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Synthesis and cytotoxic evaluation of malachite green derived oleanolic and ursolic acid piperazineamides

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The coupling of acetylated piperazinylamide spacered triterpenoic oleanolic acid and ursolic acid with meta or para substituted carboxylated malachite green analogs gave conjugates 10 , 11 , 15 , and… Click to show full abstract

The coupling of acetylated piperazinylamide spacered triterpenoic oleanolic acid and ursolic acid with meta or para substituted carboxylated malachite green analogs gave conjugates 10 , 11 , 15 , and 16 that were cytotoxic for several human tumor cell lines. Especially, an oleanolic acid-derived compound 10 was cytotoxic for MCF-7 human breast carcinoma cells (EC 50  = 0.7 μM). These derivatives represent first examples of triterpenoic acid derivatives holding a cationic scaffold derived from malachite green.

Keywords: ursolic acid; malachite green; cytotoxic evaluation; synthesis cytotoxic; acid

Journal Title: Medicinal Chemistry Research
Year Published: 2020

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