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Abstract

SYNTHESIS OF NOVEL THIAZOLYL-PYRAZOLE DERIVATIVES AS EGFR INHIBITORS

*Ghodgaonkar Sunayana and Bhandari Shashikant

ABSTRACT

In our last article we performed molecular modelling studies on a set of 42 molecules of thiazolyl-pyrazole derivatives. We deigned new chemical entities with Combilib:Vlife MDS software. We further performed docking studies to study the interaction of the designed new chemical entities with epidermal growth receptor factor (EGFR). We predicted 5 best compounds which fitted into the pocket of EGFR and may exhibit anticancer activity. In this article we present the synthesis and spectral evaluation of the synthesized compounds. We have further performed biological screening by Microculture Tetrazolium Test (MTT) assay for evaluation against breast cancer and lung cancer cell lines. Compounds KS- 1, KS-3, KS-5, KS-6, KS-11 were found to have percentage inhibition of 82.12%, 22.66%, 69.57%, 8.09%,48.02%, at a concentration of 60μg/ml and 64.03%, 21.82%, 38.83%, 3.23%, 41.37%, at a concentration of 80μg/ml as against standard drug 5-flurouracil 1.94%, This indicated that these compounds exhibited excellent activity against cell lines in vitro.

Keywords: Synthesis, IR, NMR.


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