Raltegravir is the first approved integrase inhibitor for the treatment of HIV.The rapid mutation of the virus has led to chemo-resistant strains and there is a medical need to develop new drugs to ov
Fibrosis is a pathological process in damaged tissues or organs where fibroblasts are activated to produce and deposit excess extracellular matrix.Accumulating evidence indicate that complicated proce
3-Alkyloxybenzamide derivatives as FtsZ inhibitors exhibited greatly improved on-target activity and antibacterial activity against penicillin-susceptible and-resistant S.aureus,and methicillin-resist
Despite continuous and intensive efforts to discover highly effective cancer drugs,conventional chemotherapeutic agents still exhibit poor specificity in reaching tumor tissue and are often restricted
本课题组的前期工作[1-2]表明含有长碳链的大黄素季铵盐在体内和体外都具有良好的抗癌活性.在此基础上,本文进行了如下工作.(1)继续对大黄素长碳链季铵盐的烃基结构进行优化,筛选得到了图1所示大黄素衍生物1,其抗癌活性(1.75μM,24h)和选择性均优于本课题组前期报道过的大黄素单季铵盐衍生物;(2)合成了2类大黄素双季铵盐衍生物,结构如图1中2和3所示,但它们的活性均没有超过1,原因可能是大黄素
Glucosidase is a promising target for treatment of obesity and diabetes mellitus.A series of oleanolic acid derivatives-chalcones conjugates were designed and synthesized as α-glucosidase inhibitors.T
通过体外实验与分子动力学模拟实验(in silico)相结合,研究了多聚没食子酸类化合物(pGG)抑制流感病毒血凝素(HA)的分子机制。体外实验发现pGG类星状分子通过与HA的受体结合域的保守区结合抑制HA的活性,其抑制作用与没食子酸取代基的数目正相关。原子力显微镜、电镜、非变性电泳实验、以及理论计算证实:形如pGG类的星状化合物可以将病毒颗粒胶粘起来,从而阻止病毒对宿主细胞的入侵,并有助于宿主消
A series of novel biphenyl urea derivates were synthesized and investigated for their potential to inhibit vascular endothelial growth factor receptor-2(VEGFR-2).In particular,A7,B3 and B4 displayed s
选择性差,毒副作用大仍是目前绝大多数抗肿瘤化学治疗药物的主要缺点。能够选择性的抑制或杀死肿瘤细胞一直是抗肿瘤化疗药物研发的首要目标。传统的叶酸拮抗剂如甲氨蝶呤和培美曲塞作为抗肿瘤化疗药物,在临床上已经取得了巨大成功,但仍具有选择性差、毒副作用大的缺陷。研究表明还原叶酸转运蛋白(Reduced Folate Carrier,RFC),叶酸受体(Folate Receptors,FR)和质子偶联叶酸转