biodivers. 2011;8(7):1266-73.
Guo, W., Miao, Z., Sheng, C., Yao, J., Liu, W., Zhu, L., Zhang, Y., Cheng, P., Dong, G., Zhuang, C., & Zhang, W. (2011). Synthesis of 9-(heteroarylmethylidene)amino derivatives of homocamptothecin with biological activities. Chemistry & Biodiversity, 8(7), 1266-73. https://doi.org/10.1002/cbdv.201000271
Guo W, et al. Synthesis of 9-(heteroarylmethylidene)amino Derivatives of Homocamptothecin With Biological Activities. Chem Biodivers. 2011;8(7):1266-73. PubMed PMID: 21766447.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis of 9-(heteroarylmethylidene)amino derivatives of homocamptothecin with biological activities. AU - Guo,Wei, AU - Miao,Zhenyuan, AU - Sheng,Chunquan, AU - Yao,Jianzhong, AU - Liu,Wenfeng, AU - Zhu,Lingjian, AU - Zhang,Yongqiang, AU - Cheng,Pengfei, AU - Dong,Guoqiang, AU - Zhuang,Chunlin, AU - Zhang,Wannian, PY - 2011/7/19/entrez PY - 2011/7/19/pubmed PY - 2011/11/10/medline SP - 1266 EP - 73 JF - Chemistry & biodiversity JO - Chem. Biodivers. VL - 8 IS - 7 N2 - Six 9-(heteroarylmethylidene)amino derivatives, 2a-2f, of homocamptothecin were synthesized for the first time by total synthesis in 22 steps and biologically evaluated as inhibitors of topoisomerase I. Moreover, the antitumor activities of 2a-2f against three human tumor cell lines, i.e., A-549, MDA-MB-435, and HCT-116, were determined and the results showed that compound 2c was the most active homocamptothecin derivative against the A-549 (IC(50) =0.046 μM) and HTC-116 tumor cells (IC(50) =3.67 μM), with a ca. 50 times higher activity than the reference drug topotecan (TPT) against the lung cancer cell line A-549. SN - 1612-1880 UR - https://www.unboundmedicine.com/medline/citation/21766447/Synthesis_of_9__heteroarylmethylidene_amino_derivatives_of_homocamptothecin_with_biological_activities_ L2 - https://doi.org/10.1002/cbdv.201000271 DB - PRIME DP - Unbound Medicine ER -