Euphemia Leung, Lisa I Pilkington, Mohinder M Naiya, David Barker, Ayesha Zafar, Chatchakorn Eurtivong, Jóhannes Reynisson
TOTA (trioxatriangulenium ion) is a close-shelled carbocation known to intercalate strongly with the DNA double helix (J. Reynisson, G. B. Schuster, S. B. Howerton, L. D. Williams, R. N. Barnett, C. L. Cleveland, U. Landman, N. Harrit, J. B. Chaires, J. Am. Chem. Soc. 2003, 125 , 2072). The cytotoxicity of TOTA and its four close structural analogues, ADOTA , Pr-ADOTA , Pr-DAOTA and n -Butyl-TATA were tested against the breast cancer cell line MDA-MB-231 and colon cancer cell line HCT116. The most potent derivatives Pr-ADOTA and Pr-DAOTA had IC50 values of ∼80 nM for MDA-MB-231 but slightly higher for HCT116 in the low hundreds nM range...
November 1, 2019: MedChemComm