1. In silico, in vitro, and pharmacokinetic evaluation of the synthesized SANs. A, docking for sunitinib and SAN1–5 with estimated inhibition constants (Ki in nmol/L).
In silico, in vitro, and pharmacokinetic evaluation of the synthesized SANs. A, docking for sunitinib and SAN1–5 with estimated inhibition constants (Ki in nmol/L). Molecular model of the VEGFR-2 complex with SAN1. B, summary of in vitro kinase activity in multiple RTKs in the presence of sunitinib or SANs 1–5, (±SD). C, cell-based autophosphorylation assay for PDGFR-β and VEGFR-2 for sunitinib or SANs 1–5, (±SD). D, MTT cytotoxicity assay in a panel of cell lines, (±SD). E, pharmacokinetic evaluation of the most potent SANs versus sunitinib in mice. N.D., not determined; N.A., not active.
Orestis Argyros et al. Cancer Res 2016;76:
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