The novel atypical retinoid E-3-(4'-hydroxy-3'-adamantylbiphenyl-4-yl)acrylic acid (ST1926) exhibited a potent antiproliferative activity on a large panel of human tumor cells. Despite almost complete loss of ability to activate RARs, the compd. 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.
A Novel Atypical Retinoid Endowed with Proapoptotic and Antitumor Activity / R. Cincinelli, S. Dallavalle, L. Merlini, S. Penco, C. Pisano, P. Carminati, G. Giannini, L. Vesci, C. Gaetano, B. Illy, V. Zuco, R. Supino, F. Zunino. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 46:6(2003 Mar 13), pp. 909-912. [10.1021/jm025593y]
A Novel Atypical Retinoid Endowed with Proapoptotic and Antitumor Activity
R. CincinelliPrimo
;S. DallavalleSecondo
;L. Merlini;
2003
Abstract
The novel atypical retinoid E-3-(4'-hydroxy-3'-adamantylbiphenyl-4-yl)acrylic acid (ST1926) exhibited a potent antiproliferative activity on a large panel of human tumor cells. Despite almost complete loss of ability to activate RARs, the compd. 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.
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