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INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH

A Step Towards Excellence
Published by : Advanced Scientific Research
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0975-2366
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IJPR 9[3] July - September 2017 Special Issue

July - September 9[3] 2017

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Design, Synthesis And Biological Evaluation Of Some Azole Derivatives

Author: SWEETI ASHOK SHEWALE, P.J.SHIROTE, NEETA VASANT WADD
Abstract: Isoxazole have played a crucial role in the history of heterocyclic chemistry and has been used extensively in generation of model pharmacophores and synthons in the field of organic chemistry. Owing to their versatile chemotherapeutic importance, significant research efforts focused these nuclei. Further need of the invention is to quantify or develop efficient and yield oriented process for the preparation of isoxazole derivatives. A series of five different substituted chalcones synthesized by Claisen-Schmidt condensation of 2-hydroxy-3-bromo-4-nitro-5-methyl acetophenone with different substituted aromatic aldehydes. Isoxazoles have been prepared from chalcones by treating with hydroxylamine hydrochloride. The structure of isoxazoles has been characterized by spectral analysis. In vitro study of cytotoxicity of synthesized derivatives is done using two types of Human cell line of prostate cancer and skin cancer by using MTT assay method. The adopted scheme resulted in good yield of isoxazole derivatives. Potent cytotoxic activity was observed with the derivatives SS2, SS5, SS6 on PC3 cell line and on A431 cell line potent cytotoxic activity was shown by SS1, SS4, SS6. Potent cytotoxic activity was observed due to the presence of electron withdrawing groups like NO2.
Keyword: Azole derivatives, Synthesis, Biological evaluation.
DOI: https://doi.org/10.31838/ijpr/2020.12.04.708
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