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. Author manuscript; available in PMC: 2020 Oct 1.
Published in final edited form as: Bioorg Med Chem Lett. 2019 Aug 20;29(19):126633. doi: 10.1016/j.bmcl.2019.126633

Table 1.

Summary of the bioassay results of the novel ω-OH-triazole bisphosphonates.

Compound GGDPS IC50 (μM) FDPS IC50 (μM) Fold-selectivity for GGDPS compared to FDPS Cellular LEC1 (μM)
15 11.6 + 2.6 91.2 + 25.0 8 10
25 0.67 + 0.30 81.4 + 23.5 121 0.25
1

Cellular LEC (lowest effective concentration) is defined as the lowest concentration for which an unmodified Rap1a band is visible in the immunoblot and a statistically significant increase in intracellular lambda light chain is observed in the ELISA.