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Beta'-hydroxy-alpha,beta-unsaturated ketones: a new pharmacophore for the design of anticancer drugs.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Apr 15; Vol. 16 (8), pp. 2266-9. Date of Electronic Publication: 2006 Jan 24. - Publication Year :
- 2006
-
Abstract
- A series of beta'-hydroxy-alpha,beta-unsaturated ketones were prepared by means of an iron(III) catalyzed domino process. The in vitro antiproliferative activities were examined in the human solid tumor cell lines A2780, SW1573, and WiDr. The results showed that beta'-hydroxy-alpha,beta-unsaturated ketones were more potent than alpha,beta-unsaturated ketones. The best activity profiles were obtained for the derivatives bearing cyclic or branched substituents on the side chains.
- Subjects :
- Antineoplastic Agents pharmacology
Catalysis
Cations
Colonic Neoplasms pathology
Drug Design
Female
Humans
Ketones pharmacology
Lung Neoplasms pathology
Ovarian Neoplasms pathology
Structure-Activity Relationship
Tumor Cells, Cultured
Antineoplastic Agents chemical synthesis
Cell Proliferation drug effects
Iron chemistry
Ketones chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 16
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 16439115
- Full Text :
- https://doi.org/10.1016/j.bmcl.2006.01.023