Add time:10/01/2019 Source:sciencedirect.com
A computer-generated molecular superposition of the key pharmacophores in 3-O-tetradecanoyl-2-deoxy-L-ribonolactone (1) and phorbol-12-myristate-13-acetate (PMA) indicated that the corresponding one carbon homologue, 2,5-dideoxy-3-O-tetradecanoyl-D-galactono-1,4-lactone (2) would have an improved fit to PMA. Compound 2 was synthesized, and, consistent with the model's prediction, demonstrated superior binding affinity for PK-C relative to 1.
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