Synthesis of 4,7,9-Trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide: Evaluation of Cytotoxicity and Inhibition of Protein Kinase C (CaPkc1)
The protein kinase Pkc1 of Candida albicans (CaPkc1), one of the key proteins involved in MAPK pathway, is described as a regulator of cell wall integrity during growth, morphogenesis, and response to cell wall stress. The (–)-cercosporamide is an antifungal natural product isolated from the phytopa...
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| Format: | Article |
| Language: | English |
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Wiley
2021-01-01
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| Series: | Journal of Chemistry |
| Online Access: | http://dx.doi.org/10.1155/2021/7526347 |
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| author | Dao Viet Hung Tran Khac Vu |
| author_facet | Dao Viet Hung Tran Khac Vu |
| author_sort | Dao Viet Hung |
| collection | DOAJ |
| description | The protein kinase Pkc1 of Candida albicans (CaPkc1), one of the key proteins involved in MAPK pathway, is described as a regulator of cell wall integrity during growth, morphogenesis, and response to cell wall stress. The (–)-cercosporamide is an antifungal natural product isolated from the phytopathogen fungus Cercosporidium henningsii. This phytoxin was found to inhibit selectively CaPkc1 and constitutes an interesting model for the design of novel antifungal molecules. In this research, 4,7,9-trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide (13) derived from (–)-cercosporamide was synthesized via a seven-step procedure by well-known reactions and evaluation of cytotoxicity and inhibition of CaPkc1. The bioassay showed CaPkc1 inhibitory activity 87% higher and cytotoxicity 100 times less than the reference, (–)-cercosporamide. |
| format | Article |
| id | doaj-art-caaf39a6b2ff46cea2523de3e764498b |
| institution | Kabale University |
| issn | 2090-9063 2090-9071 |
| language | English |
| publishDate | 2021-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Journal of Chemistry |
| spelling | doaj-art-caaf39a6b2ff46cea2523de3e764498b2025-02-03T01:27:22ZengWileyJournal of Chemistry2090-90632090-90712021-01-01202110.1155/2021/75263477526347Synthesis of 4,7,9-Trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide: Evaluation of Cytotoxicity and Inhibition of Protein Kinase C (CaPkc1)Dao Viet Hung0Tran Khac Vu1Phu Tho College of Medicine and Pharmacy, No. 2201 Hung Vuong, Gia Cam, Viet Tri, Phu Tho, VietnamSchool of Chemical Engineering, Hanoi University of Science and Technology, No. 1 Dai Co Viet, Hai Ba Trung, Hanoi, VietnamThe protein kinase Pkc1 of Candida albicans (CaPkc1), one of the key proteins involved in MAPK pathway, is described as a regulator of cell wall integrity during growth, morphogenesis, and response to cell wall stress. The (–)-cercosporamide is an antifungal natural product isolated from the phytopathogen fungus Cercosporidium henningsii. This phytoxin was found to inhibit selectively CaPkc1 and constitutes an interesting model for the design of novel antifungal molecules. In this research, 4,7,9-trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide (13) derived from (–)-cercosporamide was synthesized via a seven-step procedure by well-known reactions and evaluation of cytotoxicity and inhibition of CaPkc1. The bioassay showed CaPkc1 inhibitory activity 87% higher and cytotoxicity 100 times less than the reference, (–)-cercosporamide.http://dx.doi.org/10.1155/2021/7526347 |
| spellingShingle | Dao Viet Hung Tran Khac Vu Synthesis of 4,7,9-Trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide: Evaluation of Cytotoxicity and Inhibition of Protein Kinase C (CaPkc1) Journal of Chemistry |
| title | Synthesis of 4,7,9-Trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide: Evaluation of Cytotoxicity and Inhibition of Protein Kinase C (CaPkc1) |
| title_full | Synthesis of 4,7,9-Trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide: Evaluation of Cytotoxicity and Inhibition of Protein Kinase C (CaPkc1) |
| title_fullStr | Synthesis of 4,7,9-Trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide: Evaluation of Cytotoxicity and Inhibition of Protein Kinase C (CaPkc1) |
| title_full_unstemmed | Synthesis of 4,7,9-Trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide: Evaluation of Cytotoxicity and Inhibition of Protein Kinase C (CaPkc1) |
| title_short | Synthesis of 4,7,9-Trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide: Evaluation of Cytotoxicity and Inhibition of Protein Kinase C (CaPkc1) |
| title_sort | synthesis of 4 7 9 trihydroxy 1 benzofuro 3 2 d pyrimidine 6 carboxamide evaluation of cytotoxicity and inhibition of protein kinase c capkc1 |
| url | http://dx.doi.org/10.1155/2021/7526347 |
| work_keys_str_mv | AT daoviethung synthesisof479trihydroxy1benzofuro32dpyrimidine6carboxamideevaluationofcytotoxicityandinhibitionofproteinkinaseccapkc1 AT trankhacvu synthesisof479trihydroxy1benzofuro32dpyrimidine6carboxamideevaluationofcytotoxicityandinhibitionofproteinkinaseccapkc1 |