Synthesis and Antiplatelet Activity of Phenylquinolone Derivatives
| Autor: | Hsieh, Ming-Chieh, 謝明杰 |
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| Rok vydání: | 1997 |
| Druh dokumentu: | 學位論文 ; thesis |
| Popis: | 85 A series of phenylquinolones, 2-phenyl-1,8-naphthyridin-4-ones, monosubstituted 2-phenyl-4-quinolones, disubstituted 2-phenyl-4- quinolones and 4-ethoxycarbonylmethyleneoxo-2-phenylquinoline derivatives were synthesized and their antiplatelet activities were evaluated. The structure-activity relationship of these synthesized compounds were examined. Some of these compounds showed significant activity. Among them, 3-phenyl-4-quinolone (10) and 5-ethyl-2-phenyl-4-quinolone (49) showed very potent inhibitory effect on the platelet aggregation induced by arachidonic acid. These two compounds were thus selected for further pharmacological evaluation, and as the additional lead compounds for further structure modification.On the other hand, 2-phenyl-1,8-naphthyridin-4-one (37) and 6 or 7-methyl-2- phenyl-1,8-naphthyridin-4-one (38, 39) were evaluated in the National Cancer Institute''''s 60 human cancer cell lines in vitro screen. Compound 37, 38 demonstrated the most marked effects in the screen breast cancer cell lines (MDA-MB-435 and MDA-N). This compound has been selected for further in vivo test and as an additional lead compound of anticancer agent. |
| Databáze: | Networked Digital Library of Theses & Dissertations |
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