Literature DB >> 12941342

Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.

Wei He1, Michael R Myers, Barbara Hanney, Alfred P Spada, Glenda Bilder, Helen Galzcinski, Dilip Amin, Saul Needle, Ken Page, Zaid Jayyosi, Mark H Perrone.   

Abstract

RPR127963 demonstrates an excellent pharmacokinetic profile in several species and was found to be efficacious in the prevention of restenosis in a Yucatan mini-pig model upon oral administration of 1-5 mg/kg. The in vitro selectivity profile and SAR of the highly optimized PDGF-R tyrosine kinase inhibitor are highlighted.

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Year:  2003        PMID： 12941342     DOI： 10.1016/s0960-894x(03)00655-3

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


  18 in total

1.  6a-Nitro-6-(2,2,7,7-tetra-methyl-tetra-hydro-3aH-bis-[1,3]dioxolo[4,5-b:4',5'-d]pyran-5-yl)-6a,6b,7,8,9,11a-hexa-hydro-6H-spiro-[chromeno[3,4-a]pyrrolizine-11,11'-indeno-[1,2-b]quinoxaline].

Authors:  T Anuradha; J Naga Siva Rao; P R Seshadri; R Raghunathan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-12-14

2.  Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.

Authors:  Xiaokai Li; Nina Liu; Huaning Zhang; Susan E Knudson; Richard A Slayden; Peter J Tonge
Journal:  Bioorg Med Chem Lett       Date:  2010-08-21       Impact factor: 2.823

3.  2,3-Bis(4-ethoxy-phen-yl)quinoxaline.

Authors:  Ping-Ping Ye; Cai-Li Zhang; Zhi-Qiang Du
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-12-12

4.  One-pot three-component synthesis of quinoxaline and phenazine ring systems using Fischer carbene complexes.

Authors:  Priyabrata Roy; Binay Krishna Ghorai
Journal:  Beilstein J Org Chem       Date:  2010-05-25       Impact factor: 2.883

5.  4-[3-(4-Fluoro-phen-yl)quinoxalin-2-yl]-N-isopropyl-pyridin-2-amine.

Authors:  Pierre Koch; Dieter Schollmeyer; Stefan Laufer
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-05-20

6.  3-(4-Fluoro-phen-yl)-6-meth-oxy-2-(4-pyrid-yl)quinoxaline.

Authors:  Hartmut Jahns; Pierre Koch; Dieter Schollmeyer; Stefan Laufer
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-06-20

7.  Construction of hybrid polycyclic quinolinobenzo[a]phenazinone architectures using solid-state melt reaction (SSMR).

Authors:  Manickam Bakthadoss; Varathan Vinayagam
Journal:  Mol Divers       Date:  2020-05-04       Impact factor: 2.943

8.  Ethyl 1''-benzyl-2''-oxo-2',3',5',6',7',7a'-hexa-hydro-1'H-di-spiro-[indeno-[1,2-b]quinoxaline-11,2'-pyrrolizine-3',3''-indoline]-1'-carboxyl-ate monohydrate.

Authors:  Piskala Subburaman Kannan; Srinu Lanka; Sathiah Thennarasu; Gopal Vimala; Arunachalathevar Subbiahpandi
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-05-11

9.  2-[3-(2-Acetoxyphenyl)quinoxa-lin-2-yl]phenyl acetate.

Authors:  Dan-Feng Shen; Shao-Jie Lou; Dan-Qian Xu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-04-20

10.  5,6-Dimethyl-pyrazine-2,3-dicarbonitrile.

Authors:  Ghasem Rezanejade Bardajee; Alan J Lough; Mitchell A Winnik
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-10-27
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