[图书][B] Synthesis and Structure-Activity Relationship Studies of 3-(N-Butylethanimidoyl)-4-hydroxy-2H-chromen-2-one (BHC) Analogues for Myosin II Inhibition

J Brawley - 2022 - search.proquest.com
The objective of current treatments for various myopathies is to interrupt the signal from the
brain to the affected muscle group, providing relief. To prevent unwanted side effects and …

Synthesis and evaluation of 4-hydroxycoumarin imines as inhibitors of class II myosins

J Brawley, E Etter, D Heredia, A Intasiri… - Journal of medicinal …, 2020 - ACS Publications
Inhibitors of muscle myosin ATPases are needed to treat conditions that could be improved
by promoting muscle relaxation. The lead compound for this study ((3-(N-butylethanimidoyl) …

Insights into the myosin II inhibitory potency of A-ring-modified (S)-blebbistatin analogs

S Verhasselt, CV Stevens, ME Bracke… - Bioorganic & medicinal …, 2017 - Elsevier
Myosin II is an interesting target for therapeutic intervention, as it is involved in a large
number of motility-based diseases.(S)-Blebbistatin is a known micromolar inhibitor of this …

[PDF][PDF] Development of novel blebbistatin derivatives in the quest for improved non-muscle myosin II inhibitors

S Verhasselt - 2017 - biblio.ugent.be
As mentioned in the Literature overview,(S)-blebbistatin (S)-4 has two main disadvantages
which limit its application as a research tool in cell biology:(i) low water solubility (and …

Medicinal Chemistry and Use of Myosin II Inhibitor (S)-Blebbistatin and Its Derivatives

BI Roman, S Verhasselt… - Journal of medicinal …, 2018 - ACS Publications
(S)-Blebbistatin, a chiral tetrahydropyrroloquinolinone, is a widely used and well-
characterized ATPase inhibitor selective for myosin II. The central role of myosin II in many …

Synthesis of C-ring-modified blebbistatin derivatives and evaluation of their myosin II ATPase inhibitory potency

BI Roman, S Verhasselt, CW Mangodt… - Bioorganic & medicinal …, 2018 - Elsevier
Abstract (S)-Blebbistatin is a micromolar myosin II ATPase inhibitor that is extensively used
in research. In search of analogs with improved potency, we have synthesized for the first …

Skeletal, smooth and cardiac muscle myosin 2 are less sensitive for the chiral hydroxyl moiety of blebbistatin than that of non-muscle myosin 2 isoforms

AÁ Rauscher, M Gyimesi, A Malnasi-Csizmadia - Biophysical Journal, 2022 - cell.com
Myosin 2 inhibition and the traditional myosin 2 inhibitor, blebbistatin have recently become
the focus of interest of drug discovery and drug development. The effect of several …

Discovery of (S)-3′-hydroxyblebbistatin and (S)-3′-aminoblebbistatin: polar myosin II inhibitors with superior research tool properties

S Verhasselt, BI Roman, O De Wever… - Organic & …, 2017 - pubs.rsc.org
In search of myosin II inhibitors with superior research tool properties, a chemical
optimization campaign of the blebbistatin scaffold was conducted in this paper.(S) …

Improved inhibitory and ADMET properties of blebbistatin derivatives indicate that blebbistatin scaffold is ideal for drug development targeting myosin-2

M Gyimesi, AÁ Rauscher, SK Suthar, KÁ Hamow… - … of Pharmacology and …, 2021 - ASPET
Blebbistatin, para-nitroblebbistatin (NBleb) and para-aminoblebbistatin (AmBleb) are highly
useful tool compounds as they selectively inhibit the ATPase activity of myosin-2 family …

Mechanistic and structural basis for tuning of myosin activity

L Canon - 2022 - cnrs.hal.science
The eukaryotic cell nanomotors are able to perform many complex mechanical tasks,
necessary for tension generation in precise cellular locations such as transport or …