Synthesis and Biological Evaluation of Furo[2,3-d]pyrimidines as Akt1 Kinase Inhibitors

Se Young Kim; Dong Jin Kim; Beom Seok Yang

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Synthesis and Biological Evaluation of Furo[2,3-d]pyrimidines as Akt1 Kinase Inhibitors

机译：呋喃[2,3-d]嘧啶类化合物作为Akt1激酶抑制剂的合成及生物学评价

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Based on the hit compound 4 derived from focused library,a series of furo[2,3-d]pyrimidines were designed,synthesized and evaluated for the inhibitory activity against Akt1 kinase.And their structure-activity relationships were investigated.Of these compounds,3a having 2-thienyl and methyl groups at R_1 and R_2 showed the most potent activity with an IC_(50)value of 24 mu M.Introduction of the thienyl groups at C-5 and C-6 positions significantly improved potency compared to furyl and phenyl groups.

机译：基于聚焦库中的命中化合物4，设计，合成和评价了一系列呋喃[2,3-d]嘧啶类化合物，以评估其对Akt1激酶的抑制活性，并研究它们之间的结构-活性关系。在R_1和R_2上具有2-噻吩基和甲基的3a表现出最强的活性，IC_（50）值为24μM。与呋喃基和呋喃基相比，在C-5和C-6位置引入噻吩基显着提高了效力。苯基。

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《Bulletin of the Korean Chemical Society》 |2007年第7期|共5页
作者
Se Young Kim; Dong Jin Kim; Beom Seok Yang;
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正文语种 eng
中图分类化学工业;
关键词
Akt1 kinase; Inhibitory activity; Furo2; 3-dpyrimidines;

机译：Akt1激酶;抑制活性;呋喃[2;3-d]嘧啶;

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1. Synthesis and Biological Evaluation of Furo[2,3-d]pyrimidines as Akt1 Kinase Inhibitors [J] . Se Young Kim, Dong Jin Kim, Beom Seok Yang Bulletin of the Korean Chemical Society . 2007,第7期

机译：呋喃[2,3-d]嘧啶类化合物作为Akt1激酶抑制剂的合成及生物学评价
2. Selective Pneumocystis carinii dihydrofolate reductase inhibitors: design, synthesis, and biological evaluation of new 2,4-diamino-5-substituted-furo(2,3-d)pyrimidines. [J] . Gangjee A, Guo X, Queener SF, Journal of Medicinal Chemistry . 1998,第8期

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3. Synthesis and biological evaluation of pyrido(3',2':4,5)furo(3,2-d)pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors. [J] . Hayakawa M, Kaizawa H, Moritomo H, Bioorganic and Medicinal Chemistry Letters . 2007,第9期

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5. Synthesis of substituted pyrrolo[2,3-d]pyrimidines as microtubule-binding agents and HSP90 inhibitors [D] . Lin, Lu 2013

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6. Design synthesis and biological evaluation of novel 2-phenyl pyrimidine derivatives as potent Brutons tyrosine kinase (BTK) inhibitors [O] . Xinyu Li, Binyu Shi, Yu Teng, 2019

机译：新型2-苯基嘧啶衍生物作为有效的布鲁顿酪氨酸激酶（BTK）抑制剂的设计合成和生物学评估
7. Synthesis and Biological Evaluation of Furo2,3-dpyrimidines as Akt1 Kinase Inhibitors [O] . 2007

机译：呋喃2,3-D嘧啶作为AKT1激酶抑制剂的合成与生物学评价

Synthesis and Biological Evaluation of Furo[2,3-d]pyrimidines as Akt1 Kinase Inhibitors

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