Structure-activity relationship and molecular bonding parameters from room-temperature multifrequency ESR spectra of antitumor copper(II) complexes

1988 ◽  
Vol 92 (4) ◽  
pp. 992-997 ◽  
Author(s):  
Riccardo Basosi
Keyword(s):  
Room Temperature ◽  
Structure Activity Relationship ◽  
Esr Spectra ◽  
Activity Relationship ◽  
Bonding Parameters ◽  
Structure Activity ◽  
Molecular Bonding

scholarly journals High-Precision, Room Temperature Screening Assay for Inhibitors of Microsomal Prostaglandin E Synthase-1

2012 ◽  
Vol 17 (10) ◽  
pp. 1372-1378 ◽  
Author(s):  
Susanne Andersson ◽  
Mattias Norman ◽  
Rolf Olsson ◽  
Robin Smith ◽  
Gang Liu ◽  
...  
Keyword(s):  
High Precision ◽  
Room Temperature ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Prostaglandin E ◽  
Screening Assay ◽  
Prostaglandin E Synthase ◽  
Structure Activity ◽  
Liquid Transfer ◽  
Microsomal Prostaglandin E Synthase

Microsomal prostaglandin E synthase-1 (mPGES-1) is the major enzyme catalyzing the isomerization of prostaglandin (PG) H2 to PGE2. Here we report the development of a robust and practical automated assay in a 384-well format for room temperature screening of mPGES-1 inhibitors with high precision and low reagent consumption. The assay should enable precise structure-activity relationship development. It uses acetonitrile as solvent for PGH2, FeCl2/citrate as stop reagent, and a short reaction time. Combined with high-precision liquid transfer and extensive mixing after addition of reactants, these properties let the assay reach Z′ > 0.7 and high reproducibility of inhibitor IC50 values. Thorough investigation of the quality of mixing in all liquid transfer steps proved crucial for reaching high-precision performance. Abbreviations: mPGES-1 (microsomal prostaglandin E synthase-1); FRET (fluorescence resonance energy transfer); HTRF (homogeneous time-resolved fluorescence); PGH2 (prostaglandin H2); PGE2 (prostaglandin E2); SAR (structure-activity relationship); COX-2 (cyclooxygenase-2); GSH (glutathione); ALP (automated labware positioner)

Structure-activity relationship of (-) mammea A/BB derivatives against Leishmania amazonensis

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
MA Brenzan ◽  
CV Nakamura ◽  
BPD Filho ◽  
T Ueda-Nakamura ◽  
MCM Young ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Leishmania Amazonensis ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of
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