Development of LM98, a Small‐Molecule TEAD Inhibitor Derived from Flufenamic Acid

ChemMedChem ◽  
2021 ◽  
Author(s):  
Alexandre Gagnon ◽  
Léa Mélin ◽  
Shuay Abdullayev ◽  
Ahmed Fnaiche ◽  
Victoria Vu ◽  
...  
Keyword(s):  
Small Molecule ◽  
Flufenamic Acid

A privileged ternary blend enabling non-fullerene organic photovoltaics with over 14% efficiency

2020 ◽  
Vol 8 (43) ◽  
pp. 15135-15141
Author(s):  
Jing Yan ◽  
Yuan-Qiu-Qiang Yi ◽  
Jianqi Zhang ◽  
Huanran Feng ◽  
Yanfeng Ma ◽  
...  
Keyword(s):  
Small Molecule ◽  
Organic Photovoltaics ◽  
Power Conversion ◽  
Ternary Blend ◽  
Conversion Efficiencies

Two non-fullerene small molecule acceptors, NT-4F and NT-4Cl, were designed and synthesized. Power conversion efficiencies of 11.44% and 14.55% were achieved for NT-4Cl-based binary and ternary devices, respectively.

Development of small-molecule-based probes for the vitamin D receptor

2020 ◽  
Author(s):  
Tania Mutchie ◽  
Alexander Arnold
Keyword(s):  
Vitamin D ◽  
Small Molecule ◽  
Vitamin D Receptor

The small-molecule antibiotics pipeline: 2014–2018

2019 ◽  
Vol 18 (10) ◽  
pp. 739-739 ◽  
Author(s):  
Cara Lepore ◽  
Lynn Silver ◽  
Ursula Theuretzbacher ◽  
Joe Thomas ◽  
David Visi
Keyword(s):  
Small Molecule

Anisotropic forces in small molecule crystals

1985 ◽  
Vol 82 ◽  
pp. 91-97 ◽  
Author(s):  
H. Bonadeo ◽  
E. Burgos
Keyword(s):  
Small Molecule

P157 FBXO3-FBXL2 AXIS MODULATORS AS A NOVEL CLASS OF ORAL SMALL MOLECULE COMPOUNDS FOR THE TREATMENT OF CROHN’S DISEASE

2020 ◽  
Vol 158 (3) ◽  
pp. S9-S10
Author(s):  
Franca Angeli ◽  
Russell Wyborski ◽  
Bill Chen ◽  
Rama Mallampalli ◽  
Michael Lark
Keyword(s):  
Crohn’S Disease ◽  
Crohn's Disease ◽  
Small Molecule

Targeting the p53 tumor suppressor activity in glioblastomas using small molecule MDM2-inhibitor

2011 ◽  
Vol 42 (01) ◽  
Author(s):  
P. Monfared ◽  
T. Viel ◽  
G. Schneider ◽  
Y. Waerzeggers ◽  
S. Rapic ◽  
...  
Keyword(s):  
Tumor Suppressor ◽  
Small Molecule ◽  
Suppressor Activity ◽  
P53 Tumor Suppressor ◽  
Tumor Suppressor Activity ◽  
Mdm2 Inhibitor

Inhibition of the Activities of α2-Plasmin inhibitor (PI) and CI inhibitor (CI-Inh) by the Synthetic Fibrinolytic Agent, 3-Hydroxypropyl Flufenamide (Flu-HPA)

1979 ◽  
Author(s):  
L Miles ◽  
J Burnier ◽  
M Verlander ◽  
M Goodman ◽  
A Kleiss ◽  
...  
Keyword(s):  
Plasminogen Activators ◽  
Inhibitory Effect ◽  
Mechanisms Of Action ◽  
Flufenamic Acid ◽  
Clot Lysis ◽  
Factor Xiia ◽  
Dependent Inhibition ◽  
Normal Human ◽  
Plasmin Inhibitor

Flu-HPA is one of a series of flufenamic acid derivations that enhances plasminogen-dependent clot lysis in vitro. Studies of possible mechanisms of action of Flu-HPA were undertaken. The influence of Flu-HPA on the inhibition of purified plasmin by purified PI was studied. PI activity was assessed by its inhibition of the clevage of the tripeptide S-2251 (H-D-Val-Leu-Lys-pNA) by plasmin. Flu-HPA was dissolved in DMF or in methonol and preincubated with PI before addition of plasmin. At Flu-HPA concentrations greater than 1mM and up to 60mM, the inhibitory activity of PI was totally lost. The inhibitory effect of normal human plasma on plasmin was also completely abolished at concentrations of Flu-HPA between 2.5 and 40mM. The effect of Flu-HPA on the inhibition of purified plasma kallikrein by purified CI-Inh was also studied. CI-Inh activity was measured by its inhibition of cleavage of the tripeptide Bz-Pro-Phe-Arg-pNA by kallikrein. When Flu-HPA, dissolved in DMF or in methonol, was preincubated with CI-Inh, a concentration dependent inhibition of CI-Inh activity was observed. CI-Inh activity was abolished by concentrations of Flu-HPA greater than 1mM. Flu-HPA also inhibited the activity of CI-Inh on purified Factor XIIa. These observations suggest that this flufenamic acid derivative may enhance fibrinolysis not only by inhibiting PI activity but also by decreasing the inactivation of plasminogen activators by CI-Inh.

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