1,4,5,6-Tetrahydropyrrolo[3,4-c]pyrazoles: Identification of a Potent Aurora Kinase Inhibitor with a Favorable Antitumor Kinase Inhibition Profile
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- 作者：Daniele Fancelli ; Jü ; rgen Moll ; Mario Varasi ; Rodrigo Bravo ; Roberta Artico ; Daniela Berta ; Simona Bindi ; Alexander Cameron ; Ilaria Candiani ; Paolo Cappella ; Patrizia Carpinelli ; Walter Croci ; Bar
- 刊名：Journal of Medicinal Chemistry
- 出版年：2006
- 出版时间：November 30, 2006
- 年：2006
- 卷：49
- 期：24
- 页码：7247 - 7251
- 全文大小：147K
- 年卷期：v.49,no.24(November 30, 2006)
- ISSN：1520-4804
文摘
The optimization of a series of 5-phenylacetyl 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole derivatives towardthe inhibition of Aurora kinases led to the identification of compound 9d. This is a potent inhibitor ofAurora kinases that also shows low nanomolar potency against additional anticancer kinase targets. Basedon its high antiproliferative activity on different cancer cell lines, favorable chemico-physical andpharmacokinetic properties, and high efficacy in in vivo tumor models, compound 9d was ultimately selectedfor further development.