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Cytotoxic evaluation of sarcodifurines A and B, two novel dihydrofuroquinolines from Sarcomelicope follicularis (Rutaceae)
- Source :
- Journal of enzyme inhibition and medicinal chemistry. 23(5)
- Publication Year :
- 2008
-
Abstract
- Sarcodifurines A and B are two original dihydrofuroquinolines isolated from Sarcomelicope follicularis, a New Caledonian tree. The cytotoxicity and antiproliferative activity of these two alkaloids were investigated against 8 distinct cell lines representative of the most frequent solid tumors developing in human. Cytotoxicity of sarcodifurines was low on the 8 cell lines, with, for example, less than 10% of the total cells killed after 24 h exposure at 10 microM and IC(50) approximately 7.10(-5) M (MCF-7 and MDA MB 231 cell lines). Proliferation studies confirmed that sarcodifurines had a weak effect on cancer cells growth, with less than 5% growth inhibition at 10 microM. Sarcodifurine A activity was comparable to that of Sarcodifurine B, in term of cytotoxicity and antiproliferative activity on all cell lines. In spite of the weak activity of sarcodifurines and furoquinolines, rationalized pharmacomodulations to obtain planar analogs could lead to efficient topoisomerases inhibitors and DNA intercalants.
- Subjects :
- Stereochemistry
Topoisomerase Inhibitors
Biology
chemistry.chemical_compound
Cell Line, Tumor
Drug Discovery
Cytotoxic T cell
Humans
Cytotoxicity
Furans
IC50
Rutaceae
Cell Proliferation
Pharmacology
Cell Death
Topoisomerase
General Medicine
Molecular biology
Intercalating Agents
chemistry
Cell culture
Cancer cell
biology.protein
Quinolines
Growth inhibition
DNA
Subjects
Details
- ISSN :
- 14756374
- Volume :
- 23
- Issue :
- 5
- Database :
- OpenAIRE
- Journal :
- Journal of enzyme inhibition and medicinal chemistry
- Accession number :
- edsair.doi.dedup.....d94a607deec10bef2e67915dcb84522c