喹唑啉

the target compounds synthesized to synthesize a series after 4 - instead of aniline - 6 -(2 - hydroxyl replace c oxygen radicals) quinazoline compounds has laid a good foundation.

目标化合物的顺利合成为以后合成一系列4-取代苯胺-6-(2-羟基取代丙氧基)喹唑啉类化合物奠定了良好的基础。

The goal of the successful synthesis of compounds for the subsequent synthesis of a series of 4 - to replace the aniline -6 -(2 - hydroxy replace C oxy) quinazoline compounds laid a good foundation.

目标化合物的顺利合成为以后合成一系列4-取代苯胺-6-(2-羟基取代丙氧基)喹唑啉类化合物奠定了良好的基础。

3D-QSAR studies for one large set of quinazoline type epidermal growth factor receptor inhibitors were conducted using two types of molecular field analysis techniques: comparative molecular field analysis and comparative molecular similarity indices analysis .

采用了CoMFA和CoMSIA方法，进行了几类4-苯胺喹唑啉类抑制剂的三维定量构效关系的研究。

Special attention was directed toward finding inhibitors selective against KDR tyrosine kinase in order to ensure that the in vivo profile of a specific Src inhibitor could be determined. The 4-aminobenzodioxole quinazoline series gave compounds with excellent potency and selectivity.

一直以来，人们为了确保能够在体内测定Src酶专属性抑制剂的特性，把研究焦点放在对KDR酪氨酸激酶选择性的抑制剂的寻找上。4-氨基苯并间二氧五环喹唑啉系列化合物具有极好的效力和选择性。

The five quinazoline compounds were prepared by using 2????amino????4,5????dimethoxy benzoic acid as original material, which underwent ring????

我们改进了这种化合物的合成方法，用简单省时的SOCl2回流法合成五种喹唑啉类EGFR？？？？

It has been demonstrated that the methods are successfully used for QSRR studies of quinazoline derivatives, alkypyridine, haloid alkane, ketone, alcohol, sulfur alcohol compounds.

本文成功地用该方法对喹唑啉类、烷基吡啶化合物、卤代烃、醇、羰基化合物和硫醇化合物的结构保留关系进行了探讨。

From the calculations, it can be found that the van der Waals interactions, the hydrophobic interactions, as well as the H-bonding interactions are crucial for the ligand binding. The 4-phenylamino group can produce strong van der Waals adn hydrophobic interactions with the nonpolar side chains of the residues deep in the binding cleft. The R^1 and R^2 substituents on the bicyclic chromophore can also produce strong van der Waals and hydrophobic interactions with the residues located at the exterior part of the binding pocket. Moreover, the two N atoms of the quinazoline can form H-bonds with EGFR, which will produce significant contribution to biological activities. The calculated nonbonded interactions between anilinoquinazolines and EGFR, as well as the information obtained from the predicted complexes, can interpret the structure-activities of the inhibitors well, which can afford us important information for structure-based drug design.

从模拟结果得到的抑制剂和靶酶之间的相互作用模式表明范德华相互作用、疏水相互作用以及氢键相互作用对抑制剂的活性都有重要的影响，抑制剂的苯胺部分位于活性口袋的底部，能够与受体残基的非极性侧链产生很强的范德华和疏水相互作用，抑制剂双环上的取代基团也能和活性口袋外部的部分残基形成一定的范德华和疏水性相互作用，而抑制剂喹唑啉环上的氮原子能和周围的残基形成较强的氢键相互作用，对抑制剂的活性有较大的影响，计算得到抑制剂和靶酶之间的非键相互作用能以及抑制剂和靶酶之间的相互作用信息能够很好地解释抑制剂活性和结构的关系，为全新抑制剂的设计提供了重要的结构信息。

Ciardiello and colleagues tested ZD1839, a quinazoline derivative, in combination with cytotoxic agents that had differing mechanisms of action (cisplatin, carboplatin, oxaliplatin, paclitaxel, Taxotere, doxorubicin, etoposide, topotecan, and tomudex).

Ciardiello及其同事试验了将一种喹唑啉衍生物ZD1839与作用机制不同的细胞毒素药物（顺铂、卡铂、奥沙利铂、紫杉醇、泰索帝、阿霉素、依托泊甙、拓扑特肯等）合用。

Object: A specific and sensitive liquid chromatography tandem mass spectrometry method was developed for the multiresidue determination of sulfisomidine, sulfapyridine, sulfamerazine, sulfamethoxazole, sulfisoxazole, sulfadiazine, sulfamethizole, sulfachlorpyridazine, sulfamethoxypyridazine, sulfadimethoxine, sulfamonomethoxine, sulfathiazole, sulfadoxine, sulfaquinoxaline, sulfanilamide, sulfaguanidine, sulfamoxole, sulfameter, sulfadimidine, sulfacetamide, sulfaphenazole, sulfanitran, sulfabenzamide and a potentiator, trimethoprim, in meat.

目的：建立猪肉中磺胺及其增效剂多残留检测的液相色谱-串联质谱法，包括磺胺二甲异嘧啶、磺胺吡啶、磺胺甲基嘧啶、磺胺甲基异噁唑、磺胺二甲异噁唑、磺胺嘧啶、磺胺甲噻二唑、磺胺氯哒嗪、磺胺甲氧哒嗪、磺胺间二甲氧嘧啶、磺胺-6-甲氧嘧啶、磺胺噻唑、磺胺邻二甲氧嘧啶、磺胺喹噁啉、磺胺、磺胺脒、磺胺噁唑、磺胺甲氧嘧啶、磺胺二甲嘧啶、磺胺醋酰、磺胺苯吡唑、磺胺硝苯、磺胺苯酰和甲氧苄氨嘧啶。

ZD1839 and OSI-774 are 4-anilinoquinazoline selective inhibitors of tyrosine kinase of EGFR,which are currently in Pase III and Phase II development,respectively.

ZDl839和OSI-774是4-笨胺基喹唑啉类选择性的EGFR酪氨酸激酶抑制剂，目前它们正分别进行Ⅲ期及Ⅱ期临床研究。

The split between the two groups can hardly be papered over.

这两个团体间的分歧难以掩饰。

This approach not only encourages a greater number of responses, but minimizes the likelihood of stale groupthink.

这种做法不仅鼓励了更多的反应，而且减少跟风的可能性。