Phospholipase C inhibitors: a new class of agents

…, SF Chen, DL Behrens, RFIII Kaltenbach…

Index: Perrella; Chen; Behrens; Kaltenbach III; Seitz Journal of Medicinal Chemistry, 1994 , vol. 37, # 14 p. 2232 - 2237

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Citation Number: 41

Abstract

A series of nitrocoumarin and nitrochromene derivatives have been prepared and shown to inhibit the phosphatidylinositol-specific phospholipase C (PLC)(ICW C 10 pg/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 (I&= 4 pg/mL) in a manner consistent with their proposed mode of activity. Finally, the ...