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

来源：

EXPERT OPINION ON THERAPEUTIC PATENTS | 2001年 / 11卷 / 03期

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

页码：405 / 429

页数：25

共 59 条

[41] p38 Kinase inhibitors for the treatment of arthritis and osteoporosis: Thienyl, furyl, and pyrrolyl ureas [J].

Redman, AM ;

Johnson, JS ;

Dally, R ;

Swartz, S ;

Wild, H ;

Paulsen, H ;

Caringal, Y ;

Gunn, D ;

Renick, J ;

Osterhout, M ;

Kingery-Wood, J ;

Smith, RA ;

Lee, W ;

Dumas, J ;

Wilhelm, SM ;

Housley, TJ ;

Bhargava, A ;

Ranges, GE ;

Shrikhande, A ;

Young, D ;

Bombara, M ;

Scott, WJ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (01) :9-12

[42]

RICE AG, 2000, P 91 M AM ASS CANC R

[43] Transformation mediated by RhoA requires activity of ROCK kinases [J].

Sahai, E ;

Ishizaki, T ;

Narumiya, S ;

Treisman, R .

CURRENT BIOLOGY, 1999, 9 (03) :136-145

[44]

Sausville EA, 2000, ANTI-CANCER DRUG DES, V15, P1

[45] Inhibition of Rho-associated kinase results in suppression of neointimal formation of balloon-injured arteries [J].

Sawada, N ;

Itoh, H ;

Ueyama, K ;

Yamashita, J ;

Doi, K ;

Chun, TH ;

Inoue, M ;

Masatsugu, K ;

Saito, T ;

Fukunaga, Y ;

Sakaguchi, S ;

Arai, H ;

Ohno, N ;

Komeda, M ;

Nakao, K .

CIRCULATION, 2000, 101 (17) :2030-2033

[46] Paullones, a series of cyclin-dependent kinase inhibitors: Synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity [J].

Schultz, C ;

Link, A ;

Leost, M ;

Zaharevitz, DW ;

Gussio, R ;

Sausville, EA ;

Meijer, L ;

Kunick, C .

JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (15) :2909-2919

[47] Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo [J].

Sebolt-Leopold, JS ;

Dudley, DT ;

Herrera, R ;

Van Becelaere, K ;

Wiland, A ;

Gowan, RC ;

Tecle, H ;

Barrett, SD ;

Bridges, A ;

Przybranowski, S ;

Leopold, WR ;

Saltiel, AR .

NATURE MEDICINE, 1999, 5 (07) :810-816

[48] Synthesis and biological evaluations of 3-substituted indolin-2-ones: A novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases [J].

Sun, L ;

Tran, N ;

Tang, F ;

App, H ;

Hirth, P ;

McMahon, G ;

Tang, C .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (14) :2588-2603

[49] Design, synthesis, and evaluations of substituted 3-[(3-or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases [J].

Sun, L ;

Tran, N ;

Liang, CX ;

Tang, F ;

Rice, A ;

Schreck, R ;

Waltz, K ;

Shawver, LK ;

McMahon, G ;

Tang, C .

JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (25) :5120-5130

[50] Identification of substituted 3-[(4,5,6,7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rβ tyrosine kinases [J].

Sun, L ;

Tran, N ;

Liang, CX ;

Hubbard, S ;

Tang, F ;

Lipson, K ;

Schreck, R ;

Zhou, Y ;

McMahon, G ;

Tang, C .

JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (14) :2655-2663

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