Syntheses and PDT activity of new mono- and di-conjugated derivatives of chlorin e

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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.

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Journal of porphyrins and phthalocyanines

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