将2-氨基-8-羟基喹啉作为热点化合物进行进一步的结构修饰及合成。合成了一系列新的具有2-氨基-8-羟基喹啉结构的双芳基二氨基类化合物。新的化合物进行了thermal shift,细胞及酶水平的抗锥虫病的活性研究。所有衍生物都对布鲁斯锥虫具有较高的活性,活性范围在7000-900nM。其中活性最好的{Selleck Anti-infection Compound Library|Selleck Antiinfection Compound Library|Selleck Anti-infection Compound Library|Selleck Antiinfection Compound Library|selleck Anti-infection Compound Library|selleck Antiinfection Compound Library|selleck Anti-infection Compound Library|selleck Antiinfection Compound Library|Anti-infection Compound Library|Antiinfection Compound Library|Anti-infection Compound Library|Antiinfection Compound Library|Anti-infection Compound Library|Antiinfection Compound Library|Anti-infection Compound Library|Antiinfection Compound Library|Anti-infection Compound Library|Antiinfection Compound Library|Anti-infection Compound Library|Antiinfection Compound Library|Anti-infection Compound Library|Antiinfection Compound Library|Anti-infection Compound Library|Antiinfection Compound Library|Anti-infection Compound Library|Antiinfection Compound Library|buy Anti-infection Compound Library|Anti-infection Compound Library半抑制浓度|Anti-infection Compound Library价格|Anti-infection Compound Library花费|Anti-infection Compound Library溶解度|Anti-infection Compound Library购买|Anti-infection Compound Library制造商|Anti-infection Compound Library查找购买|Anti-infection Compound Library订单|Anti-infection Compound Library mouse|Anti-infection Compound Library chemical structure|Anti-infection Compound Library分子量|Anti-infection Compound Library molecular weight|Anti-infection Compound Library数据表|Anti-infection Compound Library supplier|Anti-infection Compound Library体外|Anti-infection Compound Library细胞系|Anti-infection Compound Library concentration|Anti-infection Compound Library nmr|Anti-infection Compound Library体内|Anti-infection Compound Library clinical trial|Anti-infection Compound Library cell assay|Anti-infection Compound Library screening|Anti-infection Compound Library high throughput|buy Antiinfection Compound Library|Antiinfection Compound Library半抑制浓度|Antiinfection Compound Library价格|Antiinfection Compound Library花费|Antiinfection Compound Library溶解度|Antiinfection Compound Library购买|Antiinfection Compound Library制造商|Antiinfection Compound Library查找购买|Antiinfection Compound Library订单|Antiinfection Compound Library chemical structure|Antiinfection Compound Library数据表|Antiinfection Compound Library supplier|Antiinfection Compound Library体外|Antiinfection Compound Library细胞系|Antiinfection Compound Library concentration|Antiinfection Compound Library clinical trial|Antiinfection Compound Library cell assay|Antiinfection Compound Library screening|Antiinfection Compound Library high throughput|Anti-infection Compound high throughput screening|为4b,EC50为900nM。选取了thermal shift活性最佳的化合物进行了抗甲硫氨酰-tRNA合成酶的活性测试,显示出了一定的甲硫氨酰-tRNA合成酶抑制活性,证明此系列的化合物作用于甲硫氨酰-tRNA合成酶。结合化合物在thermal shift测试中ATm有大selleck抑制剂的变化(ΔTms,9.5,8.6℃),也可以证明化合物作用的靶点为甲硫氨酰-tRNA合成酶。同时我们也进行了计算机分子模拟的研究。总之,我们应用基于分子片段的药物设计方法,应用thermal shift,发现了一类新的作用于甲硫氨酰-tRNA合成酶的结构骨架,具有进一步研究Apoptosis抑制剂与开发价值。本研究也为发现新的安全有效的治疗人类非洲锥虫病的药物开辟了新的道路。
乳腺癌是妇女中最常见的恶性肿瘤之一。早期的乳腺癌病人大约有60%为ERa阳性,ERα阳性的病例有着较好的预后并对内分泌(如他莫昔芬等)治疗有着良好的反应。然而,尽管近十几年来,他莫昔芬已成为治疗ERα阳性乳腺癌患者的金标准,但仍有部分ERα阳性的患者对内分泌治疗产生耐药性。