SYNTHESIS OF NEW DIARYL DERIVATIVES COMPRISING IMIDAZOTHIADIAZOLE MOIETY AS POTENTIAL ANTICANCER AGENTS
Authors: Chirag kumar J. Gohil1, Malleshappa N. Noolvi
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Cancer is a class of diseases characterized by out-of-control cell growth. There are so many types of cancer. In case of Women, Breast Cancer ranks second among cancer deaths in women. Approximately 60% of all breast cancer patients have hormone dependent breast cancer, which contains estrogen receptors and requires estrogen for tumor growth. Aromatase, the enzyme responsible for estrogen biosynthesis, is a particularly attractive target in the treatment of hormone-dependent breast cancer.
In the present study we have reported the synthesis of some novel Diaryl Derivatives comprising 2-Amino Thiadiazole and Imidazothiadiazole moiety. These moieties are of interest because of structural similarity with the Letrozole, which is the potent Aromatase Inhibitor and their diverse biological activities and clinical applications.
We have reported the new series of Letrozole analogues to target Aromatase Enzyme. The reaction was monitored by Thin Layer Chromatography using suitable mobile phase. The Rf values were compared and the Melting Point of the derivatives was determined. It was found that they were different from each others. Further, these derivatives were characterized and confirmed by IR, 1H-NMR, 13C-NMR and Mass Spectral Studies. For Anticancer activity, the selected compounds were submitted to National Cancer Institute (NCI) for in vitro anticancer assay and were evaluated for their anticancer activity. Primary in vitro dose anticancer assay was performed in full NCI 60 Cell panel in accordance with the protocol of the NCI, USA. Compound 1 has a 73.7 % and Compound 4 has a 52.56 % growth Inhibition of Breast Cancer cell lines
Keywords: Anticancer, Breast Cancer, Aromatase Enzyme, Letrozole, Thiadiazole, Imidazothiadiazole, NCI-USA