Facile synthesis of antimalarial 1,2-disubstituted 4-quinolones from 1,3-bisaryl-monothio-1,3-diketones

Vinayaka, A. C. and Sadashiva, M. P. and Wu, X. and Biryukov, S. S. and Stoute, J. A. and Rangappa, K. S. and Channe Gowda, D. (2014) Facile synthesis of antimalarial 1,2-disubstituted 4-quinolones from 1,3-bisaryl-monothio-1,3-diketones. Organic and Biomolecular Chemistry, 12 (42). pp. 8555-8561. ISSN 1477-0520

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Official URL: http://doi.org/10.1039/c4ob01455c


A new strategy was developed to synthesize 1,2-disubstituted 4-quinolones in good yield starting from 1,3-bisaryl-monothio-1,3-diketone substrates. The synthesized compounds were evaluated for antimalarial activity using Plasmodium falciparum strains. All compounds, except for two, showed good activity. Of these, seven compounds exhibited an excellent antimalarial activity (IC50, <2 μM). More importantly, all seven compounds were equally effective in inhibiting the growth of both chloroquine-sensitive and chloroquine-resistant strains. The cytotoxicity assessment using carcinoma and non-carcinoma human cell lines revealed that almost all synthesized compounds were minimally cytotoxic (IC50, >50 μM). This journal is

Item Type: Article
Uncontrolled Keywords: human, Cell Line, chemistry, Humans, synthesis, Tumor, tumor cell line, antimalarial agent, drug effects, Malaria, Plasmodium falciparum, 4 quinolone derivative, 4-Quinolones, Antimalarials, cell line, Facile synthesis, Falciparum
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: Arshiya Kousar Library Assistant
Date Deposited: 31 Aug 2019 10:12
Last Modified: 31 Aug 2019 10:12
URI: http://eprints.uni-mysore.ac.in/id/eprint/4283

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