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SYNTHESIS OF NOVEL SUBSTITUTED-BENZO[d]THIAZOLE2,4-DICARBOXAMIDES HAVING KINASE INHIBITION AND ANTI-PROLIFERATIVE ACTIVITY

SYNTHESIS OF NOVEL SUBSTITUTED-BENZO[d]THIAZOLE2,4-DICARBOXAMIDES HAVING KINASE INHIBITION AND ANTI-PROLIFERATIVE ACTIVITY

Author: Dattatraya D. Gaikwad, Chandrakant D. Pawar, Dattatraya N. Pansare, Sadhana L. Chavan, Umakant D. Pawar, Rohini N. Shelke, Santosh L. Chavan,Rajendra P. Pawar, Ashok M. Zine
Abstract

A series of novel derivatives containing N4-(4-fluorophenyl)-N2-substitured-benzo[d]thiazole-2,4-dicarboxamides were synthesized via anefficient, mild and convenient multistep reaction protocol with excellent yields. The structure of the synthesize compounds were confirmedby IR, 1 H NMR, 13C NMR, 19F NMR, mass spectra, elemental analysis and purity was checked by HPLC. All synthesized compounds were screened for anticancer activity against A-549 and Du-145 cancer cell lines by MTT assay. The preliminary bioassay suggests that most of the compounds show anti-proliferation with different degrees. The synthesized compound shows IC50 values in the range of 1.52-17.18 µM in both cell lines. The compounds having electron donating groups had higher anticancer activity compared compounds with electron withdrawing substitutions.

Keywords: Benzo[d]thiazoles; carboxamides; anticancer activity; kinase inhibitors.

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