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Synthesis and antitumor activity of novel 20s-camptothecin analogues.
Bioorg Med Chem Lett. 2009 Jan 15; 19(2):513-5.BM

Abstract

In an effort to decrease the toxicity and improve the stability of labile lactone ring of camptothecin, nitrogenous heterocyclic aromatic groups were introduced into 20-position of camptothecin and seventeen new 20s-camptothecin derivatives were obtained in quantitative yield. The cytotoxicity in vitro on three cancer cell lines and the stability of the lactone in phosphate-buffered solution (PBS) of these derivatives were evaluated. Most of these tested derivatives possessed better cytotoxicity than topotecan. Analogues 6, 12 exhibited the best antitumor activity in vivo in all derivatives we prepared. The results suggested that introduction of pyrazole in 10- or 20-position of camptothecin could promote antitumor activity in vitro and in vivo, simultaneously bring much increase of the stability of lactone.

Authors+Show Affiliations

Key Laboratory of Forest Plant Ecology, Northeast Forestry University, Ministry of Education, No. 26 Hexing Road, Harbin 150040, China. li_qingyong@163.comNo 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

19056266

Citation

Li, Qingyong, et al. "Synthesis and Antitumor Activity of Novel 20s-camptothecin Analogues." Bioorganic & Medicinal Chemistry Letters, vol. 19, no. 2, 2009, pp. 513-5.
Li Q, Lv H, Zu Y, et al. Synthesis and antitumor activity of novel 20s-camptothecin analogues. Bioorg Med Chem Lett. 2009;19(2):513-5.
Li, Q., Lv, H., Zu, Y., Qu, Z., Yao, L., Su, L., Liu, C., & Wang, L. (2009). Synthesis and antitumor activity of novel 20s-camptothecin analogues. Bioorganic & Medicinal Chemistry Letters, 19(2), 513-5. https://doi.org/10.1016/j.bmcl.2008.11.031
Li Q, et al. Synthesis and Antitumor Activity of Novel 20s-camptothecin Analogues. Bioorg Med Chem Lett. 2009 Jan 15;19(2):513-5. PubMed PMID: 19056266.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and antitumor activity of novel 20s-camptothecin analogues. AU - Li,Qingyong, AU - Lv,Hongyan, AU - Zu,Yuangang, AU - Qu,Zhenhuan, AU - Yao,Liping, AU - Su,Lin, AU - Liu,Chen, AU - Wang,Limin, Y1 - 2008/11/14/ PY - 2008/08/01/received PY - 2008/11/04/revised PY - 2008/11/11/accepted PY - 2008/12/6/pubmed PY - 2009/3/3/medline PY - 2008/12/6/entrez SP - 513 EP - 5 JF - Bioorganic & medicinal chemistry letters JO - Bioorg. Med. Chem. Lett. VL - 19 IS - 2 N2 - In an effort to decrease the toxicity and improve the stability of labile lactone ring of camptothecin, nitrogenous heterocyclic aromatic groups were introduced into 20-position of camptothecin and seventeen new 20s-camptothecin derivatives were obtained in quantitative yield. The cytotoxicity in vitro on three cancer cell lines and the stability of the lactone in phosphate-buffered solution (PBS) of these derivatives were evaluated. Most of these tested derivatives possessed better cytotoxicity than topotecan. Analogues 6, 12 exhibited the best antitumor activity in vivo in all derivatives we prepared. The results suggested that introduction of pyrazole in 10- or 20-position of camptothecin could promote antitumor activity in vitro and in vivo, simultaneously bring much increase of the stability of lactone. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/19056266/Synthesis_and_antitumor_activity_of_novel_20s_camptothecin_analogues_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(08)01401-7 DB - PRIME DP - Unbound Medicine ER -