Next Article in Journal
A Herbal Formula, Atofreellage, Ameliorates Atopic Dermatitis-Like Skin Lesions in an NC/Nga Mouse Model
Previous Article in Journal
Bioactive Compound Content and Cytotoxic Effect on Human Cancer Cells of Fresh and Processed Yellow Tomatoes
Open AccessArticle

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
Molecules 2016, 21(1), 28; https://doi.org/10.3390/molecules21010028
Received: 1 December 2015 / Revised: 19 December 2015 / Accepted: 22 December 2015 / Published: 25 December 2015
(This article belongs to the Section Bioorganic Chemistry)
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
Show Figures

Graphical abstract

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.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop