Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors

机译：发现新型槲皮素-3-O-氨基酸酯作为一类新的Src酪氨酸激酶抑制剂

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Quercetin-3-O-amino acid-esters, a new type of quercetin derivatives, were successfully prepared for the first time. Different from quercetin, the novel compounds show higher selectivity as inhibitors against Src tyrosine kinase (IC50 values ranging from 3.2 μM to 9.9 μM) than against EGFR tyrosine kinase. Molecular docking reveals that both hydrophobic and hydrogen bonding interactions are important to the selectivity. Therefore, this study provides a new promising scaffold for further development of new anticancer drugs targeting Src tyrosine kinase.

机译：槲皮素-3-O-氨基酸酯，一种新型槲皮素衍生物，首次成功制备。与槲皮素不同，该新型化合物对Src酪氨酸激酶的抑制剂（IC50值范围从3.2μM至9.9μM）显示出比对EGFR酪氨酸激酶更高的选择性。分子对接揭示了疏水键和氢键相互作用都对选择性很重要。因此，该研究为靶向Src酪氨酸激酶的新抗癌药物的进一步开发提供了新的有希望的支架。

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《ICMSI;International conference of molecular simulations and applied informatics technologies》|2010年|p.711-717|共7页
会议地点 Wuhan(CN);Wuhan(CN)
作者
He Huang; Hualiang Jiang; Hong Liu; Qi Jia; Jingui Ma; Guangrong Qin; Yingyi Chen; Yonghua Xi; Liping Lin; Weiliang Zhu; Jian Ding;
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Shanghai Institute of Materia Medico Chinese Academy of Sciences 555 Zuchongzhi Road Shanghai 201203 China;

School of Chinese Medicine Shanghai University of Traditional Chinese Medicine 201203 China;

School of Chinese Medicine Shanghai University of Trad;

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Quercetin; Amino acid; Src; EGFR; Inhibitor;

机译：槲皮素氨基酸; Src;表皮生长因子缓蚀剂;

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专利

1. Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors. [J] . Huang H, Jia Q, Ma J, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2009,第5期

机译：发现新型槲皮素-3-O-氨基酸酯作为一类新的Src酪氨酸激酶抑制剂。
2. Salicylate Inhibits Phosphorylation of the Nonreceptor Tyrosine Kinases, Proline-Rich Tyrosine Kinase 2 and c-Src. [J] . Wang Z, Brecher P Hypertension: An Official Journal of the American Heart Association . 2001,第1期

机译：水杨酸盐抑制非受体酪氨酸激酶，脯氨酸丰富的酪氨酸激酶2和c-Src的磷酸化。
3. Debio 0617B Inhibits Growth of STAT3-Driven Solid Tumors through Combined Inhibition of JAK, SRC, and Class III/V Receptor Tyrosine Kinases [J] . Murone Maximilien, Chessex Anne Vaslin, Attinger Antoine, Molecular cancer therapeutics . 2016,第10期

机译：Debio 0617B通过联合抑制JAK，SRC和III / V类酪氨酸激酶来抑制STAT3驱动的实体瘤的生长
4. Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors [C] . He Huang, Hualiang Jiang, Hong Liu, International conference of molecular simulations and applied informatics technologies . 2010

机译：发现新型槲皮素-3-O-氨基酸酯作为新一类SRC酪氨酸激酶抑制剂
5. Analysis of pp60c-src and pp62c-yes intracellular protein tyrosine kinase function in colon tumor cell growth regulation using herbimycin A, a tyrosine kinase specific inhibitor. [D] . Garcia, Roy. 1995

机译：使用酪氨酸激酶特异性抑制剂除草霉素A分析pp60c-src和pp62c-yes细胞内蛋白酪氨酸激酶在结肠肿瘤细胞生长调节中的功能。
6. Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors [O] . He Huang, Qi Jia, Jingui Ma, -1

机译：发现新型槲皮素-3-O-氨基酸酯作为一类新的Src酪氨酸激酶抑制剂
7. C-terminal Src kinase-homologous kinase (CHK), a unique inhibitor inactivating multiple active conformations of Src family tyrosine kinases. [O] . Yuh-Ping Chong, Andrew S. Chan, Khai-Chew Chan, 2015

机译：C-末端SRC激酶 - 同源激酶（CHK），独特的抑制剂灭活SRC家族酪氨酸激酶的多重活性构象。

Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors

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