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Molecules 2016, 21(1), 28; doi:10.3390/molecules21010028

Synthesis, Biological Evaluation and Molecular Docking Studies of 6-Aryl-2-Styrylquinazolin-4(3H)-Ones

1
Department of Chemistry, College of Science, Engineering and Technology, University of South Africa, P. O. Box 392, Pretoria 0003, South Africa
2
Department of Life and Consumer Sciences, College of Agriculture and Environmental Sciences, University of South Africa, Private Bag X06, Florida 1710, South Africa
3
Institute for Research in Molecular Medicine (INFORMM), Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia
4
Computational Chemistry Group, Department of Chemistry, Faculty of Science, University of Mauritius, Réduit 80837, Mauritius
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 1 December 2015 / Revised: 19 December 2015 / Accepted: 22 December 2015 / Published: 25 December 2015
(This article belongs to the Section Bioorganic Chemistry)
View Full-Text   |   Download PDF [2340 KB, uploaded 25 December 2015]   |  

Abstract

Suzuki-Miyaura cross-coupling of 6-bromo-2-styrylquinazolin-4(3H)-ones with arylboronic acids afforded a series of novel 6-aryl-2-styrylquinazolin-4(3H)-ones. These compounds were evaluated for potential anticancer properties against the human renal (TK-10), melanoma (UACC-62) and breast cancer (MCF-7) cell lines. Their antimicrobial properties were also evaluated against six Gram-positive and four Gram-negative bacteria, as well as two strains of fungi. Molecular docking studies (in silico) were conducted on compounds 5a, b, d and 6a, b, df to recognize the hypothetical binding motif of the title compounds within the active site of the dihydrofolate reductase and thymidylate synthase enzymes. View Full-Text
Keywords: 6-bromo-2-styrylquinazolin-4(3H)-ones; Suzuki-Miyaura cross-coupling; 6-aryl-2-styrylquinazolin-4(3H)-ones; in vitro cytotoxicity; antimicrobial activity; docking studies 6-bromo-2-styrylquinazolin-4(3H)-ones; Suzuki-Miyaura cross-coupling; 6-aryl-2-styrylquinazolin-4(3H)-ones; in vitro cytotoxicity; antimicrobial activity; docking studies
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Agbo, E.N.; Makhafola, T.J.; Choong, Y.S.; Mphahlele, M.J.; Ramasami, P. Synthesis, Biological Evaluation and Molecular Docking Studies of 6-Aryl-2-Styrylquinazolin-4(3H)-Ones. Molecules 2016, 21, 28.

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