Synthesis, Antitumor Activity and Structure-activity Studies of Novel Pyridoxine-based Structural Analogs of Saccharumoside-B

In this work, a series of novel pyridine- and pyridoxine-based saccharumoside-B derivatives were synthesized, and their antitumor activity on nine human tumor cell lines (MCF-7, MDA-MB-231, A-498, SNB-19, M-14, NCI-H322M, HCT-115, HCT-116, PC-3) and cytotoxicity on three conditionally normal cell lines (HEK-293, Chang Liver, MSC) were studied in comparison with camptothecin, doxorubicin and saccharumoside-B. Structure-activity patterns, and in particular the contribution to antitumor activity of the peripheral fragments of the studied pharmacophore were analyzed. Our synthetic explorations also allowed us to propose a new efficient approach to the synthesis of saccharumoside B, which was used as a reference drug.