Imino-tetrahydro-benzothiazole derivatives as p53 inhibitors: discovery of a highly potent in vivo inhibitor and its action mechanism

N Pietrancosta, A Moumen, R Dono…

Index: Pietrancosta, Nicolas; Maina, Flavio; Dono, Rosanna; Moumen, Anice; Garino, Cedrik; Laras, Younes; Burlet, Stephane; Quelever, Gilles; Kraus, Jean-Louis Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 6 p. 1561 - 1564

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Citation Number: 73

Abstract

Several neurological disorders manifest symptoms that result from the degeneration and death of specific neurons. p53 is an important modulator of cell death, and its inhibition could be a therapeutic approach to several neuropathologies. Here, we report the design, synthesis, and biological evaluation of novel p53 inhibitors based on the imino- tetrahydrobenzothiazole scaffold. By performing studies on their mechanism of action, we ...