Acetylenic derivatives are an important class of compounds that has attracted increasing attention as a source of new anticancer agents. The synthetic methods for their preparation are of interest especially with regard to the synthesis of enediyne antibiotics and their analogues.¹ Recently we have carried out a new synthesis of propargyl thioquinolines which exhibited significant in vitro cytotoxicity.^2-3

In the present study a series of new 3,4-disubstituted thioquinolines 5-6 which possess one or two the same or different O, S, Se-propargyl, 4-bromo-2-butynyl, 4-hydroxy-2-butynyl groups were synthesized. The obtained compounds were tested for their antiproliferative activity in vitro against the cells of human (colon cancer SW 707, leukemia CCRF/CEM) and murine (leukemia P388, melanoma B16) cancer cell lines. The most active compounds 5 have the ID₅₀ values ranging from 0.2 to 4.5 μg/ml comparable to that of referential cisplatin.

References:

1. G.B.Jones, F.S.Found, Curr.Pharm.Design, 8, 2415 (2002).

2. S.Boryczka, J.Wietrzyk, A.Nasulewicz, M.Pełczyńska, A.Opolski, Pharmazie, 57, 733 (2002).

3. W.Mól, A.Naczyński, S.Boryczka, J.Wietrzyk, A.Opolski, Pharmazie, (2005, accepted).

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