Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones

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Authors

Olawode, Emmanuel O.
Tandlich, Roman
Prinsloo, Earl
Isaacs, Michelle
Hoppe, Heinrich
Seldon, Ronnett
Warner, Digby F.
Steenkamp, Vanessa
Kaye, Perry T.

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Publisher

Elsevier

Abstract

A series of novel, substituted 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones have been prepared and shown to exhibit promising concentration-dependent activity against human SH-SY5Y cells, Plasmodium falciparum, Mycobacterium tuberculosis and P. aeruginosa. Substituent effects on observed bioactivity have been explored; the para-fluorophenyl derivative 3d exhibited activity across the range of the bioassays employed, indicating the potential of the 2-chloro-3-[(4-arylthiazol-2-yl)amino]-1,4-naphthoquinone scaffold in the development of novel, broad spectrum therapeutics.

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Keywords

2-Chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones, Anti-malarial, Anti-bacterial, Anti-tuberculosis, Cytotoxicity, HeLa cells

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Citation

Olawode, E.O., Tandlich, R., Prinsloo, E. et al. 2019, 'Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones', Bioorganic and Medicinal Chemistry Letters, vol. 29, no. 13, pp. 1572-1575.