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 ID(50) values ranging from 0.2 to 4.6 mu g/ml comparable to that of cisplatin used as referencecompounds. (C) 2008 Elsevier Ltd. All rights reserved.