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. Author manuscript; available in PMC: 2018 Jun 15.
Published in final edited form as: Bioorg Med Chem. 2017 Apr 8;25(12):3223–3234. doi: 10.1016/j.bmc.2017.04.008

Table 2.

Summary of biological evaluation of the Dimer-IDHPs (4) and relevant controls.

Structure R n PDSP # VGCC (IC50, nM) mGluR5 (nM) MDR-1 (% vs. Cyclosporin)b MDR-1 (IC50, nM)
1a H 0 21618 13.9a ND 48.9 ND
1b o-Br 0 27215 909 1524 − 12 >10,000
1c m-Br 0 27216 208 >10,000 101.9 510
1d p-Br 0 27217 36 >10,000 58.4 3096
4a H 5 27218 >10,000 >10,000 20.4 >10,000
4b o-Br 5 27219 >10,000 4858 17.7 2862
4c m-Br 5 27220 3766 8638 150.8 1296
4d p-Br 5 27221 2706 193 172.6 1394
4e p-Br 3 27222 516 546 11.6 3231
4f p-Br 2 27223 603 933 41.9 1449
5 p-Br 0 27224 127 1972 107.6 1643
6 H 0 27225 >10,000 >10,000 36.9 >10,000
a

Ref. 31.

b

One dose inhibition compared to cyclosporin (150 nM) in the PDSP fluorescence assay (vide infra). These one dose percent inhibition values represent the assay reported previously in Ref. 11.