کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1396847 | 1501199 | 2009 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and in vitro cytotoxicity of 9-anilinoacridines bearing N-mustard residue on both anilino and acridine rings
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A series of 9-anilinoacridines having an alkylating N-mustard pharmacophore on both anilino (C-3′ or C-4′) and acridine (C-4) rings with O-ethyl (O-C2) or O-butyl (O-C4) spacer were synthesized to evaluate their cytotoxicity against human lymphoblastic leukemia (CCRF-CEM) cell growth in vitro. It was revealed that these conjugates exhibited significant in vitro cytotoxicity. Among these agents, compound 13 was the most cytotoxic with IC50 value of 1.3 nM and is as potent as taxol (IC50 = 1.1 nM). The structure–activity relationship study showed that the length of the spacer and the position of the substituent do affect their cytotoxicity.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 44, Issue 7, July 2009, Pages 3056–3059
Journal: European Journal of Medicinal Chemistry - Volume 44, Issue 7, July 2009, Pages 3056–3059
نویسندگان
Ching-Huang Chen, Yi-Wen Lin, Xiuguo Zhang, Ting-Chao Chou, Tsong-Jen Tsai, Naval Kapuriya, Rajesh Kakadiya, Tsann-Long Su,