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Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin.
Bioorg Med Chem Lett. 2005 Apr 15; 15(8):2003-6.BM

Abstract

A series of new camptothecin derivatives, as topoisomerase I inhibitor, were synthesized to identify potent antitumor agents. The synthesis method was based on the Claisen rearrangement of 10-allyloxy-7-ethylcamptothecin. All of the compounds were assayed for cytotoxicity against two human tumor cell lines, Bel7402, HCT116, and showed good potency in vitro. Compounds 2, 4, 9, were assessed for the stability of lactone in human plasma. And then compound 2 was tested for antitumor activity in vitro against mouse tumor sarcoma-180. The results suggested that the small alkyl groups in the both 7- and 9-positions of camptothecin could promote liposolubility, antitumor activity in vitro and vivo, though did not bring much increase of the stability of lactone.

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 available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

15808456

Citation

Gao, Heyong, et al. "Synthesis and Antitumor Activity of 7-ethyl-9-alkyl Derivatives of Camptothecin." Bioorganic & Medicinal Chemistry Letters, vol. 15, no. 8, 2005, pp. 2003-6.
Gao H, Zhang X, Chen Y, et al. Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin. Bioorg Med Chem Lett. 2005;15(8):2003-6.
Gao, H., Zhang, X., Chen, Y., Shen, H., Sun, J., Huang, M., Ding, J., Li, C., & Lu, W. (2005). Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin. Bioorganic & Medicinal Chemistry Letters, 15(8), 2003-6.
Gao H, et al. Synthesis and Antitumor Activity of 7-ethyl-9-alkyl Derivatives of Camptothecin. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2003-6. PubMed PMID: 15808456.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin. AU - Gao,Heyong, AU - Zhang,Xiongwen, AU - Chen,Yi, AU - Shen,Hongwu, AU - Sun,Jing, AU - Huang,Min, AU - Ding,Jian, AU - Li,Chuan, AU - Lu,Wei, PY - 2004/12/29/received PY - 2005/02/21/revised PY - 2005/02/22/accepted PY - 2005/4/6/pubmed PY - 2005/8/19/medline PY - 2005/4/6/entrez SP - 2003 EP - 6 JF - Bioorganic & medicinal chemistry letters JO - Bioorg. Med. Chem. Lett. VL - 15 IS - 8 N2 - A series of new camptothecin derivatives, as topoisomerase I inhibitor, were synthesized to identify potent antitumor agents. The synthesis method was based on the Claisen rearrangement of 10-allyloxy-7-ethylcamptothecin. All of the compounds were assayed for cytotoxicity against two human tumor cell lines, Bel7402, HCT116, and showed good potency in vitro. Compounds 2, 4, 9, were assessed for the stability of lactone in human plasma. And then compound 2 was tested for antitumor activity in vitro against mouse tumor sarcoma-180. The results suggested that the small alkyl groups in the both 7- and 9-positions of camptothecin could promote liposolubility, antitumor activity in vitro and vivo, though did not bring much increase of the stability of lactone. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/15808456/Synthesis_and_antitumor_activity_of_7_ethyl_9_alkyl_derivatives_of_camptothecin_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(05)00264-7 DB - PRIME DP - Unbound Medicine ER -