Sechi, Mario and Rizzi, Giuseppe and Bacchi, Alessia and Carcelli, Mauro and Rogolino, Dominga and Pala, Nicolino and Sanchez, Tino and Taheri, Laleh and Dayam, Raveendra and Neamati, Nouri (2009) Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors. Bioorganic & Medicinal Chemistry, Vol. 17 (7), p. 2925-2935. ISSN 0968-0896. Article.
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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 (IC50 = 0.9 µM vs. 0.54 µM, 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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