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Synthesis and antitumor activity of the hexacyclic camptothecin derivatives.
Bioorg Med Chem Lett. 2005 Jul 01; 15(13):3233-6.BM

Abstract

A series of hexacyclic camptothecin derivatives were synthesized to test for antitumor activity as topoisomerase I inhibitor. The strategy of synthesis was used for the formation of additional furan and dihydrofuran rings fused with 9- and 10-positions of camptothecin. All of the hexacyclic camptothecins were assayed for cytotoxicity against four human tumor cell lines, HL60, BEL-7402, HCT-116, and HeLa, and showed very impressive cytotoxicity activity in vitro. Enzyme activity of the hexacyclic camptothecins was evaluated, being equal or superior to that of SN-38. The stability of four compounds was assessed in human plasma. Two of these compounds were chosen to test for antitumor activity in vivo against Sarcoma-180. The results suggested that additional furan and dihydrofuran rings could improve the antitumor activity in vitro and vivo, though the stability of the lactone ring did not increase.

Authors+Show Affiliations

Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, Graduate School of the Chinese Academy of Sciences, 555, Zuchongzhi Road, Zhangjiang High-Tech Park, Shanghai 201203, 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 available

Pub Type(s)

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

Language

eng

PubMed ID

15913996

Citation

Gao, Heyong, et al. "Synthesis and Antitumor Activity of the Hexacyclic Camptothecin Derivatives." Bioorganic & Medicinal Chemistry Letters, vol. 15, no. 13, 2005, pp. 3233-6.
Gao H, Zhang X, Chen Y, et al. Synthesis and antitumor activity of the hexacyclic camptothecin derivatives. Bioorg Med Chem Lett. 2005;15(13):3233-6.
Gao, H., Zhang, X., Chen, Y., Shen, H., Pang, T., Sun, J., Xu, C., Ding, J., Li, C., & Lu, W. (2005). Synthesis and antitumor activity of the hexacyclic camptothecin derivatives. Bioorganic & Medicinal Chemistry Letters, 15(13), 3233-6.
Gao H, et al. Synthesis and Antitumor Activity of the Hexacyclic Camptothecin Derivatives. Bioorg Med Chem Lett. 2005 Jul 1;15(13):3233-6. PubMed PMID: 15913996.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and antitumor activity of the hexacyclic camptothecin derivatives. AU - Gao,Heyong, AU - Zhang,Xiongwen, AU - Chen,Yi, AU - Shen,Hongwu, AU - Pang,Tao, AU - Sun,Jing, AU - Xu,Chenghui, AU - Ding,Jian, AU - Li,Chuan, AU - Lu,Wei, PY - 2005/03/31/received PY - 2005/04/26/revised PY - 2005/04/28/accepted PY - 2005/5/26/pubmed PY - 2005/10/12/medline PY - 2005/5/26/entrez SP - 3233 EP - 6 JF - Bioorganic & medicinal chemistry letters JO - Bioorg. Med. Chem. Lett. VL - 15 IS - 13 N2 - A series of hexacyclic camptothecin derivatives were synthesized to test for antitumor activity as topoisomerase I inhibitor. The strategy of synthesis was used for the formation of additional furan and dihydrofuran rings fused with 9- and 10-positions of camptothecin. All of the hexacyclic camptothecins were assayed for cytotoxicity against four human tumor cell lines, HL60, BEL-7402, HCT-116, and HeLa, and showed very impressive cytotoxicity activity in vitro. Enzyme activity of the hexacyclic camptothecins was evaluated, being equal or superior to that of SN-38. The stability of four compounds was assessed in human plasma. Two of these compounds were chosen to test for antitumor activity in vivo against Sarcoma-180. The results suggested that additional furan and dihydrofuran rings could improve the antitumor activity in vitro and vivo, though the stability of the lactone ring did not increase. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/15913996/Synthesis_and_antitumor_activity_of_the_hexacyclic_camptothecin_derivatives_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(05)00547-0 DB - PRIME DP - Unbound Medicine ER -