The 2-((5-(3-(2-Fluorophenyl)acryloyl)-4-methylthiazol-2-yl)amino)isoindoline-1,3-dione

被引:0
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作者
Fedusevych, Olha-Maria [1 ]
Lozynskyi, Andrii [1 ]
Sulyma, Marta [2 ]
Lesyk, Roman [1 ]
机构
[1] Danylo Halytsky Lviv Natl Med Univ, Dept Pharmaceut Organ & Bioorgan Chem, Pekarska 69, UA-79010 Lvov, Ukraine
[2] Danylo Halytsky Lviv Natl Med Univ, Dept Gen Bioinorgan Phys & Colloidal Chem, Pekarska 69, UA-79010 Lvov, Ukraine
关键词
thiazole; Claisen-Schmidt condensation; anticancer activity; pharmacokinetics prediction; ANTICANCER; SCREEN;
D O I
10.3390/M1785
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
In this work, the title compound was synthesized via the Claisen-Schmidt condensation of a 2-((5-acetyl-4-methylthiazol-2-yl)amino)isoindoline-1,3-dione with 2-fluorobenzaldehyde. The structure of the synthesized compound (yield 62%) was confirmed by H-1, C-13 NMR, and LC-MS spectra. According to US NCI protocols, the compound displayed a high level of antimitotic activity against tested human tumor cells, with mean GI(50)/TGI values of 15.72/50.68 mu M. The drug-like properties of the synthesized compound were evaluated using SwissAdme, revealing satisfactory drug-like parameters, and it presents interest for the design of new synthetic agents with biological activity.
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页数:7
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