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Garbapu Suresh Ratnakaram Venkata Nadh Navuluri Srinivasu Durgaprasad Yennity 《合成通讯》2017,47(17):1610-1621
A new and efficient synthetic route for dual-Src/Abl kinase inhibitor dasatinib (Sprycel®), an anticancer drug, is described. This commercially viable process yields dasatinib monohydrate free of potential impurities with consistent yield of 68% in route A and 61% in route B with HPLC purity >99.80% over four stages. 相似文献
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Oite T 《Proceedings of the Japan Academy. Series B, Physical and biological sciences》2011,87(3):81-90
In this review, I introduce the strategy developed by our laboratory to explore the mechanisms of renoprotection against progressive glomerulosclerosis leading to renal death. First, I describe the experimental rat model in which disturbances of vascular regeneration and glomerular hemodynamics lead to irreversible glomerulosclerosis. Second, I discuss the possible mechanisms determining the progression of glomerulosclerosis and introduce a new imaging system based on intravital confocal laser scanning microscopy. Third, I provide an in-depth review of the regulatory glomerular hemodynamics at the cellular and molecular levels while focusing on the pivotal role of Ca(2+)-dependent gap junctional intercellular communication in coordinating the behavior of mesangial cells. Last, I show that local delivery of renoprotective agents, in combination with diagnostic imaging of the renal microvasculature, allows the evaluation of the therapeutic effects of angiotensin II receptor and cyclooxygenase activity local blockade on the progression of glomerulosclerosis, which would otherwise lead to renal death. 相似文献
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Marisa Freitas 《Analytica chimica acta》2009,649(1):8-8272
Neutrophils, also known as polymorphonuclear leukocytes (PMN), are the most common type of white blood cells, comprising about 50-70% of all white blood cells. In the event of inflammatory processes, neutrophils display increased mobility, tissue influx ability, prolonged life span, and an increased phagocytic capacity, constituting the initial participants in the cellular defense of the organism. One of the most important defense systems of neutrophils corresponds to their ability to mediate a strong oxidative burst through the formation of reactive oxygen species (ROS) and reactive nitrogen species (RNS). While oxidative burst is important for the elimination of invading microorganisms, the overproduction of ROS and RNS or the impairment of endogenous antioxidant defenses may result to detrimental effects to the host. The nature and the extent of ROS and RNS production by neutrophils in response to different stimuli is, consequently, a matter of extensive research, with scientific reports showing an enormous variability on the detection methodologies employed. This review attempts to provide a critical assessment of the most common approaches to identify and quantify reactive species formed during the neutrophils’ oxidative burst. The detection mechanisms and performance, as well as advantages and limitations of the different methodologies, are scrutinized, focusing on the use of fluorimetric, chemiluminometric and colorimetric probes. 相似文献
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慢性肾衰肾虚证患者血清微量元素的变化及其临床意义探讨 总被引:4,自引:0,他引:4
讨论了慢性肾衰肾阳虚和肾阴虚见证者血清微量元素。结果显示:肾阳虚患者血清Cu、Cu/Zn明显高于健康对照组,而血清Zn和Fe低于对照组,肾阳虚患者血清Cu、Cu/Zn也明显高于肾阴虚组,而血清Zn是低的,在肾阴虚组与对照组之间Cu、Zn、Cu/Zn均无明显差异。 相似文献
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ZOU DingBiao QIU YaTao TU ZhengChao LIAO ChenZhong LUO JinFeng MENG QingQing YAO RiSheng LI Zheng JIANG Sheng 《中国科学:化学(英文版)》2014,57(6):823-832
We designed a series of 2-methylpyrimidine derivatives as new BCR-ABL inhibitors using scaffold-hopping strategy.These synthetic compounds exhibited significant inhibition against a broad spectrum of Bcr-Abl mutants including the gatekeeper T315I mutant.Compound 7u showed very potent kinase inhibitory activities against Bcr-Abl WT,Bcr-Abl E255K,Bcr-Abl Q252H,Bcr-Abl G250E and Bcr-Abl T315I,with IC50 values of 0.13 nM,0.17 nM,0.24 nM,0.19 nM and 0.65μM,respectively.This compound also displayed anti-proliferation activity against K562 cell line with an IC50 value of 1.1 nM,thus representing a new lead for further optimization. 相似文献
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微量元素硒的抗癌作用 总被引:1,自引:0,他引:1
对硒在恶性肿瘤的防治及其作用机理进行了总结和讨论,硒通过调节机体免疫功能、介入致癌物的代谢、抑制癌细胞生长及抗过氧化作用等发挥防癌和抗癌功能。另外,硒对白血病的治疗引起了人们的重视。 相似文献