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. 2013 Oct 9;14(12):1272–1289. doi: 10.1111/tra.12119

Table 1. Dyngo compound 4a inhibits dynamin I and CME.

Name Structure Formula weight DynI IC50 (μM) with T‐80 DynI IC50 (μM) without T‐80 CME IC50 (μM)
Library 1
Dynasore graphic file with name tra-14-1272-t1a.jpg C18H14N2O4, 322.31 479 ± 49 (n = 3) 12.4 ± 1.5 (n = 5) 34.7 ± 5.1 (n = 9)
4a graphic file with name tra-14-1272-t1b.jpg C18H14N2O5, 338.31 2.7 ± 0.7 (n = 3) 0.38 ± 0.05 (n = 5) 5.7 ± 1.0 (n = 7)
6a graphic file with name tra-14-1272-t1c.jpg C18H14N2O4, 322.31 5.5 ± 0.2 (n = 3) 3.2 ± 0.3 (n = 3) 5.8 ± 0.8 (n = 5)
1a graphic file with name tra-14-1272-t1d.jpg C18H14N2O4, 322.31 37.4 ±0.9 (n = 3) 4.4 ± 1.0 (n = 3) Not active (n = 3)
5a graphic file with name tra-14-1272-t1e.jpg C18H14N2O5, 338.31 102 ±14 (n = 2) 1.5 ± 0.04 (n = 2) 6.2 ± 2 (n = 2)
2a graphic file with name tra-14-1272-t1f.jpg C19H16N2O5, 352.34 Not active (n = 3) 3.3 ± 1.0 (n = 4) 9.6 ± 0.4 (n = 2)
3a graphic file with name tra-14-1272-t1g.jpg C18H14N2O5, 338.31 Not active (n = 2) 1.5 ± 0.3 (n = 2) 9.8 ± 1.5 (n = 2)
8a graphic file with name tra-14-1272-t1h.jpg C18H14N2O4, 322.31 Not active (n = 2) 47.0 ± 0.5 (n = 2) 179 ± 20 (n = 3)
Library 2
10a graphic file with name tra-14-1272-t1i.jpg C20H17N3O3, 347.37 Not active (n = 3) 39.5 ± 4.5 (n = 2) Not active (n = 2)
11a graphic file with name tra-14-1272-t1j.jpg C21H17N3O2, 343.38 58.9 ±1.4 (n = 2) 44.2 ±19.4 (n = 2) 63.4 ±4.4 (n = 2)
12a graphic file with name tra-14-1272-t1k.jpg C20H14N4O2, 342.35 >100 (n = 2) 24.6 ±4.1 (n = 2) Not active (n = 2)
13a graphic file with name tra-14-1272-t1l.jpg C18H12N4O3, 332.31 30.6 ±5.0 (n = 6) 17.6 ± 3.5 (n = 2) Not active (n = 3)
14a graphic file with name tra-14-1272-t1m.jpg C18H12N4O2S, 348.38 4.8 ±0.5 (n = 4) 11.6 ± 1.6 (n = 2) Not active (n = 4)

A series of dynasore analogs (Dyngo compounds) were synthesized with substitutions in the (3,4‐dihydroxybenzylidene)‐hydrazide. Illustrated is the structure of each compound, its chemical formula, formula weight and IC50 for inhibition of native sheep brain dynamin I GTPase activity stimulated by PS liposomes, either in the presence or absence of Tween‐80 (T‐80) in GTPase assay. The last column shows the CME IC50 for inhibition of Tfn‐A594 uptake in U2OS cells after a 30‐min preincubation with each compound. All compounds were tested at multiple concentrations in 1% DMSO (in CME assay) and 3% (in GTPase assay) up to at least 1 mM concentration. Results are mean ± SEM, for n = 2–9 independent experiments.