Synthesis and anticancer properties of 5-(1H-benzoimidazol-2-ylmethylene)-4-oxo-2-thioxothiazolidin-3-ylcarboxilic acids

被引：1

作者：

Horishny, Volodymyr ^{[1
]}

Chaban, Taras ^{[2
]}

Matiychuk, Vasyl ^{[3
]}

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

[3] Ivan Franko Natl Univ Lviv, Dept Organ Chem, 6 Kyryla & Mefodia, UA-79005 Lvov, Ukraine

来源：

PHARMACIA | 2021年 / 68卷 / 01期

关键词：

organic synthesis; 5-(1H-benzoimidazol-2-ylmethylene)-4-oxo-2-thioxothiazolidin-3-ylcarboxilic acids; anticancer properties; BIOLOGICAL-ACTIVITY; DRUG; SCAFFOLD; RHODANINE; QSAR;

D O I：

10.3897/pharmacia.68.e49224

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The reaction of 1H-benzoimidazole-2-carbaldehyde with 4-oxo-2-thioxothiazolidin-3-ylcarboxilic acids was studied and the combinatorial library of 5-(1H-benzoimidazol-2-ylmethylene)-4-oxo-2-thioxothiazolidin-3-ylcarboxilic acids has been prepared. The structures of target compounds 8a-f, 9 and 10a, b were confirmed by using1H NMR spectroscopy and elemental analysis. The synthesized compounds were selected by the National Cancer Institute (NCI) Developmental Therapeutic Program for the in vitro cell line screening to investigate their anticancer activity. The tested compounds displayed a weak to medium anticancer activity. The most sensitive cell lines turned out to be SNB-75 of CNS Cancer (GP = 74.84-85.73%) and UO-31, Renal cancer (GP = 71.53-82.16%) and to compound 10a K-562 Leukemia cell lines (GP = 57.14).

引用

页码：195 / 200

页数：6

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