CINECA IRIS Institutional Research Information System
IRIS è la soluzione IT che facilita la raccolta e la gestione dei dati relativi alle attività e ai prodotti della ricerca. Fornisce a ricercatori, amministratori e valutatori gli strumenti per monitorare i risultati della ricerca, aumentarne la visibilità e allocare in modo efficace le risorse disponibili.
EnglishPreviously, 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 (IC50 = 0.9 lM vs. 0.54 lM, 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.
Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors / MARIO SECHI; GIUSEPPE RIZZI; ALESSIA BACCHI; MAURO CARCELLI; DOMINGA ROGOLINO; NICOLINO PALA; TINO W. SANCHEZ C; LALEH TAHERI; RAVEENDRA DAYAM; NOURI NEAMATI. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 17:(2009), pp. 2925-2935.
Scheda prodotto non validato
Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo
| Titolo: | Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors | |
| Autori: | ||
| Data di pubblicazione: | 2009 | |
| Rivista: | ||
| Citazione: | Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors / MARIO SECHI; GIUSEPPE RIZZI; ALESSIA BACCHI; MAURO CARCELLI; DOMINGA ROGOLINO; NICOLINO PALA; TINO W. SANCHEZ C; LALEH TAHERI; RAVEENDRA DAYAM; NOURI NEAMATI. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 17:(2009), pp. 2925-2935. | |
| Handle: | http://hdl.handle.net/11388/86732 | |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
File in questo prodotto:
http://hdl.handle.net/11388/86732
Copyright © 2022