کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1358963 981374 2011 16 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Pyrrolo[3,4-h]quinolinones a new class of photochemotherapeutic agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Pyrrolo[3,4-h]quinolinones a new class of photochemotherapeutic agents
چکیده انگلیسی

Pyrrolo[3,4-h]quinolin-2-ones were synthesized as nitrogen isosters of the angular furocoumarin angelicin, with the aim of obtaining new photochemotherapeutic agents with increased antiproliferative activity and lower undesired toxic effects. A versatile synthetic pathway was approached to allow the isolation of derivatives of the new ring system with a good substitution pattern on the pyrrole moiety. Photobiological screenings of the new compounds revealed a potent phototoxic effect and a great UVA dose dependence, reaching IC50 values at submicromolar level. The induced cellular photocytotoxicity was related to apoptosis with the involvement of mitochondria and lysosomes, alteration of cell cycle profile and membrane lipid peroxidation.

A new series of pyrroloquinolinones were synthesised and evaluated for their phototoxic activity. Some of the title compounds showed, upon UVA irradiation, IC50 values comparable or lower than angelicin used as reference drug.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 7, 1 April 2011, Pages 2326–2341
نویسندگان
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