论文部分内容阅读
Brefeldin A is a secondary metabolite of Ascomycetes species.It was first isolated in 1958 by Singleton from Penicillium decumbens1.
Synthesis of brefeldin A derivatives and their biological evaluation
【摘 要】
：
Brefeldin A is a secondary metabolite of Ascomycetes species.It was first isolated in 1958 by Singleton from Penicillium decumbens1.
【机 构】
：
Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education and School of Tra
【出 处】
：
2015年全国药物化学学术会议暨第五届中英药物化学学术会议
【发表日期】
：
2015年3期
其他文献
化合物N-(2-氯-5-(2-乙酰氨基-6-苯并噻唑基)-3-吡啶基)-4-氟苯磺酰胺(A)具有优异的抗肿瘤活性[1]，但是其毒性较大。
Phosphoinositide 3-kinase delta(PI3Kδ)is an attractive target for the treatment of hematological malignancies and autoimmune diseases.
会议
N-(6-(2-甲氧基-3-(4-氟苯磺酰氨基)-5-吡啶基-2-[1,2,4]三唑[1,5-a]吡啶基乙酰胺(A)具有优异的抗肿瘤活性[1],但是其毒性较大。
3-取代-4-喹唑啉酮易于合成。本课题采用片段互换法，用3-取代-4-喹唑啉酮结构片段替代了PI3K/mTOR 双重抑制剂GSK2126458 结构中的喹啉结构片段，设计、合成了一系列N-(2-甲氧基-5-(3-取代-4-喹唑啉酮-6-基)-3-吡啶基-4-氟苯磺酰胺类化合物，采用1H NMR、13C NMR 和HRMS 表征目标化合物的结构。
二芳基脲是多种药物的药效团结构，叔胺结构的引入可改善药物的药代动力学性质。本课题用二芳基脲的结构片段和叔胺的结构片段替代吉非替尼结构中喹唑啉6 位侧链，设计、合成了一系列1-(4-取代苯基)-3-(4-芳胺基-6-喹唑啉)脲类化合物，采用1H NMR、13C NMR 和HRMS 表征目标化合物的结构。
One-Step Synthesis of Chiral Oxindole-type Analogues with Potent Anti-inflammatory and Analgesic Act
Here we report a facile approach to synthesize highly optically active oxindole-type analogues with both high yield and enantioselectivity in a single step.
利鲁唑是苯并噻唑类衍生物，主要用于治疗侧索硬化症.目前研究集中在谷氨酸调节、神经保护作用、抗抑郁、抗焦虑、治疗癫痫、镇痛等药理作用[1].1963 年利用4-三氟甲氧基苯氨和KSCN 为原料合成利鲁唑[2].
The Bcl-2 protein family works as vital regulators in intrinsic cell death pathway.Myeloid cell leukemia 1(Mcl-1),a prosurvival member of the Bcl-2 protein family,is overexpressed in many tumor types,
In recent years,there are many reports of anticancer activities of artemisinins both in vitro and in vivo[1].Carbonic anhydrase Ⅸ(CA Ⅸ)is a tumor-associated protein[2],it is highly expressed in a mult