Research Article |
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SYNTHESIS OF NOVEL SUBSTITUTED-BENZO[d]THIAZOLE- 2,4-DICARBOXAMIDES HAVING KINASE INHIBITION AND ANTI-PROLIFERATIVE ACTIVITYDattatraya 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 an
efficient, mild and convenient multistep reaction protocol with excellent yields. The structure of the synthesize compounds were confirmed
by IR, 1H 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.
Key words: Benzo[d]thiazoles; carboxamides; anticancer activity; kinase inhibitors.
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