Neamine derivatives bearing a nucleobase, adenine, cytosine, guanine or thymine with a lysine or an arginine as a linker have been synthesized and its potential as the inhibitor for HIV TAR-Tat interaction examined. Among them, modified neamine having an arginine-nucleobase showed a higher inhibition than that of the one having a lysine-nucleobase. The difference of the nucleobase anchor did not characterize inhibition specificity. Also, stereochemistry of the amino acid in the compounds causes no difference in the inhibition for TAR-Tat.
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