Novel polycarbo-substituted alkyl (thieno[3,2-c]quinoline)-2- carboxylates : synthesis and cytotoxicity studies

Show simple item record Mphahlele, Malose Jack Maluleka, Marole Maria Makhafola, Tshepiso Jan Mabeta, Peaceful Lucy 2015-01-27T12:03:51Z 2015-01-27T12:03:51Z 2014-11
dc.description.abstract Direct one-pot base-promoted conjugate addition–elimination of 6,8-dibromo-4- chloroquinoline-3-carbaldehyde with methyl mercaptoacetate and subsequent cyclization afforded methyl [(6,8-dibromothieno[3,2-c]quinoline)]-2-carboxylate. The latter undergoes Suzuki-Miyaura cross-coupling with arylboronic acids to yield exclusively the corresponding alkyl [(6,8-diarylthieno[3,2-c]quinoline)]-2-carboxylates,. The cytotoxicity of the prepared compounds was evaluated against the human breast cancer cell line MCF-7 using the MTT assay. The effects of compounds 2, 3c and 4d on cell kinetics were further determined using the xCELLigence Real Time Cell Analysis (RTCA) system. In both the MTT assay and Real Time Cell Analysis, the compounds inhibited cancer cell growth in a dose- and time-dependent manner. Furthermore, on the basis of the calculated LC50 values, the compounds compared favourably with nocodazole, a well-established anticancer drug. en_ZA
dc.description.librarian hb2015 en_ZA
dc.description.sponsorship University of South Africa and the National Research Foundation in South Africa. en_ZA
dc.description.uri en_ZA
dc.identifier.citation Mphahlele, MJ, Maluleka, MM, Makhafola, TJ & Mabeta, PL 2014, 'Novel polycarbo-substituted alkyl (thieno[3,2-c]quinoline)-2- carboxylates : synthesis and cytotoxicity studies', Molecules, vol. 19, no. 11, pp. 18527-8542. en_ZA
dc.identifier.issn 1420-3049 (print)
dc.identifier.issn 1420-3049 (online)
dc.identifier.other 10.3390/molecules191118527
dc.identifier.other 12791859400
dc.identifier.other G-9725-2014
dc.language.iso en en_ZA
dc.publisher MDPI en_ZA
dc.rights © 2014 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license ( en_ZA
dc.subject 6,8-dibromo-4-chloroquinoline-3-carbaldehyde en_ZA
dc.subject Suzuki-miyaura cross-coupling en_ZA
dc.subject Alkyl thieno[3,2-c]quinoline-2-carboxylates en_ZA
dc.subject MCF-7 cell line en_ZA
dc.subject Cytotoxicity en_ZA
dc.title Novel polycarbo-substituted alkyl (thieno[3,2-c]quinoline)-2- carboxylates : synthesis and cytotoxicity studies en_ZA
dc.type Article en_ZA

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