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Can I read Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors on EtoBox?
Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors by Mario Sechi; Giuseppe Rizzi; Alessia Bacchi; Mauro Carcelli; Dominga Rogolino; Nicolino Pala; Tino W. Sanchez; Laleh Taheri; Raveendra Dayam; Nouri Neamati is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors about?
Previously, we discovered linomide analogues as novel HIV-1 integrase (IN) inhibitors. Here, to make possible structure-activity relationships, we report on the design and synthesis of a series of substituted dihydroquinoline-3-carboxylic acids. The crystal structure of the representative compound 2c has also been solved. Among the eight new analogues, 2e showed a potency in inhibiting IN strand transfer catalytic activity similar to the reference diketo acid inhibitor L-731,988 (IC(50)=0.9 microM vs. 0.54 microM, for 2e and L-731,988, respectively). Furthermore, none of the compounds showed significant cytotoxicity in two tested cancer cell lines. These compounds represent an interesting prototype of IN inhibitors, potentially involved in a metal chelating mechanism, and further optimization is warranted.
Who reads Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Mario Sechi; Giuseppe Rizzi; Alessia Bacchi; Mauro Carcelli; Dominga Rogolino; Nicolino Pala; Tino W. Sanchez; Laleh Taheri; Raveendra Dayam; Nouri Neamati
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2009
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)