1-acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors:: Synthesis and evaluation of biological activities

被引：119

作者：

Lin, RH ^{[1
]}

Connolly, PJ ^{[1
]}

Huang, SL ^{[1
]}

Wetter, SK ^{[1
]}

Lu, YH ^{[1
]}

Murray, WV ^{[1
]}

Emanuel, SL ^{[1
]}

Gruninger, RH ^{[1
]}

Fuentes-Pesquera, AR ^{[1
]}

Rugg, CA ^{[1
]}

Middleton, SA ^{[1
]}

Jolliffe, LK ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Drug Discovery, Raritan, NJ 08869 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 13期

关键词：

D O I：

10.1021/jm050267e

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1-acyl-1H-[1,2,4]triazole-3,5-diamine analogues were synthesized as cyclin-dependent kinase (CDK) inhibitors. These compounds showed potent and selective CDK1 and CDK2 inhibitory activities and inhibited in vitro cellular proliferation in various human tumor cells. Representative compound 3b demonstrated in vivo efficacy in a human melanoma A375 xenograft model in nude mice.

引用

页码：4208 / 4211

页数：4

共 18 条

[1]

CHONG WKM, 1999, Patent No. 9921845

[2]

Emanuel Stuart L., 2004, Proceedings of the American Association for Cancer Research Annual Meeting, V45, P191

[3] CDK inhibitors in clinical development for the treatment of cancer [J].

Fischer, PM ;

Gianella-Borradori, A .

EXPERT OPINION ON INVESTIGATIONAL DRUGS, 2003, 12 (06) :955-970

[4] Cyclin-dependent kinases [J].

Harper, JW ;

Adams, PD .

CHEMICAL REVIEWS, 2001, 101 (08) :2511-2526

[5] 1-(N-arylthiocarbamoyl)amidino-3,5-dimethyl pyrazoles - Preparation and use in heterocycle synthesis [J].

Jenardanan, GC ;

Francis, M ;

Deepa, S ;

Rajasekharan, KN .

SYNTHETIC COMMUNICATIONS, 1997, 27 (19) :3457-3462

[6]

KRUEGER M, 2002, Patent No. 0294814

[7]

LI L, 1999, 218 NAT M ACS NEW OR

[8] 3-acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation [J].

Lin, RH ;

Lu, YH ;

Wetter, SK ;

Connolly, PJ ;

Turchi, IJ ;

Murray, WV ;

Emanuel, SL ;

Gruninger, RH ;

Fuentes-Pesquera, AR ;

Adams, M ;

Pandey, N ;

Moreno-Mazza, S ;

Middleton, SA ;

Jolliffe, LK .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (09) :2221-2224

[9] N-(Cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase -: 2.: N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent [J].

Misra, RN ;

Xiao, HY ;

Kim, KS ;

Lu, SF ;

Han, WC ;

Barbosa, SA ;

Hunt, JT ;

Rawlins, DB ;

Shan, WF ;

Ahmed, SZ ;

Qian, LG ;

Chen, BC ;

Zhao, RL ;

Bednarz, MS ;

Kellar, KA ;

Mulheron, JG ;

Batorsky, R ;

Roongta, U ;

Kamath, A ;

Marathe, P ;

Ranadive, SA ;

Sack, JS ;

Tokarski, JS ;

Pavletich, NP ;

Lee, FYF ;

Webster, KR ;

Kimball, SD .

JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (07) :1719-1728

[10]

ORTHO MCNEIL PHARM I, 2002, Patent No. 02057240

← 1 2 →