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Synthesis, Anticancer and Antimicrobial Screening of New Naphthalenyl-Thiazole and Quinolinyl-Thiazole

POLYCYCLIC AROMATIC COMPOUNDS(2022)

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Abstract
A new series of 4-aryl-2-(naphthalen-1-yl)thiazole (7a-b), 4-aryl/pyridyl-2-(2-substituted quinolin-4-yl)thiazole (13a-o) and 4-(pyridin-4-yl)-2-(quinolin-4-yl)thiazole (15) have been synthesized. The newly synthesized compounds were evaluated for anticancer activity against breast cell lines MDA-MB-231 and MCF-7. Among the derivatives compounds 7a, 7 b and 13e showed good activity against the MCF-7 cell line, compounds 13 m, 13o and 15 showed good activity against MDA-MB-231 cell line. The new analogs were also screened to evaluate their in vitro antimicrobial potential against Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388), Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178), Aspergillus niger (ATCC 504), and Candida albicans (NCIM 3100). Amongst the naphthalenyl-thiazole and quinolinyl-thiazole derivatives, ten compounds 7a, 7 b, 13a, 13 b, 13c, 13d, 13e, 13f, 13 h and 15 showed good activity against P. mirabilis. The structure-activity relationship study revealed that naphthalene, quinoline, and 2-phenyl quinoline tethered thiazole showed good activity against P. mirabilis. These compounds could assist in the development of lead compounds for the treatment of cancer and microbial infections.
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Key words
Quinoline, thiazole, anticancer activity, antimicrobial activity
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