Synthesis, Biological Evaluation and Molecular Docking Studies of 6-Aryl-2-Styrylquinazolin-4(3H)-Ones
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...
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MDPI AG
2015-12-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/21/1/28 |
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doaj-bfbbd0e3e90144d388e030328caf65572020-11-24T23:14:23ZengMDPI AGMolecules1420-30492015-12-012112810.3390/molecules21010028molecules21010028Synthesis, Biological Evaluation and Molecular Docking Studies of 6-Aryl-2-Styrylquinazolin-4(3H)-OnesEmmanuel Ndubuisi Agbo0Tshepiso Jan Makhafola1Yee Siew Choong2Malose Jack Mphahlele3Ponnadurai Ramasami4Department of Chemistry, College of Science, Engineering and Technology, University of South Africa, P. O. Box 392, Pretoria 0003, South AfricaDepartment of Life and Consumer Sciences, College of Agriculture and Environmental Sciences, University of South Africa, Private Bag X06, Florida 1710, South AfricaInstitute for Research in Molecular Medicine (INFORMM), Universiti Sains Malaysia, 11800 Minden, Penang, MalaysiaDepartment of Chemistry, College of Science, Engineering and Technology, University of South Africa, P. O. Box 392, Pretoria 0003, South AfricaComputational Chemistry Group, Department of Chemistry, Faculty of Science, University of Mauritius, Réduit 80837, MauritiusSuzuki-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, d–f to recognize the hypothetical binding motif of the title compounds within the active site of the dihydrofolate reductase and thymidylate synthase enzymes.http://www.mdpi.com/1420-3049/21/1/286-bromo-2-styrylquinazolin-4(3H)-onesSuzuki-Miyaura cross-coupling6-aryl-2-styrylquinazolin-4(3H)-onesin vitro cytotoxicityantimicrobial activitydocking studies |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Emmanuel Ndubuisi Agbo Tshepiso Jan Makhafola Yee Siew Choong Malose Jack Mphahlele Ponnadurai Ramasami |
| spellingShingle |
Emmanuel Ndubuisi Agbo Tshepiso Jan Makhafola Yee Siew Choong Malose Jack Mphahlele Ponnadurai Ramasami Synthesis, Biological Evaluation and Molecular Docking Studies of 6-Aryl-2-Styrylquinazolin-4(3H)-Ones Molecules 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 |
| author_facet |
Emmanuel Ndubuisi Agbo Tshepiso Jan Makhafola Yee Siew Choong Malose Jack Mphahlele Ponnadurai Ramasami |
| author_sort |
Emmanuel Ndubuisi Agbo |
| title |
Synthesis, Biological Evaluation and Molecular Docking Studies of 6-Aryl-2-Styrylquinazolin-4(3H)-Ones |
| title_short |
Synthesis, Biological Evaluation and Molecular Docking Studies of 6-Aryl-2-Styrylquinazolin-4(3H)-Ones |
| title_full |
Synthesis, Biological Evaluation and Molecular Docking Studies of 6-Aryl-2-Styrylquinazolin-4(3H)-Ones |
| title_fullStr |
Synthesis, Biological Evaluation and Molecular Docking Studies of 6-Aryl-2-Styrylquinazolin-4(3H)-Ones |
| title_full_unstemmed |
Synthesis, Biological Evaluation and Molecular Docking Studies of 6-Aryl-2-Styrylquinazolin-4(3H)-Ones |
| title_sort |
synthesis, biological evaluation and molecular docking studies of 6-aryl-2-styrylquinazolin-4(3h)-ones |
| publisher |
MDPI AG |
| series |
Molecules |
| issn |
1420-3049 |
| publishDate |
2015-12-01 |
| description |
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, d–f to recognize the hypothetical binding motif of the title compounds within the active site of the dihydrofolate reductase and thymidylate synthase enzymes. |
| topic |
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 |
| url |
http://www.mdpi.com/1420-3049/21/1/28 |
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