Selective inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from an oxicam template

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 5, 2010, Pages 1604-1609

  Wang, Jane ^a   Limburg, David ^a   Carter, Jeff ^b   Mbalaviele, Gabriel ^a   Gierse, James ^a   Vazquez, Michael ^a  

^a PFIZER INC   (United States)

^b Icagen Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLOOXYGENASE 2; ISOMERASE INHIBITOR; OXICAM DERIVATIVE; PROSTAGLANDIN E SYNTHASE 1; PROSTAGLANDIN E SYNTHASE 1 INHIBITOR; PROSTAGLANDIN E2; UNCLASSIFIED DRUG;

ARTICLE; CELL ASSAY; DRUG INHIBITION; DRUG SELECTIVITY; ENZYME ASSAY; HUMAN; HUMAN CELL; STRUCTURE ACTIVITY RELATION;

ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; CELL LINE; CYCLIC S-OXIDES; ENZYME INHIBITORS; HUMANS; INTRAMOLECULAR OXIDOREDUCTASES; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZINES;

EID: 76649142022     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.01.060     Document Type: Article

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27. 4 and filtered. Buffer (294 μL) was combined with 6 μL of 30 mM DMSO stock solutions in a Millipore polycarbonate filter solubility plate (part# MSSLBPC10) for a final a final DMSO concentration of 2%. The plates were heat sealed with a polypropylene seal. After 24 h of 200 rpm shaking at room temperature (23-25 °C), the plates were vacuum filtered into deep well receiver plates. Filtrates were injected into the chemiluminescent nitrogen detector (Antek 8060) for quantification. Apparent concentration was divided by the number of nitrogens in the sample (from the molecular formula) to determine the concentration. The results are reported here in μg/mL and μM.
28. 2α in the conditioned media were measured by ELISA.
29. 2 levels by ELISA.