کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1362668 | 981493 | 2006 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and comparative molecular field analysis (CoMFA) of argentatin B derivatives as growth inhibitors of human cancer cell lines
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Synthesis, anticancer activity, and QSAR of 14 argentatin B analogs are described. Derivative 2-formyl-(16β,24R)-16,24-epoxy-25-hydroxycycloart-1-en-3-one was 35-50 times more potent than argentatin B to inhibit the growth of four human cancer cell lines. 3D-QSAR of K562 cell line growth inhibition was performed using the X-ray crystallographic structures of six derivatives as prototypes. Comparative molecular field analysis showed that a bulky group at C-2, a C1-C2 double bond, and a low electronic density near to C-25 increase the potency of these triterpenes. Experimental Log Ps for argentatin B and one derivative were 1-2 Log units more hydrophilic than the C Log P predicted values.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 6, 15 March 2006, Pages 1889-1901
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 6, 15 March 2006, Pages 1889-1901
نویسندگان
Hortensia Parra-Delgado, César M. Compadre, Teresa RamÃrez-Apan, MarÃa J. Muñoz-Fambuena, R. Lilia Compadre, Patricia Ostrosky-Wegman, Mariano MartÃnez-Vázquez,