二炔基硫代喹啉的体外合成及其抗增殖活性
Synthesis and antiproliferative activity in vitro of diacetylenic thioquinolines.
作者信息
Mól W, Naczyński A, Boryczka S, Wietrzyk J, Opolski A
机构信息
Department of Organic Chemistry, The Medical University of Silesia, Sosnowiec, Poland.
出版信息
Pharmazie. 2006 Sep;61(9):742-6.
A series of new acetylenic thioquinolines containing propargyl, 2-butynyl, or 4-bromo-2-butynyl groups has been prepared and tested for antiproliferative activity in vitro against the cells of human [SW707 (colon cancer), CCRF/CEM (leukemia)] and murine [P388 (leukemia), B16 (melanoma)] cancer lines. All the compounds obtained exhibited antiproliferative activity. The most active compounds 4h and 41-m have ID50 values ranging from 0.2 to 3.6 microg/ml, comparable to that of the reference compound cisplatin.
已制备出一系列含有炔丙基、2-丁炔基或4-溴-2-丁炔基的新型乙炔硫代喹啉，并对其进行了体外抗增殖活性测试，以检测其对人[SW707（结肠癌）、CCRF/CEM（白血病）]和小鼠[P388（白血病）、B16（黑色素瘤）]癌细胞系的作用。所得到的所有化合物均表现出抗增殖活性。活性最强的化合物4h和41-m的半数抑制浓度（ID50）值在0.2至3.6微克/毫升之间，与参考化合物顺铂相当。
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