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SYNTHESIS, CHARACTERIZATION AND ANTICANCER SCREENING OF NEW SULFONAMIDE-THIAZOLE DERIVED ACETAMIDE COMPOUNDS

Surendra Singh, Alok Pal Jain, Amit Nayak


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    "description": "<p><strong><em>Objective:</em></strong><em> The objective of the paper is synthesis and characterization of sulfonamide-thiazole derived acetamide derivatives and evaluated for t<em>hem for the anticancer potential.</em></em></p>\n\n<p><strong><em>Material and methods:</em></strong><em> The sulfonamide-thiazole derived acetamide derivatives has been prepared by the two step process, in first step, 2-chloro-N-(4-((2,3-dihydro-4H-1,4-oxazin-4-yl)sulfonyl)phenyl) acetamide (<strong>Compound 2</strong>) was synthesized, and in step 2, N-(4-((2,3-dihydro-4H-1,4-oxazin-4-yl)sulfonyl)phenyl)-2-((4-substitutedthiazol-2-yl)amino)acet-amide <strong>(Compound 3)</strong> was synthesized by the reaction of synthesized compound 2 with different 4-substituted thiazol-2-amine to from the final compounds <strong>(compound 3)</strong>. Total eleven compounds have been synthesized and characterized by physicochemical and IR, NMR and MASS spectral analysis. The final compounds (SA-1 to SA-11) have been evaluated for anticancer activity by SRB assay method.</em></p>\n\n<p><strong><em>Result and Discussion:</em></strong><em> The IR spectrum of the compounds (SA-1 to SA-11) has shown the characteristics peak (cm<sup>-1</sup>) of N-H peak at 3331, N-H peak at 3118, aromatic C-H peak at 3039, C=O peak at 1672, C-H aliphatic peak at 2938, C-Cl peak at 850, C-Br peak at 1018, C-F peak at 1102, N-O peak at 1358 and N=O peak at 1562. The 1HNMR spectra depicted the&nbsp;&nbsp; peak of N-H at 10.25 ppm, Thiazole-H peak at 6.25 ppm, CH2 peak at 4.19. The 13CNMR spectrum denotes the peak in ppm of C=O at 170.5, C=N at 162.3 and CH2 at 45.6. Compound SA-1, mass spectrum has shown peak at m/z = 414.02, which matches the chemical formula C<sub>15</sub>H<sub>15</sub>ClN<sub>4</sub>O<sub>4</sub>S<sub>2</sub>. The result data of the synthesized compounds by SRB assay stated the IC50 value of compounds SA-1 (7.7), SA-3 (9.5), SA-4 (14.7) and SA-11 (8.1) has shown better activity as compared to the standard drug paclitaxel (31.1)</em></p>\n\n<p><strong><em>Conclusion</em></strong><em>: The </em><em>Cl, Br, NO<sub>2</sub> and F compounds enhance the activity when it attached to 4-position of the thiazole ring as well as presence of sulfonamide bearing thiazole with addition to electronegative atom enhance the anticancer activity of compounds</em></p>\n\n<p><strong>Keywords: </strong><em>Anticancer activity, thiazole, sulfonamide, SRB assay, acetamide </em></p>", 
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    "title": "SYNTHESIS, CHARACTERIZATION AND ANTICANCER SCREENING OF NEW SULFONAMIDE-THIAZOLE DERIVED ACETAMIDE COMPOUNDS", 
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