MyJournals Home  

RSS FeedsMolecules, Vol. 24, Pages 3711: New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors (Molecules)


15 october 2019 18:00:45

Molecules, Vol. 24, Pages 3711: New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors (Molecules)

Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a promising therapeutic target in cancer therapy. Combination chemotherapy using Tdp1 inhibitors as a component can potentially improve therapeutic response to many chemotherapeutic regimes. A new set of usnic acid derivatives with hydrazonothiazole pharmacophore moieties were synthesized and evaluated as Tdp1 inhibitors. Most of these compounds were found to be potent inhibitors with IC50 values in the low nanomolar range. The activity of the compounds was verified by binding experiments and supported by molecular modeling. The ability of the most effective inhibitors, used at non-toxic concentrations, to sensitize tumors to the anticancer drug topotecan was also demonstrated. The order of administration of the inhibitor and topotecan on their synergistic effect was studied, suggesting that prior or simultaneous introduction of the inhibitor with topotecan is the most effective. Digg Facebook Google StumbleUpon Twitter
21 viewsCategory: Biochemistry, Chemistry, Molecular Biology
Molecules, Vol. 24, Pages 3713: Essential Oils and Their Natural Active Compounds Presenting Antifungal Properties (Molecules)
Molecules, Vol. 24, Pages 3712: Synthesis and Glycosidase Inhibition of Broussonetine M and Its Analogues (Molecules)
blog comments powered by Disqus
The latest issues of all your favorite science journals on one page


Register | Retrieve


Molecular Biology

Use these buttons to bookmark us: Digg Facebook Google StumbleUpon Twitter

Valid HTML 4.01 Transitional
Copyright © 2008 - 2019 Indigonet Services B.V.. Contact: Tim Hulsen. Read here our privacy notice.
Other websites of Indigonet Services B.V.: Nieuws Vacatures News Tweets Travel Photos Nachrichten Indigonet Finances Leer Mandarijn