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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.
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| Titolo: | Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors | |
| Autori: | ||
| Data di pubblicazione: | 2009 | |
| Rivista: | ||
| Handle: | http://hdl.handle.net/11388/86732 | |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
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http://hdl.handle.net/11388/86732
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