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Lead ModificationG



(1)COX-1 ID50 = 5.4uM
  COX-2 ID50 = 0.008uM
  selectivity =675:1

									(2)COX-1 ID50 > 100uM
									  COX-2 ID50 = 0.004uM
(1) n=0	(2) n=1 (3) n=2 (4)n=3            selectivity >25000:1

(3)COX-1 ID50 > 100uM				(4)COX-1 ID50 > 100uM
  COX-2 ID50 = 0.062uM				  COX-2 ID50 >100uM
  selectivity >1612:1					  no selectivity 

mUߥŲcvTCOXܾʩ
									
									 


									(5)R1=F R2=CH3
									(6)R1=F R2=CH2F
									(7)R1=F R2=CF3
									(8)R1=F R2=C2H5

ѥmUߥŲcCOX-2 activity 5 > 6 > 7 > 8 










(9)COX-1 ID50 > 18.3uM		            (10)COX-1 ID50 = 3.68uM
  COX-2 ID50 = 0.15uM    				   COX-2 ID50 = 0.52uM
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(11)COX-1 ID50 = 4.21uM                 (11)COX-1 ID50 = 0.027uM
   COX-2 ID50 = 0.007uM				       COX-2 ID50 = 0.003uM
   selectivity >601:1						   selectivity 9:1

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Lead ModificationG



(1)COX-1 ID50 = 5.4uM
  COX-2 ID50 = 0.008uM
  selectivity =675:1

									(2)COX-1 ID50 > 100uM
									  COX-2 ID50 = 0.004uM
(1) n=0	(2) n=1 (3) n=2 (4)n=3            selectivity >25000:1

(3)COX-1 ID50 > 100uM				(4)COX-1 ID50 > 100uM
  COX-2 ID50 = 0.062uM				  COX-2 ID50 >100uM
  selectivity >1612:1					  no selectivity 

mUߥŲcvTCOXܾʩ
									
									 


									(5)R1=F R2=CH3
									(6)R1=F R2=CH2F
									(7)R1=F R2=CF3
									(8)R1=F R2=C2H5

ѥmUߥŲcCOX-2 activity 5 > 6 > 7 > 8 










(9)COX-1 ID50 > 18.3uM		            (10)COX-1 ID50 = 3.68uM
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