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

The series of new acetylenic thioquinolines containing propargyl, 2-butynyl, 4-bromo-2-butynyl, and 4-hydroxy-2-butynyl groups has been prepared and tested for antiproliferative activity in vitro against human [SW707 (colorectal adenocarcinoma), CCRF/CEM (leukemia)] and murine [P388 (leukemia), B16 (melanoma)] cancer lines. All the compounds obtained exhibited antiproliferative activity. The most active compounds 7, 16, 17, and 19 have the ID50 values ranging from 0.2 to 4.6 μg/ml comparable to that of cisplatin used as reference compounds.

The synthesis of new acetylenic thioquinolines containing propargyl, 2-butynyl, 4-bromo-2-butynyl, and 4-hydroxy-2-butynyl groups exhibiting anti-proliferative activity in vitro against the cells of human and murine cancer cell lines was investigated.Figure optionsDownload as PowerPoint slide