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Twelve of the 20 newly synthesized 4- substituted benzopyrones have shown potent antihistaminic H1 activity.
Specifically, 2,4,5,6-tetrasubstituted dihydropyrimidines have shown potent antimycobacterial activity.
The hepatitis C virus (HCV) NS4B inhibitors have shown potent inhibition of HCV replication in vitro.
BCR/ABL activates Ras, and compounds designed to antagonize Ras function called farnesyl transferase inhibitors (FTIs) have shown potent activity in vitro and in animal models of BCR/ABL-induced leukemia.
Considering that high levels of nitric oxide (NO) exert anti-cancer effect and the derivatives of oleanolic acid (OA) have shown potent anti-cancer activity, new O2-vinyl diazeniumdiolate-based NO releasing derivatives (5a l, 11a l) of OA were designed, synthesized, and biologically evaluated in the present study.
In vivo screening concluded that compounds A-4, C-5 and C-6 have shown potent antihyperlipidemic activity by decreasing the plasma level of triglycerides (TG), very low density lipoprotein (VLDL), low density lipoprotein (LDL), followed by increase in level of high density lipoprotein (HDL).
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Six compounds have showed potent antihistamine H1 activity.
RK-33 has shown potent activity in preclinical cancer models.
A second checkpoint immunotherapy called anti-PD1 has shown potent anti-tumor efficacy and has also been approved for use in humans, Vance said.
Although bilirubin has shown potent anti-oxidative and anti-inflammatory functions, its clinical applications have been limited due to its insolubility and short half-life.
We have identified inhibitor 4f which has shown potent enzyme inhibitory (Ki = 13 nM) and cellular (IC50 = 21 nM in neuroblastoma cells) assays.
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