Thymoquinone displayed the highest potency in our assay.
The results showed that most of the newly synthesized derivatives exhibited higher activity than ligustrazine, of which, compound VA-06 displayed the highest potency with EC50 values of 17.39 ± 1.34 μM.
Prominently, compound 4l displayed the best potency and selectivity toward A549 with an IC50 value of 20 μM, nearly comparable to the positive control cisplatin (IC50 = 10 μM) and even superior to the lead compound 22 (IC50 = 130 μM).
Among them, compound 8e displayed the strongest potency against fXa with the IC50 value of 21 nM and highly selectivity versus thrombin (IC50 = 67 μM) and excellent in vitro antithrombotic activity with its 2 × PT value of 1.2 μM and 2 × aPTT value of 0.6 μM.
At high, non-physiological, concentrations all strains displayed the same potency in whole blood.
Of the three remaining drugs, simvastatin displayed the greatest potency, followed by lovastatin and finally mevastatin (Table 1).
Of the four molecules tested in the radial inhibition assay, β defensin-2 displayed the highest potency and was effective against all pathogens tested.
In particular, it was the C5 and C6 compounds with conjugated double-bond systems that displayed the highest potency at bFFA2.
Celecoxib is unique among the coxibs and traditional NSAIDs, because this particular drug displays the greatest potency to induce apoptotic cell death.
Among the thiol-conjugated metabolites, cysteine-conjugated 6S (M2) is one of the major metabolites of 6S and displays the highest potency against the growth of human colon and lung cancer cells, which is comparable to that of 6S.
Acyl-CoA synthetase activity in the membrane fraction of Raji cells was also inhibited by triacsins, which display the same hierarchy of inhibitory potency as that against the enzyme from other sources, that is, the inhibitory potency of triacsin C (71) is greater than that triacsin A, followed by that of triacsin D (72), and is greater than or equal to that of triacsin B [85].
