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Synthesis and antitumor activity of a series of lactone-opened camptothecin derivatives.
- Source :
-
Journal of Asian natural products research [J Asian Nat Prod Res] 2019 Jan; Vol. 21 (1), pp. 51-61. Date of Electronic Publication: 2017 Oct 24. - Publication Year :
- 2019
-
Abstract
- A series of E-ring lactone-opened camptothecin (CPT) derivatives bearing with terminal aza-heterocyclic groups were synthesized, and their antitumor activity was evaluated both in vitro and in vivo. Hydroxyl-amide analogues with morpholin-4-yl displayed excellent antitumor activity in vitro and efficient inhibition on tumor xenograph model in nude mice. Ester-amide compounds acted less active in vitro cytotoxicity and lower inhibition activity in vivo. Substitutions at 7- and 10- positions favored the antitumor activity.
Details
- Language :
- English
- ISSN :
- 1477-2213
- Volume :
- 21
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Journal of Asian natural products research
- Publication Type :
- Academic Journal
- Accession number :
- 29063792
- Full Text :
- https://doi.org/10.1080/10286020.2017.1392941