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Parallel synthesis and cytotoxicity evaluation of a polyamine-quinone conjugates library.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2008 Sep 11; Vol. 51 (17), pp. 5463-7. Date of Electronic Publication: 2008 Aug 13. - Publication Year :
- 2008
-
Abstract
- A library of 24 derivatives designed by combining two natural products-derived fragments was prepared and tested to determine their anticancer potential in HT29 colon cancer cells. All library members inhibit cell proliferation as measured by MTT mitochondrial functional assay, with IC50 values in the 1-100 microM range. Entry 1b caused apoptotic EGFR-mediated intracellular signaling. Thus, polyamino-quinones emerged as readily accessible and easily diversified scaffolds for anticancer lead discovery.
- Subjects :
- Antineoplastic Agents pharmacology
Apoptosis drug effects
Cell Proliferation drug effects
Colonic Neoplasms drug therapy
Combinatorial Chemistry Techniques
Drug Screening Assays, Antitumor
ErbB Receptors metabolism
HT29 Cells
Humans
Inhibitory Concentration 50
Polyamines chemistry
Quinones chemistry
Structure-Activity Relationship
Antineoplastic Agents chemistry
Polyamines pharmacology
Quinones pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 51
- Issue :
- 17
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 18698755
- Full Text :
- https://doi.org/10.1021/jm800637b