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1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2006 Aug 15 , DOI: 10.1016/j.bmcl.2006.05.066 Jürgen Dinges , Kimba L. Ashworth , Irini Akritopolou-Zanze , Lee D. Arnold , Steven A. Baumeister , Peter F. Bousquet , George A. Cunha , Steven K. Davidsen , Stevan W. Djuric , Vijaya J. Gracias , Michael R. Michaelides , Paul Rafferty , Thomas J. Sowin , Kent D. Stewart , Zhiren Xia , Henry Q. Zhang
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2006 Aug 15 , DOI: 10.1016/j.bmcl.2006.05.066 Jürgen Dinges , Kimba L. Ashworth , Irini Akritopolou-Zanze , Lee D. Arnold , Steven A. Baumeister , Peter F. Bousquet , George A. Cunha , Steven K. Davidsen , Stevan W. Djuric , Vijaya J. Gracias , Michael R. Michaelides , Paul Rafferty , Thomas J. Sowin , Kent D. Stewart , Zhiren Xia , Henry Q. Zhang
A series of 1,4-dihydroindeno[1,2-c]pyrazoles with a 3-thiophene substituent carrying a urea-type side chain were identified as potent multitargeted (VEGFR and PDGFR families) receptor tyrosine kinase inhibitors. A KDR homology model suggested that the urea moiety is able to interact with a recognition motif in the hydrophobic specificity pocket of the enzyme.
中文翻译：
1,4-二氢茚并[1,2-c]吡唑类化合物是新型的多靶点受体酪氨酸激酶抑制剂。
一系列带有带有尿素型侧链的3-噻吩取代基的1,4-二氢茚并[1,2-c]吡唑被确定为有效的多靶点（VEGFR和PDGFR家族）受体酪氨酸激酶抑制剂。KDR同源性模型表明，尿素部分能够与酶的疏水特异性口袋中的识别基序相互作用。
更新日期：2017-01-31
中文翻译：
1,4-二氢茚并[1,2-c]吡唑类化合物是新型的多靶点受体酪氨酸激酶抑制剂。
一系列带有带有尿素型侧链的3-噻吩取代基的1,4-二氢茚并[1,2-c]吡唑被确定为有效的多靶点（VEGFR和PDGFR家族）受体酪氨酸激酶抑制剂。KDR同源性模型表明，尿素部分能够与酶的疏水特异性口袋中的识别基序相互作用。
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