کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8993439 | 1113800 | 2005 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
1,5-Benzodiazepines XIV. Synthesis of new substituted 9H-bis-[1,2,4]triazolo[4,3-a:3â²,4â²-d] [1,5]benzodiazepines and relate compounds endowed with in vitro cytotoxic properties
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: 1,5-Benzodiazepines XIV. Synthesis of new substituted 9H-bis-[1,2,4]triazolo[4,3-a:3â²,4â²-d] [1,5]benzodiazepines and relate compounds endowed with in vitro cytotoxic properties 1,5-Benzodiazepines XIV. Synthesis of new substituted 9H-bis-[1,2,4]triazolo[4,3-a:3â²,4â²-d] [1,5]benzodiazepines and relate compounds endowed with in vitro cytotoxic properties](/preview/png/8993439.png)
چکیده انگلیسی
A series of 11 new 9H-bis-[1,2,4]triazolo[4,3-a:3â²,4â²-d] [1,5]benzodiazepine derivatives 8e-o was synthesized. Ten of these compounds (8e-m,o), along with four analogues (8a-d) (previously synthesized by us) were tested in vitro in order to evaluate their cytotoxic and anti-HIV-1 properties. In this connection other six original compounds, i.e., five 9-substituted compounds prepared starting from the 6,12-diphenylderivative 8c (compounds 10, 11, 12, 13a,b) and the bis-triazolone derivative 14, were synthesized and tested for the same purpose. While none of the 20 compounds tested exhibited any appreciable anti-HIV-1 activity, some of them exhibited interesting cytotoxic properties, the best results being shown by compounds 8c,d,k and 11 (CC50 range = 3-12 μM). Therefore, these four compounds were further evaluated for their antiproliferative activity against a panel of human tumor cell lines; actually, compounds 8d, 8k and 11 showed antiproliferative properties against either or both leukemia- and lymphoma-derived cell lines in the low micromolar range.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Il Farmaco - Volume 60, Issue 2, February 2005, Pages 113-125
Journal: Il Farmaco - Volume 60, Issue 2, February 2005, Pages 113-125
نویسندگان
Mario Di Braccio, Giancarlo Grossi, Maurizio Ceruti, Flavio Rocco, Roberta Loddo, Giuseppina Sanna, Bernardetta Busonera, Marta Murreddu, Maria Elena Marongiu,