dc.contributor.author |
Kishore, Navneet
|
|
dc.contributor.author |
Binneman, Brigitte
|
|
dc.contributor.author |
Mahapatra, Anita
|
|
dc.contributor.author |
Van de Venter, Maryna
|
|
dc.contributor.author |
Du Plessis-Stoman, Debbie
|
|
dc.contributor.author |
Boukes, Gerhardt
|
|
dc.contributor.author |
Houghton, Peter James
|
|
dc.contributor.author |
Meyer, Jacobus Johannes Marion
|
|
dc.contributor.author |
Lall, Namrita
|
|
dc.date.accessioned |
2015-07-13T05:53:01Z |
|
dc.date.available |
2015-07-13T05:53:01Z |
|
dc.date.issued |
2014-09 |
|
dc.description.abstract |
In an effort to establish new candidates with enhanced anticancer activity of 5-hydroxy-7-methyl-1,4-
naphthoquinone scaffold (7-methyljuglone) previously isolated from the root extract of Euclea natalensis,
a series of 7-methyljuglone derivatives have been synthesized and assessed for cytotoxicity on selected
human cancer lines. These compounds were screened in vitro for anticancer activity on MCF-7, HeLa, SNO
and DU145 human cancer cell lines by MTT assay. Most of them exhibited significant toxicity on cancer
cell lines with lower IC50 values. The most potent derivative (19) exhibited the toxicity on HeLa and
DU145 cell lines with IC50 value of 5.3 and 6.8 lM followed by compound (5) with IC50 value of 10.1
and 9.3 lM, respectively. Structure–activity relationship reveals that the fluoro substituents at position
C-8 while hydroxyl substituents at C-2 and C-5 positions played an important role in toxicity. |
en_ZA |
dc.description.embargo |
2015-09-30 |
en_ZA |
dc.description.librarian |
hb2015 |
en_ZA |
dc.description.sponsorship |
University of Pretoria, South Africa and National Research Foundation (NRF), South Africa. |
en_ZA |
dc.description.uri |
http://www.elsevier.com/locate/bmc |
en_ZA |
dc.identifier.citation |
Kishore, N, Binneman, B, Mahapatra, A, Van De Venter, M, Du Plessis-Stoman, D, Boukes, G, Houghton, P, Meyer, JJM & Lall, N 2014, 'Cytotoxicity of synthesized 1,4-naphthoquinone analogues on selected human cancer cell lines', Bioorganic and Medicinal Chemistry, vol. 22, no. 17, pp. 5013-5019. |
en_ZA |
dc.identifier.issn |
0968-0896 (print) |
|
dc.identifier.issn |
1464-3391 (online) |
|
dc.identifier.other |
10.1016/j.bmc.2014.06.013 |
|
dc.identifier.uri |
http://hdl.handle.net/2263/47952 |
|
dc.language.iso |
en |
en_ZA |
dc.publisher |
Elsevier |
en_ZA |
dc.rights |
© 2014 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. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Bioorganic and Medicinal Chemistry Letters, vol.22, no. 17, pp. 5013-5019, 2014. doi :10.1016/j.bmc.2014.06.013. |
en_ZA |
dc.subject |
Euclea natalensis |
en_ZA |
dc.subject |
7-Methyljuglone derivatives |
en_ZA |
dc.subject |
Cytotoxicity |
en_ZA |
dc.subject |
Cell cycle analysis |
en_ZA |
dc.subject |
Cell apoptosis |
en_ZA |
dc.title |
Cytotoxicity of synthesized 1,4-naphthoquinone analogues on selected human cancer cell lines |
en_ZA |
dc.type |
Postprint Article |
en_ZA |