Phospholipase C Inhibitors: A New Class of Agents

Autor:	Shih-Fong Chen, Frank W. Perrella, Steven P. Seitz, Robert F. Kaltenbach, Davette L. Behrens
Rok vydání:	1994
Předmět:	chemistry.chemical_classification Phospholipase C biology Chemistry Biological activity Metabolism Pharmacology In vitro Enzyme Biochemistry Enzyme inhibitor Drug Discovery biology.protein Molecular Medicine Cytotoxicity IC50
Zdroj:	Journal of Medicinal Chemistry. 37:2232-2237
ISSN:	1520-4804 0022-2623
DOI:	10.1021/jm00040a016
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:	https://explore.openaire.eu/search/publication?articleId=doi_________::e48d3c71af7b89aa097391312eec1427 https://doi.org/10.1021/jm00040a016 Zobrazit plný text záznamu