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

dc.contributor.authorOlawode, Emmanuel O.
dc.contributor.authorTandlich, Roman
dc.contributor.authorPrinsloo, Earl
dc.contributor.authorIsaacs, Michelle
dc.contributor.authorHoppe, Heinrich
dc.contributor.authorSeldon, Ronnett
dc.contributor.authorWarner, Digby F.
dc.contributor.authorSteenkamp, Vanessa
dc.contributor.authorKaye, Perry T.
dc.date.accessioned2019-08-28T07:57:13Z
dc.date.issued2019-07
dc.description.abstractA 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.en_ZA
dc.description.departmentPharmacologyen_ZA
dc.description.embargo2020-07-01
dc.description.librarianhj2019en_ZA
dc.description.sponsorshipRhodes University for bursary support (to E.O.O.) and the South African Medical Research Council (SAMRC) and Rhodes University for research funding.en_ZA
dc.description.urihttp://www.elsevier.com/ locate/bmclen_ZA
dc.identifier.citationOlawode, 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.en_ZA
dc.identifier.issn0960-894X (print)
dc.identifier.issn1464-3405 (online)
dc.identifier.other10.1016/j.bmcl.2019.05.001
dc.identifier.urihttp://hdl.handle.net/2263/71217
dc.language.isoenen_ZA
dc.publisherElsevieren_ZA
dc.rights© 2019 Elsevier Ltd. All rights reserved. Notice : this is the author’s version of a work that was accepted for publication in Bioorganic and Medicinal Chemistry Letters. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. A definitive version was subsequently published in Bioorganic and Medicinal Chemistry Letters, vol. 29, no. 13, pp. 1572-1575, 2019. doi : 10.1016/j.bmcl.2019.05.001.en_ZA
dc.subject2-Chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinonesen_ZA
dc.subjectAnti-malarialen_ZA
dc.subjectAnti-bacterialen_ZA
dc.subjectAnti-tuberculosisen_ZA
dc.subjectCytotoxicityen_ZA
dc.subjectHeLa cellsen_ZA
dc.titleSynthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinonesen_ZA
dc.typePostprint Articleen_ZA

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