当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Discovery of a Monoiodo Aza-BODIPY Near-Infrared Photosensitizer: in vitro and in vivo Evaluation for Photodynamic Therapy.

Discovery of a Monoiodo Aza-BODIPY Near-Infrared Photosensitizer: in vitro and in vivo Evaluation for Photodynamic Therapy.

Abstract：

:Photodynamic therapy (PDT) as a rising platform of the cancer treatment method is receiving increased attention. Through systematic evaluation of halogen substitution on aza-4,4-difluoro-4-bora-3a,4a-diaza-s-indacenes (BODIPY), we have found that monoiodo-derived aza-BODIPYs provided greater efficacy than other halogenated aza-BODIPY PSs. 4 and 15 as monoiodinated aza-BODIPY dyes containing p-methoxyphenyl moiety were identified to be potent NIR aza-BODIPY-type PSs with IC50 values against HeLa cells at a light dose of 54 J/cm2 as low as 76 and 81 nM, respectively. 4 possessed superior phototoxicity, low dark toxicity, and good thermal/photostability and distributed majorly in mitochondria in cells. Apoptosis was verified to be the main cell death pathway, and in vitro reactive oxygen species generation was demonstrated. In vivo whole-body fluorescence imaging and ex vivo organ distribution studies suggested that 4 afforded an excellent PDT effect with a low drug dose under single-time light irradiation and revealed advantages over known PSs of ADPM06 and Ce6.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Yu Z,Zhou J,Ji X,Lin G,Xu S,Dong X,Zhao W

doi

10.1021/acs.jmedchem.0c00882

subject

Has Abstract

pub_date

2020-09-10 00:00:00

pages

9950-9964

issue

17

eissn

0022-2623

issn

1520-4804

journal_volume

63

pub_type

杂志文章

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