CAS: 150943-50-3; 4-Chloro-5-Nitropyrimidine

上下游产品

CAS号3749-47-1 5-硝基-(8ci)-4(3H)-嘧啶酮

📜5-硝基-(8Ci)-4(3H)-嘧啶酮置于n,N-二异丙基乙胺,三氯氧磷体系中,化学反应 0.5H,反应生成4-氯-5-硝基嘧啶
参考文献:Synthesis And Characterization Of Novel Pyrimidine-4,5-Diamine As Anticancer Agent
标题:Synthesis And Characterization Of Novel Pyrimidine-4,5-Diamine As Anticancer Agent
摘要:与潜在细胞不同,癌细胞持续向细胞供应脱氧核苷三磷酸,从而支持不受控制的癌症生长.嘧啶已被认为在分离白血病细胞(称为腺嘌呤生物同源体)以及其生物活性,特别是其抗癌特性方面起作用.在这种情况下,通过使用起始成分甲酰胺基/4-(二甲氨基)苯并咪唑和乙醇钠,合成了一系列新型n5-(3-取代苄基亚甲基)-N4-苯基嘧啶-4,5-二胺[5A-5F] / N5-(2-取代苄基亚甲基)-N2,N2-二甲基-N4-苯基嘧啶-2,4,5-三胺[5A-5F].合成化合物通过红外光谱,1H核磁共振和质谱分析进行表征,并进行了生物研究筛选.在本研究中,通过使用c-Src激酶和p38 Map激酶复合物进行嘧啶衍生物及其分子模拟,然后评估其抗癌活性.合成支架的筛选对hela细胞系表现出显着活性,并显示出与标准顺铂相似的活性.在所有合成化合物中,N5-(4-羟基苄亚甲基)-N4-苯基嘧啶-4,5-二胺 5A,N5-苄亚甲基-N4-苯基嘧啶-4,5-二胺 5C,N5-苄亚甲基-N2,N2-二甲基-N4-苯基嘧啶-2,4,5-三胺 5C和n5-(4-甲氧基苄亚甲基)-N4-苯基嘧啶-4,5-二胺 5E显示出最显著的抗癌活性.根据研究,观测到4-羟基,4-氟基,4-硝基,4-甲氧基和4-甲基等取代基对产生生物效应很重要.此外,在这些取代基中,N5-(4-羟基苄亚甲基)-N4-苯基嘧啶-4,5-二胺表现出最高的抗癌活性,其次是未取代的衍生物n5-苄亚甲基-N4-苯基嘧啶-4,5-二胺,其具有显著的抗癌活性.
Doi:10.26452/ijrps.V11I3.2649

专利信息

专利号:US-5350851-A
优先权日:1992-03-16
标题 :Intermediates and a process for synthesis of tetrahydropteridine C6-stereoisomers, including (6S)-tetrahydrofolate and N5-formyl-(6S)-tetrahydrofolate
发明人：BAILEY STEVEN W; AYLING JUNE E
权利人:UNIV SOUTH ALABAMA
摘要:Intermediates and a process for the synthesis of 6-monosubstituted tetrahydropteridine C6-stereoisomers, including (6S)-tetrahydrofolic acid. The intermediates are shown in their two enantiomeric forms as follows: ##STR1## wherein R 1 and R 2 are the same or different and represent hydrogen, methyl, hydroxy, amino, alkyl or dialkylamino, alkoxy, benzyloxy, or benzylthio; R 3 represents an alkene, alkyne, cycloalkyl, benzyl, alkyl (substituted with hydroxy, acetoxy, benzyloxy, alkoxy, alkylthio, amino, carboxy, oxo, or phosphate), a protected aldehyde, or ##STR2## wherein n=1 or 2, R 4 is hydrogen, formyl, methyl, or propargyl, and ZZ represents an amino acid or amino acid polymer.

专利号:US-8362019-B2
优先权日:2008-02-01
标 题:Synthesis and anti-proliferative effect of substituted imidazo[4,5-b]pyrazine compounds
发明人：WINFIELD LEYTE L
权利人:SPELMAN COLLEGE; WINFIELD LEYTE L
摘要:This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. In particular, the disclosure provides for substituted imidazo[4,5-b]pyrazine compounds having the general formula n ntheir salts, pharmaceutical compositions, and methods of treatment using the subject compounds and compositions.

专利号:WO-9319069-A1
优先权日:1992-03-16
标题:Intermediates and a process for synthesis of tetrahydropteridine c6-stereoisomers, including (6s)-tetrahydrofolate and n5-formyl-(6s)-tetrhydrofolate

专利号:EP-0631581-A1
优先权日:1992-03-16
标题 :Intermediates and a process for synthesis of tetrahydropteridine c6-stereoisomers, including (6s)-tetrahydrofolate and n5-formyl-(6s)-tetrhydrofolate

专利号:AU-3804193-A
优先权日:1992-03-16
标 题:Intermediates and a process for synthesis of tetrahydropteridine C6-stereoisomers, including (6S)-tetrahydrofolate and N5-formyl-(6S)-tetrhydrofolate

专利号:US-2012095038-A1
优先权日:2008-02-01
标 题:Synthesis and anti-proliferative effect of benzimidazole derivatives