Synthesis and Anticancer and Antiviral Activities of New 2-Pyrazoline-Substituted 4-Thiazolidinones

被引:56
作者
Havrylyuk, Dmytro [1 ]
Zimenkovsky, Borys [1 ]
Vasylenko, Olexandr [2 ]
Lesyk, Roman [1 ]
机构
[1] Danylo Halytsky Lviv Natl Med Univ, Dept Pharmaceut Organ & Bioorgan Chem, UA-79010 Lvov, Ukraine
[2] Natl Acad Sci Ukraine, Inst Bioorgan Chem & Petrochem, UA-02094 Kiev, Ukraine
关键词
IN-VITRO; BIOLOGICAL EVALUATION; ANTITUMOR-ACTIVITY; DERIVATIVES; THIAZOLIDINONE; MOIETY;
D O I
10.1002/jhet.1056
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
2-(4,5-Dihydropyrazol-1-yl)-thiazol-4-ones (25) have been synthesized starting from 3-phenyl-5-aryl-1-thiocarbamoyl-2-pyrazolines via [2+3]-cyclization with 2-bromopropionic acid, maleic anhydride, N-arylmaleimides, and aroylacrylic acids. The in vitro anticancer activity of , , , , and were tested by the National Cancer Institute. Compounds , , and demonstrated selective inhibition of leukemia cell lines growth at a single concentration (105 M). The screening of antiviral activity for a broad panel of viruses revealed that N-(4-methoxyphenyl)-2-{2-[5-(4-methoxyphenyl)-3-phenyl-4,5-dihydropyrazol-1-yl]-4-oxo-4,5-dihydrothiazol-5-yl}-acetamide was highly active against Tacaribe TRVL 11 573 virus strain (EC50 = 0.71 g/mL, selectivity index = 130).
引用
收藏
页码:E55 / E62
页数:8
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