Synthesis, characterization, anti-cancer and anti-bacterial study of isatin conjugated 4-azidopyrazoline derivatives | Abstract

Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

ISSN: 0975-413X
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Synthesis, characterization, anti-cancer and anti-bacterial study of isatin conjugated 4-azidopyrazoline derivatives

Author(s): Reddy Raghunath Babu, Radhika T., Tejaswini B., Madhava Reddy B. and Harinadha Babu V

New derivatives of isatin conjugated 4-azidopyrazolines were synthesized 5(a-e) and characterized by physical and spectral data. From p-aminoacetophenone, 1-(4-azidophenyl)ethanone (1) was prepared by diazotization and subsequent reaction with sodium az ide. Claisen-Schmidt condensation of compound (1) with different aromatic/hetero aldehydes gave chalcones 2(a-e) which were converted into pyrazolines 3(a-e) using hydrazine hydrate and treated with chloroacetyl chloride to give 1-(3-(4-azidophenyl-5-(4-aryl/hetero aryl)-4,5-dihydro-1Hpyrazol- 1-yl)-2-chloroethanones 4(a-e). Condensation of compounds 4(a-e) with isatin gave the final compounds 5(a-e). The synthesized compounds were evaluated for anti-bacterial and in vitro anti-cancer properties. Among the five compounds, 5b&5d showed significant activity against p.aeruginosa with MIC values at 6.25 and 12.5 μg/ml. In MTT assy for cytotoxicity activity, compound 5a showed highest activity against NCI-H23 and MCF-7 cell lines with IC50 values at 1.06 & 3.92 μM/ml, while the other compounds were moderately active with IC50 values >20 μM/ml. In vivo anticancer activity studies against Ehrlich ascites carcinoma (EAC) revealed that compound 5a has highest increase in life span (% ILS) and mean survival time (MST) with 73.47 % and 31.5 ± 0.48 days respectively. A good correlation was observed between the results of in vitro and in vivo anticancer study of the compounds.


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