Abstract

Ethynyl-4(3H)quinazolinone and 2-(1,3-butadienyl)-4(3H)quinazolinone have been synthesized by cyclizations from appropriate precursors. These two molecules are of interest as analogues of the known p-53 reactivator 2-vinyl-4(3H)quinazolinone.

Highlights

  • The tumor suppressor protein p-53 is expressed at low levels in most cells and tissues under normal conditions

  • We have recently demonstrated that 2-vinyl-4(3H)quinazolinone (1) is a interesting reactivator of p-53.2 The effect is similar to, but stronger than, that of CP-31398, 2

  • After a period at reflux the solvent was evaporated and the residue dissolved in dioxane (30 mL); 2aminobenzamide (13.6 g, 0.1 mol) was added, and the mixture heated (75 °C, 1h)

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Summary

Introduction

The tumor suppressor protein p-53 is expressed at low levels in most cells and tissues under normal conditions. Cellular stress such as DNA damage, oncogene activation induces p-53 protein levels, leading to an array of biological responses. The high frequency of p-53 mutations in human tumors, and the high levels of mutant p-53 expression in tumors makes p-53 an attractive target for novel cancer therapy.. Several studies have demonstrated ways to restore normal function to mutant p-53.2 The high frequency of p-53 mutations in human tumors, and the high levels of mutant p-53 expression in tumors makes p-53 an attractive target for novel cancer therapy. Several studies have demonstrated ways to restore normal function to mutant p-53.2

Results and Discussion
Cl O
OH O
OO O
Experimental Section

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