Background: Prostate cancer represents the second most frequently diagnosed malignancy in
men, and is considered as the fifth leading cause of death from cancer in men. The aims of this paper are
shown the development of new, rapid, and clean synthetic routes toward focused libraries of such
compounds is therefore of great importance to both medicinal and synthetic chemists.
Methods: The preparation of benzochromene and benzoquinoline derivatives using the Michael addition
between benzylidenemalononitrile derivatives and the 1-tetralones respective, in presence of catalytic
amount of piperidine, or in presence of ammonium acetate, and catalytic amount of acetic acid respectively
is reported, together a studies of their activity against human prostate cancer cells PC-3 and LNCaP in vitro.
Results: From a total of 56 compounds, 12 were cytotoxic, inhibiting PC-3 cell viability, and the three most
active compounds were also cytotoxic to LNCaP and MatLyLu cells. An important remark is that the three
compounds were significantly more toxic to cancer cells compared to non-cancer cells (HK-2 and BPH-1).
Conclusion: Three compounds proved to be most active, showed cytotoxic effects in different human and
non-human prostate cancer cell line. The mechanism of the antitumor activity of this structure seems to
be related by inhibition of MMP-9.