The reaction of cyanoacetylhydrazine with chloroacetyl chloride gave N?-(2-chloroacetyl)-2-cyanoacetohydrazide. The latter underwent cyclization to afford 1-(5 amino-3-hydroxy-1H-pyrazol-1-yl)-2-chloroethanone, which underwent nucleophilic substitution to give 3-(5-amino-3-hydroxy-1H- pyrazol-1-yl)-3-oxopropanenitrile. The latter two compounds were used as key synthons to synthesize new thiophene, pyran, thiazole and some fused heterocyclic derivatives. The antitumor activity of the newly synthesized compounds was evaluated against three human tumor cells lines, namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268) and some of these compounds were found to exhibit much higher inhibitory effects towards the three tumor cell lines than the Gram positive control doxorubicin. � 2012 by the authors.
Background: Chalcones, 2-pyrazolines and thiazoles have been reported to possess various pharmacological activities. Objective: Synthesis of new chalcones and utilizing them as a building block for constructing a series ...
Hassan G.S.; Abdel Rahman D.E.; Abdelmajeed E.A.; Refaey R.H.; Alaraby Salem M.; Nissan Y.M.(Elsevier Masson SAS, 2019)
New pyrazole derivatives 2�5 were synthesized and evaluated for their COX-1 and COX-2 inhibitory activity in vitro. All compounds showed good inhibitory activity at a nanomolar level and most compounds exhibited selectivity ...
Abbas I.M.; Abdallah M.A.; Gomha S.M.; Kazem M.S.H.(HeteroCorporation, 2017)
A new series of azolopyrimidine derivatives incorporating pyrazole moiety were synthesized by reaction of 1-(pyrazol-3-yl)-2-propenone with a number of heterocyclic amines in the presence of a catalytic amount of acetic ...