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Synthesis of novel 5-(3-alkylquinolin-2-yl)-3-aryl isoxazole derivatives and their cytotoxic activity.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2014 Mar 01; Vol. 24 (5), pp. 1349-51. Date of Electronic Publication: 2014 Jan 25. - Publication Year :
- 2014
-
Abstract
- The propargyl alcohol on reaction with aldoxime and NaOCl in DCM gave exclusively (3-arylisoxazol-5-yl) methanol 1. The compound 1 was oxidized to an aldehyde 2 followed by reaction with aniline resulted in Schiff's base 3. The compounds 3 were further reacted with various aldehydes having α-hydrogen using molecular iodine as catalyst and which yielded 5-(3-alkylquinolin-2-yl)-3-aryl isoxazole derivatives 4. All the final compounds 4 were screened against four human cancer cell lines (A549, COLO 205, MDA-MB 231 and PC-3) and among these compounds 4n showed potent cytotoxicity against all the cell lines at IC50 values of <12 μM.<br /> (Copyright © 2014 Elsevier Ltd. All rights reserved.)
- Subjects :
- Aniline Compounds chemistry
Antineoplastic Agents chemistry
Antineoplastic Agents toxicity
Cell Line, Tumor
Cell Survival drug effects
Drug Screening Assays, Antitumor
Humans
Isoxazoles chemical synthesis
Isoxazoles toxicity
Schiff Bases chemistry
Antineoplastic Agents chemical synthesis
Isoxazoles chemistry
Quinolines chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 24
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24507927
- Full Text :
- https://doi.org/10.1016/j.bmcl.2014.01.038