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A novel atypical retinoid endowed with proapoptotic and antitumor activity

Journal of Medicinal Chemistry, ISSN: 0022-2623, Vol: 46, Issue: 6, Page: 909-912
2003
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Article Description

The novel atypical retinoid E-3-(4′-hydroxy-3′-adamantylbiphenyl-4-yl)acrylic acid (ST1926, 4) exhibited a potent antiproliferative activity on a large panel of human tumor cells. Despite almost complete loss of ability to activate RARs, the compound was an effective apoptosis inducer and surprisingly produced DNA damage, that likely contributes to the proapoptotic activity. Following oral administration, 4 was well tolerated and caused tumor growth inhibition in the ovarian carcinoma, A2780/DX, and in the human melanoma, MeWo, growing in nude mice, thus supporting the therapeutic interest of the novel agent.

Bibliographic Details

Cincinelli, Raffaella; Dallavalle, Sabrina; Merlini, Lucio; Penco, Sergio; Pisano, Claudio; Carminati, Paolo; Giannini, Giuseppe; Vesci, Loredana; Gaetano, Carlo; Illy, Barbara; Zuco, Valentina; Supino, Rosanna; Zunino, Franco

American Chemical Society (ACS)

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics

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