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Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.

Publication ,  Journal Article
Lau, CK; Brideau, C; Chan, CC; Charleson, S; Cromlish, WA; Ethier, D; Gauthier, JY; Gordon, R; Guay, J; Kargman, S; Li, CS; Prasit, P; Xu, L ...
Published in: Bioorganic & medicinal chemistry letters
November 1999

A series of 3-heteroaryloxy4-phenyl-2-5H)-furanones were prepared and evaluated for their potency and selectivity as COX-2 inhibitors. This led to the identification of L-778,736 as a potent, orally active and selective inhibitor of the COX-2 enzyme.

Duke Scholars

Published In

Bioorganic & medicinal chemistry letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

November 1999

Volume

9

Issue

22

Start / End Page

3187 / 3192

Related Subject Headings

  • Rats
  • Pyridines
  • Prostaglandin-Endoperoxide Synthases
  • Membrane Proteins
  • Medicinal & Biomolecular Chemistry
  • Isoenzymes
  • Humans
  • Furans
  • Cyclooxygenase Inhibitors
  • Cyclooxygenase 2 Inhibitors
 

Citation

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Lau, C. K., Brideau, C., Chan, C. C., Charleson, S., Cromlish, W. A., Ethier, D., … Xu, L. (1999). Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors. Bioorganic & Medicinal Chemistry Letters, 9(22), 3187–3192. https://doi.org/10.1016/s0960-894x(99)00560-0
Lau, C. K., C. Brideau, C. C. Chan, S. Charleson, W. A. Cromlish, D. Ethier, J. Y. Gauthier, et al. “Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.Bioorganic & Medicinal Chemistry Letters 9, no. 22 (November 1999): 3187–92. https://doi.org/10.1016/s0960-894x(99)00560-0.
Lau CK, Brideau C, Chan CC, Charleson S, Cromlish WA, Ethier D, et al. Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors. Bioorganic & medicinal chemistry letters. 1999 Nov;9(22):3187–92.
Lau, C. K., et al. “Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.Bioorganic & Medicinal Chemistry Letters, vol. 9, no. 22, Nov. 1999, pp. 3187–92. Epmc, doi:10.1016/s0960-894x(99)00560-0.
Lau CK, Brideau C, Chan CC, Charleson S, Cromlish WA, Ethier D, Gauthier JY, Gordon R, Guay J, Kargman S, Li CS, Prasit P, Riendeau D, Thérien M, Visco DM, Xu L. Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors. Bioorganic & medicinal chemistry letters. 1999 Nov;9(22):3187–3192.
Journal cover image

Published In

Bioorganic & medicinal chemistry letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

November 1999

Volume

9

Issue

22

Start / End Page

3187 / 3192

Related Subject Headings

  • Rats
  • Pyridines
  • Prostaglandin-Endoperoxide Synthases
  • Membrane Proteins
  • Medicinal & Biomolecular Chemistry
  • Isoenzymes
  • Humans
  • Furans
  • Cyclooxygenase Inhibitors
  • Cyclooxygenase 2 Inhibitors