Abstract

DESIGN, SYNTHESIS AND IN-VIVO ANTI-TUMOUR ACTIVITIES OF SOME NOVEL 2-((1H-INDOL-4-YL) OXY)-1-(4,5-DIPHENYL-1HPYRAZOL- 1-YL) ETHANONE DERIVATIVES

Kumara Prasad S. A.*, Srinivasa U., Subrahmanyam E.V.S., Shabaraya A.R.

Abstract

The synthesis of new series of 2-((1H-indol-4-yl)oxy)-1-(4,5-diphenyl- 1H-pyrazol-1-yl) ethanone was carried out by employing the general scheme developed in our laboratory using appropriate reagents. In the present work substituted Pyrazoles (4a-j) were synthesized by three steps. In the first step synthesis of chalcones by reacting substituted aldehydes with acetophenone yielded chalcones (I) and in second step synthesis of acetohydrazide by successive reactions of esterification and hydrazones with 4-hydroxy indole yielded 2-((1H-indol-4- yl)oxy)acetohydrazide (III). Finally the synthesis of title compound by condensation of (I) and (III) with ethanol in the formation of 2-((1Hindol- 4-yl)oxy)-1-(4,5-diphenyl-1H-pyrazol-1-yl) ethanone. The final compounds were purified by recrystallization from appropriate solvents and the structures were characterized by spectral analysis IR, 1H NMR, MASS spectra. Then the synthesized compounds were screened for the in-vivo anti-tumour activity conducted using the standard methodologies.

Keywords: Chalcone, Acetohydrazide, Pyrazole, Anti-tumour activity.