Amidrazones as Precursors of Biologically Active Compounds – Synthesis of Diaminopyrazoles for Evaluation of Anticancer Activity

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.

Synthesis, antiviral, cytotoxicity and antitumor evaluations of A4 type of porphyrin derivatives

“…1H-Pyrazole based heterocyclic structures have also attracted a synthetic interest for being essential moieties in many chemotherapeutic agents with potential antiparasitic [27], antimalarial [28] and antiviral activities [29,30]. As far as the anticancer activity is concerned, literature citation revealed that a wide range of pyrazole derivatives was reported to contribute to a variety of antineoplastic potentials against a wide range of cancer cell lines [31,32]. In this research work, we report for the first time the synthesis and characterization of novel meso-tetrapyrazolylporphyrins and their pharmaceutical screening as antiviral and antitumor agents.…”

A convenient synthesis and molecular modeling study of novel pyrazolo[3,4-d]pyrimidine and pyrazole derivatives as anti-tumor agents

“…Furthermore, it has also been found that 1H-pyrazole based heterocyclic structures have attracted synthetic interest for being an essential moieties in many chemotherapeutic agents with potential antiparasitic 19,20 , anti-malarial 21 and antiviral activities 22,23 . As far as the anticancer activity is concerned, literature citation revealed that a wide range of pyrazole derivatives were reported to contribute to a variety of anti-neoplastic potentials against a wide range of cancer cell lines [24][25][26][27] . Moreover, many pyrazole derivatives are associated with anti-fungal, anti-bacterial 28 and antipyretic 29 properties.…”

Synthesis and Anticancer Activity of New Substituted Pyrazoles and Their Derived 1,2,4‐Triazoles and Sugar Derivatives

“…Pyrazole‐based heterocyclic structures have also attracted synthetic interest for being essential moieties in many chemotherapeutic agents with potential antiparasitic , antimalarial , and antiviral activities . As far as the anticancer activity is concerned, literature citation revealed that a wide range of pyrazole derivatives were reported to contribute to a variety of antineoplastic potentials against a wide range of cancer cell lines . On the other hand, 1,2,4‐triazole derivatives are known to exhibit antimicrobial , antitubercular , anticancer , anticonvulsant , anti‐inflammatory, and analgesic properties.…”