Identification of 7-phenylaxaminothieno[3,2-b]pyridine-6-carbonitriles as a new class of Src kinase inhibitors

被引：48

作者：

Boschelli, DH ^{[1
]}

Wu, BQ ^{[1
]}

Sosa, ACB ^{[1
]}

Durutlic, H ^{[1
]}

Ye, F ^{[1
]}

Raifeld, Y ^{[1
]}

Golas, JM ^{[1
]}

Boschelli, F ^{[1
]}

机构：

[1] Wyeth Res, Pearl River, NY 10965 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 27期

关键词：

D O I：

10.1021/jm049237m

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We disclose here a new class of kinase inhibitors, obtained by replacing the phenyl ring of a 3-quinoline-carbonitrile system with a thiophene ring. When suitably substituted, the resultant 7-phenylaminothieno[3,2-b]pyridine-6-carbonitrile analogues show potent inhibition of Src kinase activity.

引用

收藏

页码：6666 / 6668

页数：3

相关论文

共 21 条

[1] Substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles as Src kinase inhibitors [J].

Berger, D ;

Dutia, M ;

Powell, D ;

Wissner, A ;

DeMorin, F ;

Raifeld, Y ;

Weber, J ;

Boschelli, F .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (20) :2989-2992

[2] Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity [J].

Boschelli, DH ;

Ye, F ;

Wang, YD ;

Dutia, M ;

Johnson, SL ;

Wu, BQ ;

Miller, K ;

Powell, DW ;

Yaczko, D ;

Young, M ;

Tischler, M ;

Arndt, K ;

Discafani, C ;

Etienne, C ;

Gibbons, J ;

Grod, J ;

Lucas, J ;

Weber, JM ;

Boschelli, F .

JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (23) :3965-3977

[3] 7-alkoxy-4-phenylamino-3-quinolinecarbonitriles as dual inhibitors of Src and Abl kinases [J].

Boschelli, DH ;

Wang, YND ;

Johnson, S ;

Wu, BQ ;

Ye, F ;

Sosa, ACB ;

Golas, JM ;

Boschelli, F .

JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (07) :1599-1601

[4] Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity [J].

Boschelli, DH ;

Fe, Y ;

Wu, BQ ;

Wang, YD ;

Sosa, ACB ;

Yaczko, D ;

Powell, D ;

Golas, JM ;

Lucas, J ;

Boschelli, F .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2003, 13 (21) :3797-3800

[5] Inhibition of Src kinase activity by 4-anilino-7-thienyl-3-quinolinecarbonitriles [J].

Boschelli, DH ;

Wang, DY ;

Ye, F ;

Yamashita, A ;

Zhang, N ;

Powell, D ;

Weber, J ;

Boschelli, F .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (15) :2011-2014

[6] Synthesis and Src kinase inhibitory activity of a series of 4-phenylamino-3-quinolinecarbonitriles [J].

Boschelli, DH ;

Wang, YD ;

Ye, F ;

Wu, BQ ;

Zhang, N ;

Dutia, M ;

Powell, DW ;

Wissner, A ;

Arndt, K ;

Weber, JM ;

Boschelli, F .

JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (05) :822-833

[7] Role of Src in signal transduction pathways [J].

Courtneidge, SA .

BIOCHEMICAL SOCIETY TRANSACTIONS, 2002, 30 :11-17

[8] Src in cancer: deregulation and consequences for cell behaviour [J].

Frame, MC .

BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER, 2002, 1602 (02) :114-130

[9]

Golas JM, 2003, CANCER RES, V63, P375

[10] Role of Src expression and activation in human cancer [J].

Irby, RB ;

Yeatman, TJ .

ONCOGENE, 2000, 19 (49) :5636-5642