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Design Synthesis and Anti-Proliferative Activities of 26-Substituted Thieno32-dpyrimidine Derivatives Containing Electrophilic Warheads

机译：含有亲电子战斗部的26-取代的噻吩并32-d嘧啶衍生物的设计合成和抗增殖活性

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Thieno[3,2-d]pyrimidine as an effective pharmacophore has been extensively studied. However, its 2,6-substituted derivatives are rarely reported. In the present study, eighteen 2,6-substituted thieno[3,2-d]pyrimidine derivatives containing electrophilic warheads were designed based on the first known Fibroblast growth factor receptor-4 (FGFR4) inhibitor Blu9931. Unexpectedly, all of the derivatives exhibited negligible activity against FGFR4. However, most of the target compounds exhibited antiproliferative activities against four human cancer cell lines, including A431, NCI-H1975, Ramos and SNU-16. Compound >12 showed the most potent antiproliferative activities on the above four cell lines with IC50 values of 1.4 μM, 1.2 μM, 0.6 μM, and 2.6 μM, respectively. Additionally, the antiproliferative activity of >12 against MDA-MB-221 proved that >12 had the selectivity towards certain tumor cell lines. Furthermore, preliminary structure-activity relationship analysis was discussed based on the experimental data.

机译：噻吩并[3,2-d]嘧啶作为一种有效的药效团已被广泛研究。但是，很少报道其2，6-取代的衍生物。在本研究中，基于第一个已知的成纤维细胞生长因子受体4（FGFR4）抑制剂Blu9931设计了18种含有亲电战斗部的2,6-取代的噻吩并[3,2-d]嘧啶衍生物。出乎意料的是，所有衍生物对FGFR4的活性都可忽略不计。但是，大多数目标化合物对四种人类癌细胞系（包括A431，NCI-H1975，Ramos和SNU-16）都具有抗增殖活性。化合物> 12 对上述四种细胞系表现出最强的抗增殖活性，IC50值分别为1.4μM，1.2μM，0.6μM和2.6μM。另外，> 12 对MDA-MB-221的抗增殖活性证明> 12 对某些肿瘤细胞系具有选择性。此外，基于实验数据讨论了初步的构效关系分析。

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期刊名称 Molecules
作者
Qiumeng Zhang; Zonglong Hu; Qianqian Shen; Yi Chen; Wei Lu;
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作者单位

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年(卷),期 2017(22),5
年度 2017
页码 788
总页数 16
原文格式 PDF
正文语种
中图分类分子生物学;
关键词
thieno32-dpyrimidines; antitumor activities; acrylamide warheads;

机译：噻吩并32-d嘧啶;抗肿瘤活性;丙烯酰胺战斗部;

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1. Design, Synthesis and Anti-Proliferative Activities of 2,6-Substituted Thieno[3,2- d ]pyrimidine Derivatives Containing Electrophilic Warheads [J] . Qiumeng Zhang, Zonglong Hu, Qianqian Shen, Molecules . 2017,第5期

机译：含亲电子战斗部的2,6-取代的噻吩并[3,2-d]嘧啶衍生物的设计，合成及抗增殖活性
2. Design, Synthesis and Anti-Proliferative Activities of 2,6-Substituted Thieno[3,2-d]pyrimidine Derivatives Containing Electrophilic Warheads [J] . Qiumeng Zhang, Zonglong Hu, Qianqian Shen, Molecules . 2017,第5期

机译：含有亲电子战斗部的2,6-取代的噻吩并[3,2-d]嘧啶衍生物的设计，合成和抗增殖活性
3. Synthesis of novel 26-substituted milbemycin A4 derivatives and their acaricidal activities. [J] . Tsukiyama T, Kajino H, Tsukamoto Y, The Journal of Antibiotics: An International Journal . 2004,第7期

机译：新型26-取代的米尔倍霉素A4衍生物的合成及其杀螨活性。
4. DESIGN,SYNTHESIS,CHARACTERISATION AND ANTIFUNGAL ACTIVITY OF NOVEL PYRIMIDONE DERIVATIVES [C] . P.Vijaybhanu, D.R.Harish Kumar, L.Ramya Conference on Drug Design and Discovery Technologies . 2020

机译：新型嘧啶衍生物的设计，合成，表征和抗真菌活性
5. Part One. Synthesis of optically active tryptophan derivatives with potential activity as indoleamine 2,3-dioxygenase inhibitors: An approach via asymmetric catalytic hydrogenation. Part Two. Design, synthesis and pharmacology of selective ligands for alpha1-containing GABA(A)/benzodiazepine receptor subtypes: SAR studies of beta-carbolines at positions -3 and -6 and their corresponding bivalent ligands. Part Three. First enantiospecific total synthesis of the important biogenetic intermediates, (+)-polyneuridine and (+)-polyneuridine aldehyde, as well as 16-epi-vellosimine and macusine A. [D] . Yin, Wenyuan. 2007

机译：第一部分。具有吲哚胺2,3-二加氧酶抑制剂潜在活性的旋光色氨酸衍生物的合成：一种通过不对称催化氢化的方法。第二部分。含α1的GABA（A）/苯并二氮杂receptor受体亚型的选择性配体的设计，合成和药理作用：位于-3和-6位的β-咔啉及其相应的二价配体的SAR研究。第三部分。重要生物遗传中间体，（+）-聚神经氨酸和（+）-聚神经氨酸醛，以及16-表-维西辛和Macusine A的首次对映体全合成。
6. Discovery of New Pyrazolopyridine Furopyridine and Pyridine Derivatives as CDK2 Inhibitors: Design Synthesis Docking Studies and Anti-Proliferative Activity [O] . Adel A.-H. Abdel-Rahman, Amira K. F. Shaban, Ibrahim F. Nassar, 2021

机译：发现新的吡唑吡啶呋骨和吡啶衍生物作为CDK2抑制剂：设计合成对接研究和抗增殖活动
7. Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity [O] . Adel A.-H. Abdel-Rahman, Amira K. F. Shaban, Ibrahim F. Nassar, 2021

机译：发现新的吡唑吡啶，呋骨和吡啶衍生物作为CDK2抑制剂：设计，合成，对接研究和抗增殖活动

Design Synthesis and Anti-Proliferative Activities of 26-Substituted Thieno32-dpyrimidine Derivatives Containing Electrophilic Warheads

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