Design, synthesis, and studies of small molecule STAT3 inhibitors

被引：84

作者：

Bhasin, Deepak ^{[1
]}

Cisek, Katryna ^{[1
]}

Pandharkar, Trupti ^{[1
]}

Regan, Nicholas ^{[1
]}

Li, Chenglong ^{[1
]}

Pandit, Bulbul ^{[1
]}

Lin, Jiayuh ^{[2
]}

Li, Pui-Kai ^{[1
]}

机构：

[1] Ohio State Univ, Coll Pharm, Div Med Chem & Pharmacognosy, Columbus, OH 43210 USA

[2] Ohio State Univ, Columbus Childrens Res Inst, Ctr Childhood Canc, Columbus, OH 43205 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 01期

关键词：

D O I：

10.1016/j.bmcl.2007.10.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of small molecule STAT3 inhibitors originally derived from our lead compound STA 21 were synthesized and evaluated. The most potent compound in this series, compound 1, exhibited the same anti-proliferative activities as STA 21 against prostate cancer cell lines that express constitutively active STAT3. Molecular docking showed compound 1 bound to the STAT3 beta SH2 domain in a similar manner as STA 21. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：391 / 395

页数：5

共 31 条

[1]

Barton BE, 2004, MOL CANCER THER, V3, P11

[2] STATs in oncogenesis [J].

Bowman, T ;

Garcia, R ;

Turkson, J ;

Jove, R .

ONCOGENE, 2000, 19 (21) :2474-2488

[3] Signal transducers and activators of transcription as regulators of growth, apoptosis and breast development [J].

Bromberg, J .

BREAST CANCER RESEARCH, 2000, 2 (02) :86-90

[4]

Buettner R, 2002, CLIN CANCER RES, V8, P945

[5] Constitutive activation of Stat3 signaling confers resistance to apoptosis in human U266 myeloma cells [J].

Catlett-Falcone, R ;

Landowski, TH ;

Oshiro, MM ;

Turkson, J ;

Levitzki, A ;

Savino, R ;

Ciliberto, G ;

Moscinski, L ;

Fernández-Luna, JL ;

Nuñez, G ;

Dalton, WS ;

Jove, R .

IMMUNITY, 1999, 10 (01) :105-115

[6]

Catlett-Falcone Robyn, 1999, Current Opinion in Oncology, V11, P490, DOI 10.1097/00001622-199911000-00010

[7] JAK-STAT PATHWAYS AND TRANSCRIPTIONAL ACTIVATION IN RESPONSE TO IFNS AND OTHER EXTRACELLULAR SIGNALING PROTEINS [J].

DARNELL, JE ;

KERR, IM ;

STARK, GR .

SCIENCE, 1994, 264 (5164) :1415-1421

[8] Stat3 enhances the growth of LNCaP human prostate cancer cells in intact and castrated male nude mice [J].

DeMiguel, F ;

Lee, SO ;

Lou, W ;

Xiao, X ;

Pflug, BR ;

Nelson, JB ;

Gao, AC .

PROSTATE, 2002, 52 (02) :123-129

[9] Stat3 activation in prostatic carcinomas [J].

Dhir, R ;

Ni, ZY ;

Lou, W ;

DeMiguel, F ;

Grandis, JR ;

Gao, AC .

PROSTATE, 2002, 51 (04) :241-246

[10] Down-regulation of signal transducer and activator of transcription 3 expression using vector-based small interfering RNAs suppresses growth of human prostate tumor in vivo [J].

Gao, LF ;

Zhang, L ;

Hu, JD ;

Li, F ;

Shao, YT ;

Zhao, D ;

Kalvakolanu, DV ;

Kopecko, DJ ;

Zhao, XJ ;

Xu, DQ .

CLINICAL CANCER RESEARCH, 2005, 11 (17) :6333-6341

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