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合成修饰的甲氧沙林在光和暗反应中增强细胞毒性。

Synthetically modified methoxsalen for enhanced cytotoxicity in light and dark reactions.

机构信息

Department of Chemistry, Lehigh University, Bethlehem, PA 18015 USA.

Department of Environmental and Occupational Health, Rutgers University School of Public Health, Piscataway, NJ 08854, USA.

出版信息

Bioorg Med Chem Lett. 2019 Feb 15;29(4):619-622. doi: 10.1016/j.bmcl.2018.12.048. Epub 2018 Dec 22.

DOI:10.1016/j.bmcl.2018.12.048
PMID:30638875
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6364570/
Abstract

Linear furocoumarins, also known as psoralens, are clinically useful photo-activated pharmaceuticals employed to address hyperproliferative skin diseases. Seven diverse cytotoxic pharmacophores have been synthetically attached to 8-methoxypsoralen via a 5-amino functionality. The resulting unique set of compounds was evaluated for dark and light toxicity against PAM212 keratinocytes in culture.

摘要

线性呋喃香豆素，又称补骨脂素，是临床上有用的光激活药物，用于治疗皮肤过度增生性疾病。通过 5-氨基功能基，将七种不同的细胞毒性药效团合成到 8-甲氧基补骨脂素上。对所得的一组独特化合物进行了黑暗和光照毒性评估，以测试其对 PAM212 角质细胞系的毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/facb/6364570/6d4605dc7c1e/nihms-1518495-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/facb/6364570/9ea0f0e00f14/nihms-1518495-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/facb/6364570/6d4605dc7c1e/nihms-1518495-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/facb/6364570/9ea0f0e00f14/nihms-1518495-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/facb/6364570/6d4605dc7c1e/nihms-1518495-f0003.jpg

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