1036766-56-9Relevant articles and documents
Synthesis of 3-(1-adamantyl)-4-methoxyphenylboric acid
Tribulovich,Garabadzhiu,Kalvins
, p. 868 - 869 (2010)
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Novel adamantyl retinoid-related molecules with POLA1 inhibitory activity
Cardile, Francesco,Cincinelli, Raffaella,Colelli, Fabiana,Dallavalle, Sabrina,Darwiche, Nadine,Fucci, Alessandra,Gervasoni, Silvia,Guglielmi, Mario B.,La Porta, Ilaria,Luca D'Andrea, Egildo,Musso, Loana,Pisano, Claudio,Signorino, Giacomo,Vistoli, Giulio
, (2020/09/15)
Atypical retinoids (AR) or retinoid-related molecules (RRMs) represent a promising class of antitumor compounds. Among AR, E-3-(3′-adamantan-1-yl-4′-hydroxybiphenyl-4-yl)acrylic acid (adarotene), has been extensively investigated. In the present work we report the results of our efforts to develop new adarotene-related atypical retinoids endowed also with POLA1 inhibitory activity. The effects of the synthesized compounds on cell growth were determined on a panel of human and hematological cancer cell lines. The most promising compounds showed antitumor activity against several tumor histotypes and increased cytotoxic activity against an adarotene-resistant cell line, compared to the parent molecule. The antitumor activity of a selected compound was evaluated on HT-29 human colon carcinoma and human mesothelioma (MM487) xenografts. Particularly significant was the in vivo activity of the compound as a single agent compared to adarotene and cisplatin, against pleural mesothelioma MM487. No reduction of mice body weight was observed, thus suggesting a higher tolerability with respect to the parent compound adarotene.
METHOD FOR PREPARATION OF 6-[3(1-ADAMANTYL) -4-METHOXYPHENYL]-2-NAPHTOIC ACID
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Page/Page column 2, (2010/04/23)
A method for preparation of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid is disclosed based on “one pot” synthesis approach including a direct synthesis of boronic acid derivative from 2-(1-adamantyl)-4-bromoanisole and cycloboranes with a subsequent Suzuki-Miyaura coupling with 6-halonaphthenoates and basic hydrolysis of the reaction product in ethylene glycol or 1,2-propanediol.