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参考文献:设计,合成和生物学评估带有1,2,3-三唑部分的新型尿嘧啶衍生物作为胸苷酸合酶(ts)抑制剂和潜在的抗肿瘤药物
标题:设计,合成和生物学评估带有1,2,3-三唑部分的新型尿嘧啶衍生物作为胸苷酸合酶(ts)抑制剂和潜在的抗肿瘤药物
摘要:胸苷酸合酶抑制剂的研究一直是抗癌药物开发的热点.在此,根据两种ts抑制剂的结构和药理特性,通过药物设计的分子组装原理,我们设计合成了30种新颖的尿嘧啶衍生物作为ts抑制剂.通过mtt分析评估了这些化合物对四种癌细胞系(a549,Ovcar-3,Sgc-7901和hepg2)的抗增殖能力.它们中的大多数对所有测试的细胞系均表现出优异的活性.此外,Hts分析结果表明,这些化合物具有独特的体外抑制hts活性的能力.值得注意的是,化合物13J对a549细胞表现出最强的活性(ic 50 = 1.18μm)和极显着的酶抑制(ic 50 = 0.13μm),优于培美曲塞(ptx,Ic 50 = 3.29μm和ic 50 = 2.04μm).流式细胞仪分析表明,化合物13J可以通过将细胞周期阻滞在g1 / S期来抑制a549细胞的增殖,进而诱导细胞凋亡.进一步的蛋白质印迹分析表明化合物13J可能下调周期检查点蛋白cyclin
Doi:10.1016/j.Ejmech.2019.03.047

专利信息

专利号:US-8618281-B2
优先权日:2006-01-03
标 题 :Geometric synthesis of porphyrin rods
发明人：LINDSEY JONATHAN S; YU LIANHE; THAMYONGKIT PATCHANITA; BHISE ANIL D
权利人:LINDSEY JONATHAN S; YU LIANHE; THAMYONGKIT PATCHANITA; BHISE ANIL D; UNIV NORTH CAROLINA STATE
摘要:A method of making a compound of Formula I′ n ncomprises reacting a compound of the formula DLCHO, with a compound of the formulan n nto produce the compound of Formula I′. Methods of using the compounds are also described, particularly as intermediates for the synthesis of porphyrin rods, which porphyrin rods are in turn useful for (among other things) the production of molecular memory devices.

专利号:US-10919904-B2
优先权日:2016-08-17
标 题 :Northern-southern route to synthesis of bacteriochlorins
发明人：LIU YIZHOU; LINDSEY JONATHAN S; ALLU SRINIVASA RAO; FUJITA HIKARU
权利人:UNIV NORTH CAROLINA STATE
摘要:Described herein are chlorins, bacteriochlorins, methods and intermediates for the synthesis of bacteriochlorins, and methods of using such bacteriochlorins for, among other things, diagnostic and therapeutic purposes such as luminescent compounds in flow cytometry, and as active agents in photodynamic therapy (PDT).

专利号:US-6916982-B2
优先权日:2000-07-21
标题:Synthesis of perylene-porphyrin building blocks and polymers thereof for the production of light-harvesting arrays
发明人：LOEWE ROBERT S; TOMIZAKI KIN-YA; LINDSEY JONATHAN S
权利人:UNIV NORTH CAROLINA STATE
摘要:The present invention provides methods, compounds, and compositions for the synthesis of light harvesting arrays, such arrays comprising: (a) a first substrate comprising a first electrode; and (b) a layer of light harvesting rods electrically coupled to said first electrode, each of said light harvesting rods comprising a polymer of Formula I:n nX 1 X m+1 ) m   (I)n nwherein m is at least 1; X 1 is a charge separation group, and X 2 through X m+1 are chromophores. At least one of X 2 through X m+1 has at least one perylene group coupled thereto.

专利号:US-2017101698-A1
优先权日:2015-10-13
标 题:Functionalized Adsorbents for the Recovery of Rare Earth Elements from Aqueous Media
发明人：Karamalidis Athanasios; WASHBURN NEWELL R; NOACK CLINTON W; PERKINS KEDAR; DZOMBAK DAVID A
权利人:CARNEGIE MELLON UNIV A PENNSYLVANIA NON-PROFIT CORP
摘要:The disclosure relates to the design and synthesis of selected ligands, dendrimers, polymers and other solid phase substrates for selective chelation of rare earth elements (i.e. lanthanides), and use of those selective ligands for synthesis of resins, polymers and other types of solid supports for separation and recovery of lanthanides from aqueous media. Recovery of critical elements from aqueous media occurs in a simple two-step process: pre-concentration of REE on the adsorbent and recovery by acid elution. The present invention can be used for design of selective ligands immobilized on solid substrates for extraction of various constituents, such as lanthanides, actinides, radionuclides, trace metals, etc., from aqueous media.

专利号:US-2022356182-A1
优先权日:2009-03-27
标题 :Inhibitors of hepatitis c virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-7741475-B2
优先权日:2006-02-13
标题:Synthesis of monovalent and polyvalent arabinans and mannose-capped arabinans of the protective cell-wall coat of mycobacterium tuberculosis
发明人：FRASER-REID BERTRAM; LU JUN
权利人:NATURAL PRODUCTS & GLYCOTECHNO
摘要:The present application provides arabinans and mannose-capped arabinan compositions of formulas I-VIII, described herein, and methods of making the compositions.