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排序方式: 共有364条查询结果,搜索用时 15 毫秒
1.
M. Jonathan Fray Paul Allen Paul R. Bradley Clare E. Challenger Michael Closier Tim J. Evans Mark L. Lewis John P. Mathias Carly L. Nichols Yvonne M. Po-Ba Hayley Snow Mark H. Stefaniak Hannah V. Vuong 《Tetrahedron》2006,62(29):6869-6875
The synthesis of ten substituted aminomethylene tetrahydro-isoquinolines is described, proceeding in eight steps from 5-hydroxyisoquinoline via reductive amination of N-Boc tetrahydro-isoquinoline 5-carboxaldehyde. Likewise, reductive amination was used to prepare four substituted dihydro-isoindoles from the corresponding aldehyde. The dihydro-isoindole ring system was conveniently accessed via a 2+2+2 cycloaddition reaction. 相似文献
2.
Martin Christlieb Hannah J. Claughton Andrew R. Cowley Julia M. Heslop Jonathan R. Dilworth 《Transition Metal Chemistry》2006,31(1):88-92
During the condensation of 4-methyl-4-phenyl-3-thiosemicarbazide (3) with 2,3-butanedione an unexpected by-product, 8a-methyl-6,8a-dihydro-8-methyl-2-[N-methyl-N-phenylamino]-5H-1,3,4-thiadiazolo[3,2-d][1,2,4]triazine-5-thione, (5) was obtained in addition to the desired bis(thiosemicarbazone) (4). An X-ray crystal structure was obtained and is presented together with a proposed mechanism for its formation. A brief investigation
of the coordination chemistry of bicycle (5) was carried out. The formation of cyclic compounds during the synthesis of analogues with extended backbones is also described. 相似文献
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4.
Cancer immunotherapy with immune checkpoint inhibitors (ICIs) has revolutionized the treatment of advanced cancers. However, the tumor microenvironment (TME) functions as a formidable barrier that severely impairs the efficacy of ICIs. While the crosstalk between tumor vessels and immune cells determines the nature of anti-tumor immunity, it is skewed toward a destructive cycle in growing tumors. First, the disorganized tumor vessels hinder CD8+ T cell trafficking into the TME, disable effector functions, and even kill T cells. Moreover, VEGF, the key driver of angiogenesis, interferes with the maturation of dendritic cells, thereby suppressing T cell priming, and VEGF also induces TOX-mediated exhaustion of CD8+ T cells. Meanwhile, a variety of innate and adaptive immune cells contribute to the malformation of tumor vessels. Protumoral M2-like macrophages as well as TH2 and Treg cells secrete pro-angiogenic factors that accelerate uncontrolled angiogenesis and promote vascular immaturity. While CD8+ T and CD4+ TH1 cells suppress angiogenesis and induce vascular maturation by secreting IFN-γ, they are unable to infiltrate the TME due to malformed tumor vessels. These findings led to preclinical studies that demonstrated that simultaneous targeting of tumor vessels and immunity is a viable strategy to normalize aberrant vascular-immune crosstalk and potentiate cancer immunotherapy. Furthermore, this combination strategy has been evidently demonstrated through recent pivotal clinical trials, granted approval from FDA, and is now being used in patients with kidney, liver, lung, or uterine cancer. Overall, combining anti-angiogenic therapy and ICI is a valid therapeutic strategy that can enhance cancer immunity and will further expand the landscape of cancer treatment.Subject terms: Cancer immunotherapy, Cancer microenvironment, Tumour angiogenesis, Tumour immunology, Targeted therapies 相似文献
5.
Robert E. Linder Hannah Weiler-Feilchenfeld Günter Barth Edward Bunnenberg Carl Djerassi 《Theoretical chemistry accounts》1974,36(2):135-143
CNDO calculations of the MCD spectra of 7- and 9-methyladenine have been carried out in two approximations. A minor modification of the CNDO/S method of Jaffé and coworkers shows an improvement over Jaffé's parameterization with respect to band separations and the signs of the MCDB terms, but is not applicable ton→ π* transitions. 相似文献
6.
Andrew M. Steer Hannah L. Bolt William D.G. Brittain Steven L. Cobb 《Tetrahedron letters》2018,59(27):2644-2646
Herein the synthesis of an Fmoc/OtBu orthogonally protected iodotyrosine derivative is reported. This has been achieved via a simple two-step process in an overall 58% yield from commercially available Fmoc-Tyr(tBu)-OH. The Fmoc/OtBu orthogonally protected iodotyrosine was also shown to be amenable to Suzuki-Miyaura cross-coupling to deliver a novel bi-aryl tyrosine derivative. 相似文献
7.
The reaction of aryl acetylide anions with phenyl isocyanate and subsequent addition of a protonating agent such as ethanol affords good yields of 3-aminomaleimides, formed by the cyclization of one molecule of alkyne with two isocyanates. When the reaction is quenched with water instead, cyclopentadienone imines are formed as the major products. 相似文献
8.
Dr. Markus Zegke Hannah L. M. Spencer Dr. Rianne M. Lord 《Chemistry (Weinheim an der Bergstrasse, Germany)》2019,25(53):12275-12280
A range of oxobis(phenyl-1,3-butanedione) vanadium(IV) complexes have been successfully synthesized from cheap starting materials and a simple and solvent-free one-pot dry-melt reaction. This direct, straightforward, fast and alternative approach to inorganic synthesis has the potential for a wide range of applications. Analytical studies confirm their successful synthesis, purity and solid-state coordination, and we report the use of such complexes as potential drug candidates for the treatment of cancer. After a 24 hour incubation of A549 lung carcinoma cells with the compounds, they reveal cytotoxicity values elevenfold greater than cisplatin and remain non-toxic towards normal cell types. Additionally, the complexes are stable over a range of physiological pH values and show the potential for interactions with bovine serum albumin. 相似文献
9.
10.
In connection with research at present being pursued in these laboratories we required quantities of thioacetal (1) for study. Reaction of Wieland-Miescher ketone (2) with one equivalent of 1,2-ethanedithiol gave only (3) resulting from reaction at the α,β-unsaturated carbonyl group. The structure for (3) was deduced primarily from C n. m. r. which showed a saturated carbonyl absorption (δ212.6)1. The preferential reaction of 1,2-ethanedithiol with α,β-unsaturated ketone 相似文献