Synthesis of 1-(2-chloro-2-phenylethyl)-6-methylthio-1H-pyrazolo(3,4-d)pyrimidines 4-amino substituted and their biological evaluation.

Schenone S; Bruno O; Bondavalli F; Ranise A; Mosti L; Menozzi G; Fossa P; Manetti F; Morbidelli L; Trincavelli L; Martini C; Lucacchini A

首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis of 1-(2-chloro-2-phenylethyl)-6-methylthio-1H-pyrazolo(3,4-d)pyrimidines 4-amino substituted and their biological evaluation.

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Synthesis of 1-(2-chloro-2-phenylethyl)-6-methylthio-1H-pyrazolo(3,4-d)pyrimidines 4-amino substituted and their biological evaluation.

机译：1-（2-氯-2-苯基乙基）-6-甲硫基-1H-吡唑并（3,4-d）嘧啶4-氨基取代基的合成及其生物学评价。

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A new series of 4-amino-6-methylthio-1H-pyrazolo[3,4-d]pyrimidines (2a-m) bearing the 2-chloro-2-phenylethyl chain at the N1 position, has been synthesized. The affinity of these compounds for A1 adenosine receptor (A1AR) was measured. The compounds showed poor affinity. A more interesting result was obtained by 2a, 2d, 2g, which demonstrated inhibitory activity on cell proliferation of the A-431 cell line stimulated by epithelial growth factor (EGF) and on EGF receptor tyrosine kinase (EGFR-TK) phosphorylation.

机译：合成了一系列新的4-氨基-6-甲硫基-1H-吡唑并[3,4-d]嘧啶（2a-m），在N1位带有2-氯-2-苯乙基链。测量了这些化合物对A1腺苷受体（A1AR）的亲和力。化合物显示出较差的亲和力。通过2a，2d，2g获得了更有趣的结果，该结果显示了对上皮生长因子（EGF）刺激的A-431细胞系的细胞增殖和EGF受体酪氨酸激酶（EGFR-TK）磷酸化的抑制活性。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2004年第2期|共8页
作者
Schenone S; Bruno O; Bondavalli F; Ranise A; Mosti L; Menozzi G; Fossa P; Manetti F; Morbidelli L; Trincavelli L; Martini C; Lucacchini A;
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正文语种 eng
中图分类基础医学;
关键词
Pyrimidines; Synthesis; 2a; Epidermal Growth Factor; 嘧啶类;

机译：Pyrimidines;Synthesis;2a;Epidermal Growth Factor;嘧啶类;

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1. Synthesis of 1-(2-chloro-2-phenylethyl)-6-methylthio-1H-pyrazolo(3,4-d)pyrimidines 4-amino substituted and their biological evaluation. [J] . Schenone S, Bruno O, Bondavalli F, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2004,第2期

机译：1-（2-氯-2-苯基乙基）-6-甲硫基-1H-吡唑并（3,4-d）嘧啶4-氨基取代基的合成及其生物学评价。
2. Synthesis and biological activity of 4-substituted 1-(1-(2-hydroxyethoxy)-methyl-1,2,3-triazol-(4 & 5)-ylmethyl)-1H-pyrazolo(3,4-d)pyrimidines. [J] . Moukha Chafiq O, Taha ML, Lazrek HB, Nucleosides, nucleotides and nucleic acids . 2001,第10a11期

机译：4-取代的1-（1-（1-（2-羟基乙氧基）-甲基-1,2,3-三唑-（4和5）-基甲基）-1H-吡唑并（3,4-d）嘧啶的合成及生物活性。
3. A SHORT SYNTHESIS OF 4-SUBSTITUTED 1-(HYDROXYALKYL)-1H-PYRAZOLO[3,4-D]PYRIMIDINES [J] . Zacharie B., Rej R., Attardo G., Tetrahedron . 1996,第7期

机译：短合成4-取代的1-（羟基烷基）-1H-吡唑并[3,4-D]嘧啶
4. Synthesis and Biological study of 2-( 5-aryl-4,5-dihydro-1-substituted-pyrazol-3-yl )-substituted-naphthalene-1 -ol [C] . SUBODH BHANDARKAR, BHAVANA KHOBRAGADE International Conference on Advanced Materials Development Performance . 2015

机译：2-（5-芳基-4,5-二氢-1-取代-Pyrazol-3-基-1- 1-醇的合成与生物学研究 - 萘-1- 1-ol
5. Classical antifolates: Synthesis of 5-substituted, 6-substituted and 7-substituted pyrrolo[2,3-d]pyrimidines as targeted anticancer therapies [D] . Wang, Yiqiang 2013

机译：经典抗叶酸药物：5取代，6取代和7取代的吡咯并[2,3-d]嘧啶的合成作为靶向抗癌药物
6. Design synthesis molecular modelling and biological evaluation of novel substituted pyrimidine derivatives as potential anticancer agents for hepatocellular carcinoma [O] . Naglaa Mohamed Ahmed, Mahmoud Youns, Moustafa Khames Soltan, 2019

机译：新型取代嘧啶衍生物作为肝细胞癌潜在抗癌剂的设计合成分子建模和生物学评估
7. Pyrimidine derivatives and related compounds. XLVI. Thermal and photochemical transformation of 5-substituted 6-azido-1,3-dimethyluracils into fused pyrimidines such as isoxazolo(3,4-d)pyrimidines, pyrazolo(3,4-d)pyrimidines, and pyrimido(4,5-d)(1,2,3)triazine. [O] . KOSAKU HIROTA, KAZUO MARUHASHI, TETSUJI ASAO, 1983

机译：嘧啶衍生物和相关化合物。 XLVI。将5取代的6-氮杂-1,3-二甲基丙酮酸的热和光化学转化变成熔融嘧啶，如异恶唑（3,4-D）嘧啶，吡唑（3,4-D）嘧啶和嘧啶（4,5-D. ）（1,2,3）三嗪。

Synthesis of 1-(2-chloro-2-phenylethyl)-6-methylthio-1H-pyrazolo(3,4-d)pyrimidines 4-amino substituted and their biological evaluation.

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