CAS: 16732-65-3; 6-Bromo-1H-Indole-2-Carboxylic Acid

相似化合物

103858-53-3 372089-59-3 105191-12-6

上下游产品

CAS号103858-53-3 6-溴吲哚-2-羧酸乙酯 | CAS号33599-61-0 6-溴色氨酸 | CAS号52415-29-9 6-溴吲哚 | CAS号5318-27-4 6-氨基吲哚 | CAS号105191-12-6 6-溴吲哚-2-甲醛 | CAS号103858-53-3 6-溴吲哚-2-羧酸乙酯 | CAS号923197-75-5 6-溴-1H-吲哚-2-基)甲醇

6-溴吲哚-2-羧酸乙酯置于sodium Hydroxide体系中,用 四氢呋喃,水 用作溶剂,化学反应生成6-溴吲哚-2-羧酸
参考文献:Af9/enl 与 Af4 或 Dot1L 之间蛋白质-蛋白质相互作用的小分子抑制剂的发现,结构-活性关系和体外抗癌活性.
标题:Af9/enl 与 Af4 或 Dot1L 之间蛋白质-蛋白质相互作用的小分子抑制剂的发现,结构-活性关系和体外抗癌活性.
摘要:涉及混合谱系白血病 (Mll) 基因的染色体易位导致 5-10% 的急性白血病,且临床结果不佳.最常见的 Mll 融合伴侣蛋白 Af9/enl 和 Af4 或组蛋白甲基转移酶 Dot1L 之间的蛋白质-蛋白质相互作用 (Ppi) 是 Mll 重排 (Mll-R) 白血病的药物靶点.几种苯并噻吩甲酰胺化合物被鉴定为这些 Ppi 的新型抑制剂,Ic50 值低至 1.6 μm.对 77 种苯并噻吩以及相关吲哚和苯并呋喃化合物的构效关系研究表明,4-哌啶-1-基苯基或 4-吡咯烷-1-基苯基取代基对于活性至关重要.该抑制剂抑制mll靶基因hoxa9,Meis1和myc的表达,并选择性抑制mll-R和其他急性髓系白血病细胞的增殖,Ec50值低至4.7 μm.这些抑制剂是 Af9/enl 生物学研究的有用化学探针,也是进一步开发针对 Mll-R 和其他白血病的药物的药理学先导物.
Doi:10.3390/cancers15215283

专利信息

专利号:WO-2011050245-A1
优先权日:2009-10-23
标 题:Bicyclic heteroaryls as kinase inhibitors
发明人：FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS
权利人:FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS
摘要:The invention is directed to heteroaryl compounds useful as inhibitors of various kinase enzymes. In various embodiments, the invention provides a heteroaryl compound having inhibitory bioactivity with respect to a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Flt kinase, an Aurora kinase, or a Src kinase, or any combination thereof. Compounds of the invention include bicyclic heteroaryl compounds of formula (I), which can contain a bridging nitrogen atom at a ring junction. The invention further provides methods of synthesis of compounds of the invention, pharmaceutical compositions, pharmaceutical combinations, and methods of treatment of malconditions using compounds of the invention.

专利号:CN-118496228-A
优先权日:2024-03-15
标题 :Green synthesis method and activity research of C2-spiro indoline derivative