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CAS号32315-10-9 三光气 | CAS号591-19-5 3-溴苯胺 | CAS号72755-05-6 3-bromobenzoyl azide | CAS号1711-09-7 3-溴苯甲酰氯 | CAS号75-44-5 光气 | CAS号86764-82-1 1,1-dibenzyl-3-... | CAS号86781-61-5 3-(3-bromopheny... | CAS号944709-54-0 3-(3-bromopheny...3-Bromobenzoyl Azide 以 1,2-二氯乙烷 用作溶剂,化学反应 2.0H,反应生成3-溴苯基异氰酸酯
参考文献:新型脲基苯甲酰胺衍生物作为强效聚(adp-核糖)聚合酶-1(parp-1)抑制剂的设计,合成,生物学评价和分子对接研究
标题:新型脲基苯甲酰胺衍生物作为强效聚(adp-核糖)聚合酶-1(parp-1)抑制剂的设计,合成,生物学评价和分子对接研究
摘要:Poly(Adp-Ribose) Polymerase-1 (Parp-1) 是负责修复 Dna 单链断裂的 Dna 修复酶的关键成员之一.Parp-1的抑制已被证明是一种通过靶向dna修复途径选择性杀死肿瘤细胞的有前景的策略.在此,基于基于结构的药物设计策略,设计合成了一系列新型脲基苯甲酰胺衍生物.评价了对hct116,Mda-Mb-231,Hela,A579和a375等五种人类癌细胞系的抗癌活性,并总结了初步的构效关系.其中,化合物23F和27F对 Hct116 细胞具有有效的抗增殖作用,Ic 50值分别为 7.87 μm 和 8.93 μm.此外,两种化合物均表现出优异的 Parp-1 抑制活性,Ic 50值分别为 5.17 Nm 和 6.06 Nm.机理研究表明,23F和27F能有效抑制hct116细胞的集落形成和细胞迁移.此外,23F和27F可导致细胞周期停滞在g2/m期,并通过
Doi:10.1016/j.Ejmech.2022.114790
专利信息
专利号:US-4267070-A
优先权日:1979-10-30
标题:Catalyst for the synthesis of aromatic monoisocyanates
发明人:NEFEDOV BORIS K; MANOV-JUVENSKY VLADIMIR I; DERGUNOV JURY I; RYSIKHIN ANATOLY I; CHIMISHKIAN ALEXANDR L
权利人:NEFEDOV BORIS K; MANOV JUVENSKY VLADIMIR I; DERGUNOV JURY I; RYSIKHIN ANATOLY I; CHIMISHKIAN ALEXANDR L
摘要:A catalyst for the synthesis of aromatic monoisocyanates comprising 1.64 to 16.6% by weight of palladium chloride, 0.16 to 47.6% by weight of an oxide of a metal of Group VB of the periodic system, 1.5 to 81.8% by weight of an oxide of a metal of Group VI B of the periodic system, 1.64 to 89.8% by weight of pyridine or an alkylsubstituted pyridine. n The use of the catalyst according to the invention in the synthesis of aromatic monoisocyanates makes it possible to obtain a high degree of conversion of the starting compound of up to 100%, a high yield of the desired product of up to 97%, and increased productivity of the catalyst of up to 40 g of the desired product per g of PdCl 2 per hour.
专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:CN-111471171-B
优先权日:2019-01-24
标 题:A kind of aryl sulfonic acid intermediate and its preparation method, and its application for the synthesis of low temperature sensitive admixture for concrete
专利号:US-6861523-B2
优先权日:2002-02-08
标 题 :1,3,5- trisubstituted-1,3,5-triazine-2,4,6-trione compounds and libraries
发明人:YU YONGPING; OSTRESH JOHN M; HOUGHTEN RICHARD A
权利人:TORREY PINES INST
摘要:The solid-phase synthesis of individual 1,3-disubstituted and 1,3,5-trisubstituted-1,3,5-triazine-2,4,6-triones and libraries thereof from a resin is described. Reaction of resin-bound amino acids with isocyanates yields resin-bound ureas, which further react with chlorocarbonyl isocyanate to selectively afford the resin-bound 1,3-disubstituted-1,3,5-triazine-2,4,6-triones. Selective alkylation at the N-5 position of the resin-bound 1,3-disubstituted-1,3,5-triazine-2,4,6-triones produces a trisubstituted triazinetrione. The products are cleaved from their solid support and obtained in good yield and purity.
专利号:CN-115385973-B
优先权日:2022-07-13
标题:Application of oligomeric nucleic acid-tetrahydrothiazole compounds in the synthesis of gene-encoded compound libraries
专利号:CN-115385973-A
优先权日:2022-07-13
标题 :Application of oligomeric nucleic acid-tetrahydrothiazole compounds in the synthesis of gene-encoded compound libraries