Protein kinase inhibitors: emerging pharmacophores 1997-2000

被引:78
作者
Dumas, J [1 ]
机构
[1] Bayer Corp, Div Pharmaceut, Bayer Res Ctr, W Haven, CT 06516 USA
关键词
angiogenesis; cancer; cell cycle; inflammation; kinase; MAPK; receptor kinase;
D O I
10.1517/13543776.11.3.405
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Kinase inhibition is a major area for therapeutic intervention against a variety of diseases including cancer, inflammatory disorders and diabetes. While this mode of action remains very promising at this time, it faces critical challenges, such as drug safety, and biopharmaceutical profile. This review provides an update on kinase inhibitor pharmacophores from a structural standpoint. Advances in older inhibitor classes as well as new emerging lead structures will be presented.
引用
收藏
页码:405 / 429
页数:25
相关论文
共 59 条
[1]  
Adams J L, 1999, Curr Opin Drug Discov Devel, V2, P96
[2]  
BARRETT SD, 1999, 218 ACS NAT M NEW OR
[3]   Restenosis following angioplasty in the swine coronary artery is inhibited by an orally active PDGF-receptor tyrosine kinase inhibitor, RPR101511A [J].
Bilder, G ;
Wentz, T ;
Leadley, R ;
Amin, D ;
Byan, L ;
O'Conner, B ;
Needle, S ;
Galczenski, H ;
Bostwick, J ;
Kasiewski, C ;
Myers, M ;
Spada, A ;
Merkel, L ;
Ly, C ;
Persons, P ;
Page, K ;
Perrone, M ;
Dunwiddie, C .
CIRCULATION, 1999, 99 (25) :3292-3299
[4]   New inhibitors of p38 kinase [J].
Boehm, JC ;
Adams, JL .
EXPERT OPINION ON THERAPEUTIC PATENTS, 2000, 10 (01) :25-37
[5]   New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis [J].
Bold, G ;
Altmann, KH ;
Frei, J ;
Lang, M ;
Manley, PW ;
Traxler, P ;
Wietfeld, B ;
Brüggen, J ;
Buchdunger, E ;
Cozens, R ;
Ferrari, S ;
Furet, P ;
Hofmann, F ;
Martiny-Baron, G ;
Mestan, J ;
Rösel, J ;
Sills, M ;
Stover, D ;
Acemoglu, F ;
Boss, E ;
Emmenegger, R ;
Lässer, L ;
Masso, E ;
Roth, R ;
Schlachter, C ;
Vetterli, W ;
Wyss, D ;
Wood, JM .
JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (12) :2310-2323
[6]  
Bridges A, 1998, EMERGING DRUGS, V3, P279, DOI [10.1517/ 14728214.3.1.279, DOI 10.1517/14728214.3.1.279]
[7]   Tyrosine kinase inhibitors .8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor [J].
Bridges, AJ ;
Zhou, H ;
Cody, DR ;
Rewcastle, GW ;
McMichael, A ;
Showalter, HDH ;
Fry, DW ;
Kraker, AJ ;
Denny, WA .
JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (01) :267-276
[8]  
CHENG S, 2000, 219 ACS NAT M SAN FR
[9]   Progress in the development of inhibitors of SH2 domains [J].
Cody, WL ;
Lin, ZW ;
Panek, RL ;
Rose, DW ;
Rubin, JR .
CURRENT PHARMACEUTICAL DESIGN, 2000, 6 (01) :59-98
[10]  
DAVIS ST, 2000, P 91 M AM ASS CANC R