Literature DB >> 12217372

Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors.

Mark E Fraley1, William F Hoffman, Robert S Rubino, Randall W Hungate, Andrew J Tebben, Ruth Z Rutledge, Rosemary C McFall, William R Huckle, Richard L Kendall, Kathleen E Coll, Kenneth A Thomas.   

Abstract

We have synthesized and evaluated the activity of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines as a new class of KDR kinase inhibitors. Starting with screening lead 1, potency against isolated KDR was fully optimized with 3-thienyl and 4-methoxyphenyl substituents at the 6- and 3-positions (3g, KDR IC(50)=19 nM), respectively. The synthesis and SAR of these compounds are described.

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Year:  2002        PMID： 12217372     DOI： 10.1016/s0960-894x(02)00525-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  17 in total

1.  Synthesis of some new pyrazolo[1,5-a]pyrimidine, pyrazolo[5,1-c]triazine, 1,3,4-thiadiazole and pyridine derivatives containing 1,2,3-triazole moiety.

Authors:  Nadia A Abdelriheem; Yasser H Zaki; Abdou O Abdelhamid
Journal:  Chem Cent J       Date:  2017-06-12       Impact factor: 4.215

2.  In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.

Authors:  Jijun Hao; Joshua N Ho; Jana A Lewis; Kaleh A Karim; R Nathan Daniels; Patrick R Gentry; Corey R Hopkins; Craig W Lindsley; Charles C Hong
Journal:  ACS Chem Biol       Date:  2010-02-19       Impact factor: 5.100

3.  A facile, regioselective synthesis of novel 3-(N-phenylcarboxamide)pyrazolo[1,5-a]pyrimidine analogs in the presence of KHSO4 in aqueous media assisted by ultrasound and their antibacterial activities.

Authors:  Shunan Kaping; Ivee Boiss; Laishram Indira Singha; Philippe Helissey; Jai N Vishwakarma
Journal:  Mol Divers       Date:  2015-10-28       Impact factor: 2.943

4.  Vascular endothelial growth factor receptor 1 contributes to Escherichia coli K1 invasion of human brain microvascular endothelial cells through the phosphatidylinositol 3-kinase/Akt signaling pathway.

Authors:  Wei-Dong Zhao; Wei Liu; Wen-Gang Fang; Kwang Sik Kim; Yu-Hua Chen
Journal:  Infect Immun       Date:  2010-08-30       Impact factor: 3.441

5.  Investigation of a novel molecular descriptor for the lead optimization of 4-aminoquinazolines as vascular endothelial growth factor receptor-2 inhibitors: application for quantitative structure-activity relationship analysis in lead optimization.

Authors:  Joel K Kawakami; Yannica Martinez; Brandi Sasaki; Melissa Harris; Wendy E Kurata; Alan F Lau
Journal:  Bioorg Med Chem Lett       Date:  2011-01-14       Impact factor: 2.823

6.  Intersegmental vessel formation in zebrafish: requirement for VEGF but not BMP signalling revealed by selective and non-selective BMP antagonists.

Authors:  J E Cannon; P D Upton; J C Smith; N W Morrell
Journal:  Br J Pharmacol       Date:  2010-09       Impact factor: 8.739

7.  Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors.

Authors:  Gregory D Cuny; Paul B Yu; Joydev K Laha; Xuechao Xing; Ji-Feng Liu; Carol S Lai; Donna Y Deng; Chetana Sachidanandan; Kenneth D Bloch; Randall T Peterson
Journal:  Bioorg Med Chem Lett       Date:  2008-06-27       Impact factor: 2.823

8.  Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism.

Authors:  Paul B Yu; Charles C Hong; Chetana Sachidanandan; Jodie L Babitt; Donna Y Deng; Stefan A Hoyng; Herbert Y Lin; Kenneth D Bloch; Randall T Peterson
Journal:  Nat Chem Biol       Date:  2007-11-18       Impact factor: 15.040

Review 9.  Applications of small molecule BMP inhibitors in physiology and disease.

Authors:  Charles C Hong; Paul B Yu
Journal:  Cytokine Growth Factor Rev       Date:  2009-11-14       Impact factor: 7.638

10.  Interactions between vascular endothelial growth factor and neuroglobin.

Authors:  Kunlin Jin; Xiao Mao; Lin Xie; David A Greenberg
Journal:  Neurosci Lett       Date:  2012-05-11       Impact factor: 3.046
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