SYNTHESIS OF NOVEL SUBSTITUTED-BENZO[d]THIAZOLE-2,4-DICARBOXAMIDES HAVING KINASE INHIBITION AND ANTI-PROLIFERATIVE ACTIVITY

Abstract

A series of novel derivatives containing N 4-(4-fluorophenyl)-N 2-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, 1 H NMR, 13 C NMR, 19 F 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.

Synthesis, antimicrobial and anti‐tubercular activity study of N‐(substituted‐benzyl)‐4‐(trifluoromethyl)thiazole‐2‐sulfonamide and 2‐(N‐(substituted‐benzyl)sulfamoyl)thiazole‐4‐carboxylic acid

“…Thiazole nuclei were identified as one of the important class of heterocyclic compounds because of its significant and versatile biological and pharmacological properties. From the available literature, the diversified biological activities of thiazole and in continuation of our research on bioactive heterocyclic compound, as an antimicrobial and anticancer agent [29][30][31][32] we have synthesized a series of N-(substituted-benzyl)-4-(trifluoromethyl)thiazole-2-sulfonamide and 2-(N-(substituted-benzyl)sulfamoyl)thiazole-4-carboxylic acid derivatives (4a-4i and 7a-7i) depicted below in Scheme 1.…”

Thionyl Chloride Induced Convenient Synthesis of Benzamides From 3-Bromo-5-Nitrobenzoic Acid and Amines Under Solvent Free Conditions

“…13 We have been engaged in the development of aromatic compounds as anti-cancer agents and have shown structureactivity relationships with several substituted benzoic acids (containing NO2 and Br group) to which a heterocyclic aromatic amide group containing ring bound, 14 therefore the amidation reactions of 3-bromo-5-nitro benzoic acid was performed in the presence of SOCl2 as promoter in a solvent and catalyst free conditions. 15 In continuation of our work, [16][17][18][19][20][21][22][23][24][25][26][27][28][29][30][31][32][33] we have developed the new protocol synthesis of benzamides from 3-bromo-5nitrobenzoic acid and amines.…”