Synthesis, Antiproliferative, and Antiangiogenic Activities of Benzochromene and Benzoquinoline Derivatives on Prostate Cancer in vitro

Author(s): Gricelda Mata, Juan Rodrigues, Neira Gamboa, Katiuska Charris, Gricela Lobo, Melina Monasterios, Milagros Avendano, Michael Lein, Klaus Jung, Claudia Abramjuk, Bianca Nitzsche, Michael Hopfner, Jaime Charris

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 4 , 2017

Become EABM
Become Reviewer
Call for Editor


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.

Keywords: Benzochromene, benzoquinoline, prostate, cancer, MMP-9.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2017
Page: [398 - 413]
Pages: 16
DOI: 10.2174/1570180814666161118163844
Price: $65

Article Metrics

PDF: 49
PRC: 2