Sar in the alkoxy lactone series:: The discovery of DFP, a potent and orally active COX-2 inhibitor

被引：49
|
作者：
Leblanc, Y
Roy, P
Boyce, S
Brideau, C
Chan, CC
Charleson, S
Gordon, R
Grimm, E
Guay, J
Léger, S
Li, CS
Riendeau, D
Visco, D
Wang, Z
Webb, J
Xu, LJ
Prasit, P
机构：
[1] Merck Frosst Ctr Therapeut Res, Pointe Claire, PQ H9R 4P8, Canada
[2] Merck Res Labs, Harlow, Essex, England
[3] Merck Res Labs, Rahway, NJ USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 15期
关键词：
D O I：
10.1016/S0960-894X(99)00365-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Extensive SAR has been established in the alkoxy lactone series and this has lead to the discovery of DFP (5,5-dimethyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2-(5H)-furanone), a potent COX-2 inhibitor exhibiting in vivo efficacy in all models studied. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2207 / 2212
页数：6
相关论文
共 50 条
  • [41] Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR
    Petros, Andrew M.
    Huth, Jeffrey R.
    Oost, Thorsten
    Park, Cheol-Min
    Ding, Hong
    Wang, Xilu
    Zhang, Haichao
    Nimmer, Paul
    Mendoza, Renaldo
    Sun, Chaohong
    Mack, Jamey
    Walter, Karl
    Dorwin, Sarah
    Gramling, Emily
    Ladror, Uri
    Rosenberg, Saul H.
    Elmore, Steven W.
    Fesik, Stephen W.
    Hajduk, Philip J.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (22) : 6587 - 6591
  • [42] DISCOVERY OF A NOVEL AND POTENT CHOLESTEROL ABSORPTION INHIBITOR (CAI) AS PROMISING ORALLY ACTIVE LIPID LOWERING DRUG
    Kanou, M.
    Nisiwaki, Y.
    Nakano, A.
    Sugimoto, Y.
    Yamanaka, Y.
    Kondo, S.
    ATHEROSCLEROSIS SUPPLEMENTS, 2009, 10 (02)
  • [43] Discovery and preclinical characterization of BMN 673, a highly potent and orally active PARP inhibitor as an anticancer agent
    Wang, Bing
    Chu, Daniel
    Shen, Yuqiao
    Feng, Ying
    Myers, Peter
    Post, Leonard
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2011, 242
  • [44] SELECTIVE CYCLOOXYGENASE INHIBITORS - NOVEL 4-SPIRO 1,2-DIARYLCYCLOPENTENES ARE POTENT AND ORALLY-ACTIVE COX-2 INHIBITORS
    REITZ, DB
    HUANG, HC
    LI, JJ
    GARLAND, DJ
    MANNING, RE
    ANDERSON, GD
    GREGORY, SA
    KOBOLDT, CM
    PERKINS, WE
    SEIBERT, K
    ISAKSON, PC
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1995, 5 (08) : 867 - 872
  • [45] Novel 1,2-diarylcyclobutenes: Selective and orally active COX-2 inhibitors.
    Frenette, R
    Friesen, RW
    Dube, D
    Fortin, R
    Prescott, S
    Cromlish, W
    Greig, G
    Kargman, S
    Wong, E
    CHan, CC
    Gordon, R
    Xu, L
    Riendeau, D
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1997, 213 : 70 - MEDI
  • [46] Orally active small molecule inhibitors of TNF-α and COX-2 for the treatment of inflammatory disorders
    Pandey, B
    Balse, P
    Nag, A
    Gutula, S
    Neogi, P
    Nag, B
    Dey, D
    FASEB JOURNAL, 2004, 18 (04): : A455 - A455
  • [47] Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators
    Iino, Tomoharu
    Tsukahara, Daisuke
    Kamata, Kenji
    Sasaki, Kaori
    Ohyama, Sumika
    Hosaka, Hideka
    Hasegawa, Takuro
    Chiba, Masato
    Nagata, Yasufumi
    Eiki, Jun-ichi
    Nishimura, Teruyuki
    BIOORGANIC & MEDICINAL CHEMISTRY, 2009, 17 (07) : 2733 - 2743
  • [48] Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer
    Yao, Wenqing
    Zhuo, Jincong
    Burns, David M.
    Xu, Meizhong
    Zhang, Colin
    Li, Yun-Long
    Qian, Ding-Quan
    He, Chunhong
    Weng, Lingkai
    Shi, Eric
    Lin, Qiyan
    Agrios, Costas
    Burn, Timothy C.
    Caulder, Eian
    Covington, Maryanne B.
    Fridman, Jordan S.
    Friedman, Steven
    Katiyar, Kamna
    Hollis, Gregory
    Li, Yanlong
    Liu, Changnian
    Liu, Xiangdong
    Marando, Cindy A.
    Newton, Robert
    Pan, Max
    Scherle, Peggy
    Taylor, Nancy
    Vaddi, Kris
    Wasserman, Zelda R.
    Wynn, Richard
    Yeleswaram, Swamy
    Jalluri, Ravi
    Bower, Michael
    Zhou, Bing-Bing
    Metcalf, Brian
    JOURNAL OF MEDICINAL CHEMISTRY, 2007, 50 (04) : 603 - 606
  • [49] Discovery of DS-5272 as a promising candidate: A potent and orally active p53-MDM2 interaction inhibitor
    Miyazaki, Masaki
    Uoto, Kouichi
    Sugimoto, Yuuichi
    Naito, Hiroyuki
    Yoshida, Keisuke
    Okayama, Tooru
    Kawato, Haruko
    Miyazaki, Masaya
    Kitagawa, Mayumi
    Seki, Takahiko
    Fukutake, Setsuko
    Aonuma, Masashi
    Soga, Tsunehiko
    BIOORGANIC & MEDICINAL CHEMISTRY, 2015, 23 (10) : 2360 - 2367
  • [50] Comparison of the effects of the selective COX-2 inhibitor, DFP, and indomethacin on leukocyte-endothelial cell interactions in the rat mesentery
    Calatayud, S
    Allcock, GH
    Perretti, M
    Mitchell, JA
    Warner, TD
    BRITISH JOURNAL OF PHARMACOLOGY, 2001, 133 : U102 - U102
12345