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Synthesis and evaluation of novel chlorophyll a derivatives as potent photosensitizers for photodynamic therapy.

Abstract：

:Chlorophyll a exhibits excellent photosensitive activity in photosynthesis. The unstability limited its application as photoensitizer drug in photodynamic therapy. Here a series of novel chlorophyll a degradation products pyropheophorbide-a derivatives were synthesized and evaluated for lung cancer in PDT. These compounds have strong absorption in 660-670 nm with high molar extinction coefficient, and fluorescence emission in 660-675 nm upon excitation with 410-415 nm light. They all have much higher ROS yields than pyropheophorbide-a, and compound 10 was even higher than [3-(1-hexyloxyethyl)]-pyrophoeophorbide a (HPPH). Distinctive phototoxicity was observed in vitro and the inhibition effect was in light dose-dependent and drug dose-dependent style. They can effectively inhibit the growth of lung tumor in vivo. Among them, compound 8 and 11 have outstanding photodynamic anti-tumor effects without obvious skin photo-toxicity, so they can act as new drug candidates for photodynamic therapy.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Gao YH,Zhu XX,Zhu W,Wu D,Chen DY,Yan YJ,Wu XF,O'Shea DF,Chen ZL

doi

10.1016/j.ejmech.2019.111959

subject

Has Abstract

pub_date

2020-02-01 00:00:00

pages

111959

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(19)31111-0

journal_volume

187

pub_type

杂志文章

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