共查询到20条相似文献,搜索用时 31 毫秒
1.
Seela F Lin W Kazimierczuk Z Rosemeyer H Glaron V Peng X He Y Ming X Andrzejewska M Gorska A Zhang X Eickmeier H La Colla P 《Nucleosides, nucleotides & nucleic acids》2005,24(5-7):859-863
The synthesis of base modified L-nucleosides is described with pyrrolo[2,3-d]pyrimidines, pyrazolo[3,4-d]pyrimidines, benzimidazoles, and imidazo[1,2-a]-s-triazines as nucleobases. The conformation of the nucleosides is studied and the antiviral activity is evaluated. 相似文献
2.
An efficient solid phase synthesis of pyrimido[4,5-d]pyrimidine derivatives is described. Reaction of polymer-bound pyrimidine 1 with urea or thiourea followed by cleavage from the support provided 4-aminopyrimido[4,5-d]pyrimidines 4 and 5 while treatment of 6 with phenyl isocyanate or phenyl isothiocyanate followed by cleavage from resin afforded 3-phenylpyrimido[4,5-d]pyrimidines 9 and 10. 相似文献
3.
Cunde Wang Hangxian Xu Zengyang Xie Xingbin Wang Zonglei Zhang Qian Sun 《Steroids》2010,75(12):1033-1038
A novel and practical procedure was developed for the preparation of steroidal[17,16-d]pyrimidines by chlorotrimethylsilane (TMSCl)-promoted one-pot multicomponent Biginelli-like condensations of steroid-17-ones, urea and aromatic aldehydes. First, treatment of the steroid-17-ones with urea and aromatic aldehydes in dimethylformamide (DMF)/acetonitrile (ACN) gives the corresponding Biginelli products, following the aromatising reaction of the Biginelli products at the same time under air to yield the desired steroidal[17,16-d]pyrimidines (78-88%). Since steroidal[17,16-d]pyrimidines with hydroxyl group can be subsequently converted into steroidal[17,16-d]pyrimidine derivatives, this general method provides a highly efficient route to these biologically important compounds. 相似文献
4.
M. Nogueras M. L. Quijano A. Sénchez M. Melgarejo 《Nucleosides, nucleotides & nucleic acids》2013,32(1-2):373-374
Abstract The synthesis of some glycosyl derivatives of furo[2,3-d] and pyrrolo[2,3-d]pyrimidines is described. 相似文献
5.
V. Alexieva I. Sergiev E. Karanov E. Golovinsky E. Stanoeva M. Haimova G. Petrov 《Journal of Plant Growth Regulation》1994,13(3):123-129
The synthesis and physiological activity of some novel 4-substituted triazolo[4,5-d]pyrimidines and 4-substituted pyrazolo[3,4-d]pyrimidines are described. Most of the compounds possessed high anticytokinin activity towards purine (benzyladenine) and phenylurea (4-PU-30) type cytokinins. 1-Benzyl-4-ethoxycarbonylpiperazinyl-1H-1,2,3-triazolo[4,5-d]pyrimidine almost completely removed cytokinin stimulated effects—betacyanin synthesis in Amaranthus caudatus cotyledons; growth of radish cotyledons and retention of chlorophyll in leaf explants. Some chemical structurephysiological activity relationships have been established. 相似文献
6.
Choi HS Wang Z Richmond W He X Yang K Jiang T Sim T Karanewsky D Gu XJ Zhou V Liu Y Ohmori O Caldwell J Gray N He Y 《Bioorganic & medicinal chemistry letters》2006,16(8):2173-2176
A series of 2-amino-9-aryl-7H-pyrrolo[2,3-d]pyrimidines were designed and synthesized to target focal adhesion kinase (FAK). A number of these pyrrolopyrimides exhibited low micromolar inhibitory activities against focal adhesion kinase, and their preliminary SAR was established via systematic chemical modifications. The 2-amino-9-aryl-7H-pyrrolo[2,3-d]pyrimidines represent a new class of kinase inhibitors. 相似文献
7.
Zhao A Gao X Wang Y Ai J Wang Y Chen Y Geng M Zhang A 《Bioorganic & medicinal chemistry》2011,19(13):3906-3918
A series of thieno[2,3-d]pyrimidines and furo[2,3-d]pyrimidines were synthesized and evaluated for the c-Met inhibition. Thieno[2,3-d]pyrimidine 6b stood out as the most potent showing an IC(50) of 35.7 nM. This compound displayed high inhibitory effect on cell proliferation in BaF3-TPR-Met cells and showed high selectivity for c-Met family against other 14 tested kinases. However, compound 6b was found ineffective in the c-Met-dependent U-87MG human gliobastoma xenograft model that may be relevant to its poor PK profile. 相似文献
8.
Pier Giovanni Baraldi Maria Giovanna Pavani Maria del Carmen Nu?ez Patrizia Brigidi Beatrice Vitali Roberto Gambari Romeo Romagnoli 《Bioorganic & medicinal chemistry》2002,10(2):449-456
The reaction of Appel's salt with o-amino nitrile heterocycles 10-19 gave the corresponding 4-chloro-5-heteroimmine-1,2,3-dithiazoles 20-29 which were evaluated for their antibacterial, antifungal and antitumor activity. Although all these N-heteroimines were devoid of significant antibacterial activity, they showed significant antifungal activity. Moreover, the same derivatives represent highly versatile intermediates in heterocyclic synthesis, in fact the pyrazoleimino dithiazoles 20-26 can be converted in one step into 2-cyano derivatives of the corresponding 4-methoxy-pyrazolo[3,4-d]pyrimidines 30-35 by sodium methoxide in refluxing methanol. This provides a general and attractive route to 4-methoxy-6-cyano pyrazolo[3,4-d]pyrimidines from 1-substituted 5-amino pyrazoles 10-19 in two simple steps. Finally, the isosteric replacement of the pyrazole ring atoms to give the imidazole[3,4-d]pyrimidine and triazole [4,5-d] pyrimidine ring systems was examined. 相似文献
9.
Burchat AF Calderwood DJ Hirst GC Holman NJ Johnston DN Munschauer R Rafferty P Tometzki GB 《Bioorganic & medicinal chemistry letters》2000,10(19):2171-2174
Pyrrolo[2,3-d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are novel, potent and selective inhibitors of lck in vitro. Exploration of C-6 position of the pyrrolo[2,3-d]pyrimidine and the terminal phenyl group structure-activity relationship (SAR) is detailed. Compound 1 is orally active in animal models. 相似文献
10.
Abstract 2′,3′ -Dideoxy-L-C-nucleosides, 4-amino-8-(2,3-dideoxy-L-glyceropento-furanosyl)pyrazolo[1,5-a]-1,3,5-triazines (9 and 10), 4-amino-7-(2,3-dideoxy-L-glycero-pentofuranosyl)-3H,5H-pyrrolo[3,2-d]pyrimidines (17 and 18), 7-(2,3-dideoxy-L-glyceropentofuranosyl)-4-oxo-3H,5H-pyrrolo[3,2-d]pyrimidines (23 and 24) and 2,4-diamino-5-(2,3-dideoxy-L-glyceropentofuranosyl)pyrimidines (28 and 29) have been synthesized from L-gulonic γ-lactone 1. 相似文献
11.
Alberti MJ Auten EP Lackey KE McDonald OB Wood ER Preugschat F Cutler GJ Kane-Carson L Liu W Jung DK 《Bioorganic & medicinal chemistry letters》2005,15(16):3778-3781
The discovery, synthesis, potential binding mode, and in vitro kinase profile of several pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines as potent kinase inhibitors are discussed. 相似文献
12.
Electron rich 6-[(dimethylamino)methylene]amino uracil 1, undergoes [4+2] cycloaddition reactions with various in situ generated glyoxylate imine and imine oxides 6 to provide novel pyrimido[4,5-d]pyrimidine derivatives of biological significance, after elimination of dimethylamine from the (1:1) cycloadducts and oxidative aromatisation. This procedure provides a convenient method for the direct synthesis of pyrimido[4,5-d]pyrimidines in excellent yields when carried out in the solid state and under microwave irradiations. 相似文献
13.
Design, synthesis, and structure-activity relationship studies of ATP analogues as DNA gyrase inhibitors 总被引:2,自引:0,他引:2
Lübbers T Angehrn P Gmünder H Herzig S Kulhanek J 《Bioorganic & medicinal chemistry letters》2000,10(8):821-826
We report herein the design and synthesis of ATP-analogues, namely 4-amino-pyrazolo[3,4-d]pyrimidines and 4-amino-pyrazolo[1,5-a][1,3,5]triazines, with DNA gyrase inhibitory activity. Among these series, some compounds exhibited promising antibacterial activity. 相似文献
14.
Altmann E Missbach M Green J Susa M Wagenknecht HA Widler L 《Bioorganic & medicinal chemistry letters》2001,11(6):853-856
7-Heterocyclyl-5-aryl-pyrrolo[2,3-d]pyrimidines represent a new class of highly potent and selective inhibitors of the tyrosine kinase pp60(c-Src). 相似文献
15.
Miyazaki Y Maeda Y Sato H Nakano M Mellor GW 《Bioorganic & medicinal chemistry letters》2008,18(6):1967-1971
4-Amino-5,6-diaryl-furo[2,3-d]pyrimidines have been identified as inhibitors of glycogen synthase kinase-3beta (GSK-3beta). One representative derivative, 4-amino-3-(4-(benzenesulfonylamino)-phenyl)-2-(3-pyridyl)-furo[2,3-d]pyrimidine (12) exhibited potent GSK-3beta inhibitory activity in low nanomolar level of IC(50). The binding mode was proposed from a docking study. 相似文献
16.
Yuan J Gulianello M De Lombaert S Brodbeck R Kieltyka A Hodgetts KJ 《Bioorganic & medicinal chemistry letters》2002,12(16):2133-2136
The synthesis of a series of 3-aryl pyrazolo[4,3-d]pyrimidines as potential corticotropin-releasing factor (CRF-1) antagonists is described. The effects of substitution on the aromatic ring, the amino group and the pyrazolo ring on CRF-1 receptor binding were investigated. 相似文献
17.
Packard GK Papa P Riggs JR Erdman P Tehrani L Robinson D Harris R Shevlin G Perrin-Ninkovic S Hilgraf R McCarrick MA Tran T Fleming Y Bai A Richardson S Katz J Tang Y Leisten J Moghaddam M Cathers B Zhu D Sakata S 《Bioorganic & medicinal chemistry letters》2012,22(1):747-752
The serine/threonine specific protein kinase B-Raf is part of the MAPK pathway and is an interesting oncology target. We have identified thieno[2,3-d]pyrimidines as a core scaffold of small molecule B-Raf inhibitors. The SAR of analogs in this series will be described. 相似文献
18.
Miyazaki Y Matsunaga S Tang J Maeda Y Nakano M Philippe RJ Shibahara M Liu W Sato H Wang L Nolte RT 《Bioorganic & medicinal chemistry letters》2005,15(9):2203-2207
A novel class of furo[2,3-d]pyrimidines has been discovered as potent dual inhibitors of Tie-2 and VEGFR2 receptor tyrosine kinases (TK) and a diarylurea moiety at 5-position shows remarkably enhanced activity against both enzymes. One of the most active compounds, 4-amino-3-(4-((2-fluoro-5-(trifluoromethyl)phenyl)amino-carbonylamino)phenyl)-2-(4-methoxyphenyl)furo[2,3-d]pyrimidine (7k) is <3 nM on both TK receptors and the activity is rationalized based on the X-ray crystal structure. 相似文献
19.
Hunt F Austin C Austin R Bonnert R Cage P Christie J Christie M Dixon C Hill S Jewell R Martin I Robinson D Willis P 《Bioorganic & medicinal chemistry letters》2007,17(10):2731-2734
As part of a Lead Optimisation programme to identify small molecule antagonists of the human CXCR2 receptor, a series of substituted thiazolo[4,5-d]pyrimidines was prepared via the application of a novel tandem displacement reaction. 相似文献
20.
A series of 4-alkoxy-2-methylthiopyrrolo[2,3-d] pyrimidines having alkoxy groups from methoxy to hexyloxy along with the parent 4-hydroxy compound have been tested for cytokinin and anticytokinin activity using tobacco tissue culture. None of the compounds showed any cytokinin activity but several of the compounds were strongly active as anticytokinins, the most active was 4-pentyloxy-2-methyl-thiopyrrolo[2,3-d] pyrimidine. Increasing or decreasing the chain length resulted in a lowering of activity; the hydroxy and methoxy compounds were totally inactive over the concentration range tested. The results are discussed in relation to steric and other considerations. 相似文献