CAS: 42059-78-9; 6-Ethyl-4-Oxo-4H-Chromene-3-Carbaldehyde

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CAS号24539-92-2 5-乙基-2-羟基苯乙酮 | CAS号68-12-2 N,N-二甲基甲酰胺 | CAS号123-07-9 4-乙基苯酚 | CAS号3245-23-6 乙酸4-乙基苯酯 | CAS号50743-19-6 6-乙基-4-氧代-4H-色烯-3-腈

乙酸-4-乙基苯酚酯置于aluminum (Iii) Chloride,三氯氧磷体系中,化学反应生成 6-乙基-3-甲酰基色酮
参考文献:设计,合成和对接研究具有色酮部分作为mtor /pi3Kα抑制剂的噻吩并嘧啶衍生物
标题:设计,合成和对接研究具有色酮部分作为mtor /pi3Kα抑制剂的噻吩并嘧啶衍生物
摘要:设计并合成了两个带有色酮部分的噻吩并嘧啶衍生物(10A-K,16A-J).评价所有化合物在10Um浓度下对mtor激酶的抑制活性.进一步评估了四种选择的化合物针对mtor激酶,Pi3Kα激酶和两种癌细胞系的ic 50值.一些目标化合物表现出中等至出色的mtor /pi3Kα激酶抑制活性和细胞毒性.最有前途的化合物16I对mtor /pi3Kα激酶表现出非常好的抑制活性,对具有ic 50的h460和pc-3细胞系具有非常好的抗肿瘤效力值分别为0.16+/-0.03μm,2.35+/-0.19μm,1.20+/-0.23μm和0.85+/-0.04μm,分别是化合物i活性的8.6,> 5,7.9和19.1倍(1.37+/-0.07μm,> 10μm,9.52+/-分别为0.29μm,16.27+/-0.54μm).结构活性关系(sars)和对接研究表明,色酮部分对于这些化合物的有效抗肿瘤活性和细胞毒性是必需的.色酮部
DOI:10.1016/j.Ejmech.2015.01.061

专利信息

专利号:US-3984441-A
优先权日:1971-06-21
标 题:Chromonealdehyde compounds and process for the production thereof
发明人：NOHARA AKIRA; UMETANI TOMONOBU; MIYATA YOSHIBUMI; SANNO YASUSHI
权利人:TAKEDA CHEMICAL INDUSTRIES LTD
摘要:There are provided compounds of the general formula ##SPC1## n Wherein R is a hydroxy, alkyl, acyloxy, halogen, nitro, substituted or unsubstituted amino, alkoxy, carboxy or a group derived from a carboxy group and m is 0, 1 or 2 except where m is 2, the two R groups are both hydroxy groups. n The present invention is also concerned with a process for preparing the chromonealdehyde compounds. The chromonealdehyde compounds are characterized by antiallergic properties and are therefore useful as prophylactic and therapeutic agents for allergic asthma, allergic dermatitis and other allergic diseases and also are valuable as intermediates for the synthesis of other pharmaceutical compounds having the chromone nucleus.