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1. Amidrazones as precursors of biologically active compounds--synthesis of diaminopyrazoles for evaluation of anticancer activity.

Author

Cocco MT, Congiu C, Lilliu V, and Onnis V

Subjects
Antineoplastic Agents pharmacology, Cell Line, Tumor, Cell Proliferation drug effects, Diamines pharmacology, Humans, Isocyanates chemistry, Pyrazoles pharmacology, Antineoplastic Agents chemical synthesis, Diamines chemical synthesis, Hydrazones chemistry, Pyrazoles chemical synthesis
Abstract

The regioselectivity of coupling phenyl isocyanate to 3-(2-acylhydrazino)-3-aminopropenenitriles and ethyl 3-(2-acylhydrazino)-3-aminopropenoates as simple access to aminopyrazole derivatives, endowed with potential antitumoral activity, is reported. 3-(2-Acylhydrazino)-3-aminopropenenitriles react with phenyl isocyanate to afford 3-amino-3-(2-acylhydrazino)-2-phenylaminocarbonyl-2-propenenitriles. These key intermediates were cyclized into 3,5-diaminopyrazole-4-carboxamide derivatives. Preliminary results of poor antiproliferative activities of these compounds are also reported.

Published
2006
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