| Autor: |
Steven P. Seitz, Frank W. Perrella, Davette L. Behrens, Shih-Fong Chen, Robert F. Kaltenbach |
| Rok vydání: |
2010 |
| Předmět: |
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| Zdroj: |
ChemInform. 25 |
| ISSN: |
0931-7597 |
| DOI: |
10.1002/chin.199448154 |
| Popis: |
A series of nitrocoumarin and nitrochromene derivatives have been prepared and shown to inhibit the phosphatidylinositol-specific phospholipase C(PLC)(IC50 < 10 micrograms/mL) isolated from human melanoma. The inhibition of PLC by nitrocoumarin 4a was time-dependent and irreversible. The inhibition of PLC was shown to interfere with inositide metabolism in whole cells (IC50 = 4 micrograms/mL) in a manner consistent with their proposed mode of activity. Finally, the compounds were shown to be growth inhibitory to cultured melanoma cells (ID50 = 2 micrograms/mL), suggesting that PLC may be an attractive new target for chemotherapeutic intervention. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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