Novel pyrimidinyl pyrazole derivatives were synthesized and examined for cytotoxic and antitumor activity. Mannich reaction was employed to construct this scaffold. Among the compounds synthesized, a series of propene derivatives exhibited a potent cytotoxic activity against some tumor cell lines including multidrug resistant cell lines due to the overexpression of P-glycoprotein. The vinyl bon...

A new class of quinoline derivatives containing pyrazoline-5-one and pyrazole moiety (3a-j and 4a-j) have been synthesized by condensation of various oxobutyrates/pentane-2,4-dione derivatives with 8-quinolinoxyacetic acid hydrazide. Elemental analysis, IR, H NMR and mass spectral data support the structures of the newly synthesized compounds. The synthesized compounds have been evaluated for t...

A series of novel pyrazoline derivatives 5-(substituted aryl)-3-(3,4-dimethoxyphenyl)-1-(2,4dinitrophenyl)-4,5-dihydro-1H-pyrazole (5a-l) were synthesized by heating 2,4-dinitrophenyl hydrazine (4) with (E)-3-(3,4-dimethoxyphenyl)-1-substituted aryl prop-2-en-1-one (3) in presence of catalytic amount of concentrated H2SO4. The structures of the novel derivatives were confirmed by various spectr...

A series of pyrano[2,3-c]pyrazole derivatives of indole was synthesized by multi-component reactions using the conventional and microwave irradiation approach. Particularly valuable features of this method include high yield, broad substrate scope, shorter reaction times and straightforward procedure. Antimicrobial screening of the synthesized derivatives against eight human pathogens, namely B...

The reaction of cyanoacetyl hydrazine (1) with the -haloketones 2a-2c in 1,4-dioxane afforded the hydrazidehydrazone derivatives 3a-3c. The latter products were used in a series of heterocyclization to give 1,3,4-oxadiazine, 1,2,4triazine and pyrazole derivatives. All compounds synthesized through this work are new products and their antitumor evaluation towards three human tumor cell lines rep...

Background: Pyrazolopyridines are heterocyclic compounds with nitrogen atoms in the ring, and they have been used as one of important pharmacophores drug design. Pyrazole derivatives synthesised applied pharmaceutical industry active drugs. The recent commercial success pyrazole COX-2 inhibitors has brought even more attention to significance this ring medicinal chemistry. Objective: This study...

A facile and eminent method has been reported for the preparation of amido alkyl naphthols. Amido naphthol derivatives were synthesized by condensation pyrazole aldehydes, β-naphthol acetamide in presence a heterogeneous SiO2 supported sodium hydrogen sulphate catalyst using acetic acid as solvent. This protocol is advantageous its shorter reaction hours, simplest workup technique, excellent yi...

Hydrazonyl bromides 2a,b reacted with active methylene compounds (dibenzoylmethane, acetylacetone, ethyl acetoacetate, phenacyl cyanide, acetoacetanilide, ethyl cyanoacetate, cyanoacetamide and malononitrile) to afford the corresponding 1,3,4,5- tetrasubstituted pyrazole derivatives 5-12a,b. Reaction of 12a,b with formamide, formic acid and triethyl orthoformate give the pyrazolo[3,4-d]pyrimidi...

4-Imino-1-p-tolyl-1,4-dihydropyrazolo[3,4-d]pyrimidin-5-ylamine (2) and (1-p-tolyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-hydrazine (3) were prepared starting from ethyl 4-cyano-1-p-tolyl-1H-pyrazol-5-ylimidoformate (1). The structure of compound 3 was confirmed through preparation of the pyrazole derivatives 4 and 5. Also, the synthesis and structural characterization of pyrazolo[4,3-e][1,2,4]triaz...

Three new 2-methoxy acetylenic acids (1-3) and a known derivative (4), in addition to three new natural pyrazole alkaloids (5-7) were isolated from an Indonesian marine sponge of the genus Cinachyrella. Compounds 5 and 6 have previously been reported as synthetic compounds. The structures of the new compounds were established on the basis of one- and two-dimensional NMR spectroscopy as well as ...