کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1370236 981814 2011 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis of polyfunctionalized piperidone oxime ethers and their cytotoxicity on HeLa cells
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis of polyfunctionalized piperidone oxime ethers and their cytotoxicity on HeLa cells
چکیده انگلیسی

A series of twenty 2,6-diarylpiperidin-4-one O-methyloximes were synthesized with fluoro/chloro/bromo/methyl/methoxy/ethoxy/isopropyl substituents on various positions of the phenyl at C-2 and C-6 in association with/without methyl substituent on the secondary amino group and methyl/ethyl/isopropyl substituents on the active methylene centers. Regardless of their substitution all compounds predominantly exist in the chair conformation except 3m, which adopts a twist-boat conformation. All the synthesized compounds were evaluated for their in vitro antiproliferative activity against human cervical carcinoma (HeLa) cell line. The cytotoxicity of the test compounds was determined by measuring the number of live cells after 24 h of treatment by MTT assay method. This preliminary SAR suggests some lead molecules 3c–f, 3j–k, 4d–g, and 4i with a scope of further structural optimization of the piperidone pharmacophore toward the development of anticancer drug synthesis.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 22, 15 November 2011, Pages 6678–6686
نویسندگان
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