Journal
MOLECULES
Volume 25, Issue 22, Pages -Publisher
MDPI
DOI: 10.3390/molecules25225443
Keywords
triterpenoic acid; maslinic acid; tormentic acid; betulinic acid; oleanolic acid; rhodamine B; cytotoxicity
Funding
- German Research Foundation (DFG)
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The combination of the correct triterpenoid, the correct spacer and rhodamine B (RhoB) seems to be decisive for the ability of the conjugate to accumulate in mitochondria. So far, several triterpenoid rhodamine B conjugates have been prepared and screened for their cytotoxic activity. To obtain cytotoxic compounds with EC50 values in a low nano-molar range combined with good tumor/non-tumor selectivity, the Rho B unit has to be attached via an amine spacer to the terpenoid skeleton. To avoid spirolactamization, secondary amines have to be used. First results indicate that a homopiperazinyl spacer is superior to a piperazinyl spacer. Hybrids derived from maslinic acid or tormentic acid are superior to those from oleanolic, ursolic, glycyrrhetinic or euscaphic acid. Thus, a tormentic acid-derived RhoB conjugate 32, holding a homopiperazinyl spacer can be regarded, at present, as the most promising candidate for further biological studies.
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