Synthesis and in vitro antiproliferative activity of novel (4-chloro- and 4-acyloxy-2-butynyl)thioquinolines

被引：9

作者：

Boryczka, Stanislaw ^{[1
]}

Mol, Wojciech ^{[1
]}

Milczarek, Magdalena ^{[2
]}

Wietrzyk, Joanna ^{[2
]}

Bebenek, Ewa ^{[1
]}

机构：

[1] Med Univ Silesia, Dept Organ Chem, PL-41200 Sosnowiec, Poland

[2] Polish Acad Sci, Ludwik Hirszfeld Inst Immunol & Expt Therapy, Dept Expt Oncol, PL-53114 Wroclaw, Poland

来源：

MEDICINAL CHEMISTRY RESEARCH | 2011年 / 20卷 / 08期

关键词：

Acetylenic thioquinolines; (4-Chloro-2-butynyl)thioquinolines; (4-Acyloxy-2-butynyl)thioquinolines; Antiproliferative activity; AZINYL SULFIDES; ANTICANCER; LIPOPHILICITY; CHEMISTRY; ENEDIYNES;

D O I：

10.1007/s00044-010-9495-y

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

The series of new acetylenic thioquinolines containing propargyl, 4-chloro-2-butynyl, and 4-acyloxy-2-butynyl groups have been prepared and tested for antiproliferative activity in vitro against human [SW707 (colorectal adenocarcinoma), CCRF/CEM (leukemia), T47D (breast cancer)] and murine [P388 (leukemia), B16 (melanoma)] cancer lines. Most of the obtained compounds exhibited antiproliferative activity, especially compounds 8, 12, and 21 showed the ID50 values ranging from 0.4 to 3.8 mu g/ml comparable to that of cisplatin used as reference compounds.

引用

页码：1402 / 1410

页数：9

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