CAS: 169243-86-1; Fmoc-Phe(4-F)-Oh

相似化合物

177966-64-2 264276-42-8 18125-46-7

上下游产品

4-fluoro-1-iodobenzene (S)-methyl 2-amino-3-(4-fluorophenyl)propanoate (fluorenylmethoxy)carbonyl chloride Z-DL-Phe(4F)OMe

Dl-对氟苯丙氨酸置于甲酸,Palladium 10% On Activated Carbon,碳酸氢钠,Sodium Carbonate,Sodium Hydroxide体系中,用 1,4-二氧六环,甲醇,水,N,N-二甲基甲酰胺,丙酮 用作溶剂,化学反应 9.0H,反应生成Fmoc-L-4-氟苯丙氨酸
参考文献:含卤化氨基酸的 Bim-23052 新类似物的合成,体外生物活性,水解稳定性和对接
标题:含卤化氨基酸的 Bim-23052 新类似物的合成,体外生物活性,水解稳定性和对接
摘要:一种有效的生长抑素类似物,Bim-23052 (Dc-23-99) D-Phe-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-Nh 2,已在 Nm 浓度下建立了体外生长激素抑制活性.它还具有对一些生长抑素受体的高亲和力的特点,这些受体主要分布在许多肿瘤细胞的细胞膜中.在此,我们报告了使用标准固相肽法 Fmoc/otbu-Strategy 合成一系列含有卤化 Phe 残基的 Bim-23052 类似物.在体外针对两种人类肿瘤细胞系(乳腺癌细胞系和肝细胞癌细胞系)以及人类非致瘤性上皮细胞系测试了这些化合物的细胞毒性作用.含有氟苯丙氨酸的类似物在 μm 范围内具有细胞毒性,因为含有 Phe (2-F) 的类似物对人肝细胞癌细胞系显示出更好的选择性.所提出的研究还表明,根据测试的细胞系,卤化 Phe 残基的积累不会增加细胞毒性.计算出的选择性指数揭示了母体化合物 Bim-23052
Doi:10.1007/s00726-020-02915-3

专利信息

专利号:WO-2015131100-A1
优先权日:2014-02-28
标题:Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids
发明人：YU JIN-QUAN
权利人:SCRIPPS RESEARCH INST
摘要:The use of ligands to tune the reactivity and selectivity of transition metal-catalysts for C(-sp3)-H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C(sp3)-H arylation using pyridine and quinoline derivatives: the former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ligands enables the sequential diarylation of a methyl group in an alanine derivative with two different aryl iodides, affording a wide range of β-Ar-p-Ar ' -cc-amino acids with excellent levels of diastereoselectivity (d.r. > 20:1). Both configurations of the β-chiral center can be accessed by choosing the order in which the aryl groups are installed. The use of a quinoline derivative as a ligand also enables C(sp3)-H olefination of a protected alanine.

专利号:US-2024215280-A1
优先权日:2022-10-31
标 题:In situ core/shell perovskite nanocrystal material, method of preparation thereof, and light emitting device comprising the same
发明人：LEE TAE-WOO; KIM JOO SUNG
权利人:SEOUL NAT UNIV R&DB FOUNDATION; PEROLED CO LTD
摘要:The present inventive concept relates to an in situ core/shell perovskite nanocrystal film formed by an in situ nanocrystal synthesis process, a method for producing the same, and a light emitting device comprising the same as a light-emitting layer. The in situ core/shell perovskite nanocrystal film formed by the in situ nanocrystal synthesis process according to the present inventive concept exhibits a strong charge confinement effect by nanocrystal formation, and can simultaneously greatly improve the luminescence efficiency and lifetime by maintaining the fast charge transport capability of polycrystalline perovskite.

专利号:US-11279734-B2
优先权日:2017-12-01
标 题:Solution-phase affinity selection of inhibitors from combinatorial peptide libraries
发明人：PENTELUTE BRADLEY L; TOUTI FAYCAL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present invention provides novel peptides (e.g., peptides, macrocyclic peptides, mini-proteins) that modulate protein-protein interactions or salts thereof, and methods of making and using the inventive peptides. In some embodiments, the peptides are high affinity inhibitors (e.g., K D of at most 100 nM, at most 10 nM, at most 1 nM) of a protein-protein interaction. In certain embodiments, these peptides interfere with p53-MDM2 binding interactions (e.g., by binding to MDM2 (GenBank® Gene ID: 4193)). In some embodiments, the peptides interfere with the dimerization of the C-terminal domain of the human immunodeficiency virus (HIV) capsid protein (C-CA), comprising residues 146-231 of the HIV capsid protein (e.g., by binding to the C-terminal domain of the HIV capsid protein (C-CA), thereby inhibiting the dimeric interface of HIV capsid protein, thereby inhibiting viral assembly). These inventive peptides were rapidly generated and identified using novel methods described herein comprising combinatorial peptide synthesis and/or solution affinity selection.

专利号:US-6482921-B1
优先权日:1999-01-28
标题:Uridyl peptide antibiotic (UPA) derivatives, their synthesis and use
发明人：BOOJAMRA CONSTANTINE G; LEMOINE REMY C; HECKER SCOTT; LEE VING J; LEGER ROGER
权利人:ESSENTIAL THERAPEUTICS INC
摘要:The present invention relates to dihydro derivatives of the uridyl peptide antibiotics mureidomycin, pacidimycin and napsamycin which have antibiotic activity against a number of bacterial strains including strains resistant to current therapeutic antibiotics.

专利号:US-8338565-B2
优先权日:2008-08-20
标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha
发明人：LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P
权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP
摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.

专利号:US-2024158692-A1
优先权日:2022-10-31
标题 :In-situ core/shell nanoparticle structured metal halide perovskite luminescent material, light emitting device including the same, and manufacturing method thereof
发明人：LEE TAE-WOO; KIM JOO SUNG
权利人:SEOUL NAT UNIV R&DB FOUNDATION; PEROLED CO LTD
摘要:The present inventive concept relates to an in situ core/shell perovskite nanocrystal film formed by an in situ nanocrystal synthesis process, a method for producing the same, and a light emitting device comprising the same as a light-emitting layer. The in situ core/shell perovskite nanocrystal film formed by the in situ nanocrystal synthesis process according to the present inventive concept exhibits a strong charge confinement effect by nanocrystal formation, and can simultaneously greatly improve the luminescence efficiency and lifetime by maintaining the fast charge transport capability of polycrystalline perovskite.