engleski

Substituted Adamantylphthalimides: Synthesis, Antiviral and Antiproliferative Activity

Three groups of adamantylphthalimides, bearing different substituents at the phthalimide moiety, N-(4′-R2)phthalimidoadamantanes, 1-7, 3-[N-(4′-R2)phthalimido]-1-adamantanols, 8-10 and 3-[N-(4′-R2)phthalimido]adamantane-1-carboxylic acids 11-15, were synthesized and screened against tumor cells and viruses. The most potent compounds are not substituted at the adamantane and bear OH or NH2 substituent at the phthalimide (compounds 3 and 5). The antiproliferative activity of 3 and 5 is in micromolar range, much higher than the one of thalidomide. Minor antiviral activity against cytomegalovirus and varicella-zoster virus was found for 3 and 5 but these compounds lacked selectivity. The results presented are important for the rational design of next generation of compounds with anticancer and antiviral activity.

Adamantane ; Antiproliferative activity ; Antiviral activity ; Phthalimide

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