Mphahlele, Malose JackMaluleka, Marole MariaMakhafola, Tshepiso JanMabeta, Peaceful Lucy2015-01-272015-01-272014-11Mphahlele, 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. 18527-8542.1420-3049 (print)1420-3049 (online)10.3390/molecules19111852712791859400G-9725-2014http://hdl.handle.net/2263/43445Direct 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© 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 (http://creativecommons.org/licenses/by/4.0/).6,8-dibromo-4-chloroquinoline-3-carbaldehydeSuzuki-miyaura cross-couplingAlkyl thieno[3,2-c]quinoline-2-carboxylatesMCF-7 cell lineCytotoxicityArticle