A novel atypical retinoid endowed with proapoptotic and antitumor activity

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

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish
Pages (from-to)909-912
Number of pages4
JournalJournal of Medicinal Chemistry
Volume46
Issue number6
DOIs
Publication statusPublished - Mar 13 2003

ASJC Scopus subject areas

  • Organic Chemistry

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