越来越多的研究表明，内源性的H2S在很多人体器官和组织发挥重要的生理功能，包括心血管、神经、消化、血液、内分泌和免疫等多种人体机能系统.在结肠癌、唐氏综合症、低血压、高血压和胰腺炎等很多病理条件下，内源性H2S含量都发现有异常变化.Cystathionine β-synthase(CBS)和cystathionine γ-lyase(CSE)是产生H2S的关键酶，因此寻找这两个酶的抑制剂或激活剂被
Kinases play pivotal role play pivotal roles in virtually all aspects of cellular physiology1.Potent and selective kinase inhibitors are highly desirable,both as tool compounds for dissecting complex
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