Synthesis of 4,7,9-Trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide: Evaluation of Cytotoxicity and Inhibition of Protein Kinase C (CaPkc1) | Zendy

Viet Hung Dao | Zendy; Tran Khac Vu | Zendy

Open Access

Synthesis of 4,7,9-Trihydroxy[1]benzofuro[3,2-d]pyrimidine-6-carboxamide: Evaluation of Cytotoxicity and Inhibition of Protein Kinase C (CaPkc1)

Author(s) -

Viet Hung Dao,

Tran Khac Vu

Publication year - 2021

Publication title -

journal of chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.436

H-Index - 50

eISSN - 2090-9063

pISSN - 2090-9071

DOI - 10.1155/2021/7526347

Subject(s) - chemistry , cytotoxicity , candida albicans , pyrimidine , bioassay , carboxamide , kinase , protein kinase a , stereochemistry , mapk/erk pathway , natural product , biochemistry , fungus , in vitro , microbiology and biotechnology , botany , genetics , biology

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.

The content you want is available to Zendy users.

Already have an account? Click here to sign in.

Having issues? You can contact us here

Accelerating Research