Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones
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Date
Authors
Olawode, Emmanuel O.
Tandlich, Roman
Prinsloo, Earl
Isaacs, Michelle
Hoppe, Heinrich
Seldon, Ronnett
Warner, Digby F.
Steenkamp, Vanessa
Kaye, Perry T.
Journal Title
Journal ISSN
Volume Title
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.
Description
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.