CAS: 135-73-9; 2-Bromo-4'-Phenylacetophenone

相似化合物

4072-67-7 635-84-7 92-91-1

上下游产品

biphenyl-4-acetaldehyde biphenyl 2-Bromoacetyl bromide 1-(4-phenyl-phenyl)-1-ethanol 2-biphenyl-4-yl-indolizine 3-hydroxy-1-(4-phenyl-phenacyl)-pyridinium; bromide 2-([1,1'-biphenyl]-4-yl)imidazo[1,2-a]pyridine 7-methyl-2-(biphenyl-4-yl)imidazo[1,2-a]pyridine

联苯单乙酮置于溴,溶剂黄146体系中,化学反应生成2-溴-4-苯基乙酰苯
参考文献:能够诱导细胞凋亡的磺酰化 1,2,3-三唑掺入苯磺酰胺对碳酸酐酶 Ix 的选择性抑制
标题:能够诱导细胞凋亡的磺酰化 1,2,3-三唑掺入苯磺酰胺对碳酸酐酶 Ix 的选择性抑制
摘要:抽象的 为了寻找具有细胞凋亡诱导特性的选择性碳酸酐酶 (Ca) Ix 抑制剂,我们设计并合成了 4-和 3-(5-芳基-(4-苯基磺酰基)-1 H-1,2,3-三唑的两个子集-1-基)苯磺酰胺.检测所有化合物对人碳酸酐酶 (Hca) 亚型 I,Ii,Iv 和 Ix 的抑制作用.大多数合成化合物对 Hca I 和 Hca Iv 亚型有微弱的抑制作用.与三取代类似物不同,许多四取代苯磺酰胺对 Hca Ii 异构体表现出低纳摩尔抑制.所有目标化合物对肿瘤相关异构体 Hca Ix 均表现出非常好的抑制特性,K 值范围为 16.4 至 66.0 Nm.测定了一些 Hca Ix 的选择性和有效抑制剂对山羊睾丸细胞的体外凋亡诱导.化合物10D和10H显示出有趣的细胞凋亡诱导潜力.本研究可能为设计基于具有细胞凋亡干扰的 Hca 抑制剂的新型抗癌药物的策略提供见解.
Doi:10.1080/14756366.2022.2077333

专利信息

专利号:WO-9837078-A1
优先权日:1997-02-20
标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-6136984-A
优先权日:1996-04-22
标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-6933303-B2
优先权日:2001-10-19
标 题:Heteroaryl-fused nitrogen heterocycles as therapeutic agents
发明人：MJALLI ADNAN M M; ANDREWS ROBERT C; XIE RONGYUAN; YARRAGUNTA RAVINDRA R; REN TAN
权利人:TRANSTECH PHARMA INC
摘要:This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.

专利号:US-8906915-B2
优先权日:2009-12-17
标 题:Compounds, compositions, and methods for controlling biofilms
发明人：DE KEERSMAECKER SIGRID; DE VOS DIRK; ERMOLATEV DENIS; STEENACKERS HANS; VAN DER EYCKEN ERIK; VANDERLEYDEN JOZEF; SAVALIYA BHARAT S
权利人:DE KEERSMAECKER SIGRID; DE VOS DIRK; ERMOLATEV DENIS; STEENACKERS HANS; VAN DER EYCKEN ERIK; VANDERLEYDEN JOZEF; SAVALIYA BHARAT S; UNIV LEUVEN KATH
摘要:The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.

专利号:WO-9740034-A1
优先权日:1996-04-22
标题:Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes

专利号:JP-2000508664-A
优先权日:1996-04-22
标题:Solid-phase and combinatorial synthesis of substituted thiophenes and arrays of substituted thiophenes