Syntheses and PDT activity of new mono- and di-conjugated derivatives of chlorin e
Syntheses of three new chlorin e conjugates for PDT of tumors are reported. One of the new compounds is conjugated with lysine at the 13-position, but the others are mono-conjugated or diconjugated with the non-amino acid species ethanolamine. Cellular experiments with the three new compounds and previously synthesized non-amino acid 15-conjugates (-), 13-monoconjugates , , and a 13,15-diconjugate are reported. cytotoxicity experiments show that the 13-conjugates are more toxic than the 15-conjugates, and the most toxic derivative (dark- and photo-toxicity) is the 13-ethylenediamine conjugate . The most useful PDT photosentitizers appear to be the ethanolamine derivatives, conjugated at the 15- and the 13,15-positions; these show high phototoxicity but relatively low dark toxicity compared with , and also the highest dark/photo cytotoxicity ratios.
Publication Source (Journal or Book title)
Journal of porphyrins and phthalocyanines
Chen, H., Humble, S. W., Waruna Jinadasa, R. G., Zhou, Z., Nguyen, A. L., Vicente, M. G., & Smith, K. M. (2017). Syntheses and PDT activity of new mono- and di-conjugated derivatives of chlorin e. Journal of porphyrins and phthalocyanines, 21 (4-6), 354-363. https://doi.org/10.1142/S1088424617500262