تفاصيل الوثيقة
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نوع الوثيقة |
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مقال في مجلة دورية |
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عنوان الوثيقة |
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A facile synthesis of some 3-cyano-1,4,6-trisubstituted-2(1H)-pyridinones and their biological evaluation as anticancer agents A facile synthesis of some 3-cyano-1,4,6-trisubstituted-2(1H)-pyridinones and their biological evaluation as anticancer agents |
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الموضوع |
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كيمياء |
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لغة الوثيقة |
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الانجليزية |
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المستخلص |
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The synthesis of some new 3-cyano-1,4,6-trisubstituted-2(1H)-pyridinones supported with various pharmacophores and functionalities at positin-1 is described. The in vitro anticancer activity of 24 of the newly synthesized compounds was evaluated according to the protocol of the NCI in vitro disease-oriented human cells screening panel assay. The results revealed that five compounds 4a-c, 7b, and 12b were able to display moderate antitumor potential against some of the tested subpanel tumor cell lines at the GI50 and TGI levels, however, with marginal or no cytotoxic (LC 50) activity. The obtained data suggested that better antitumor activity was linked to derivatives with either 4-bromophenyl or 3,4-dimethoxyphenyl moieties, together with a 1-methyl-1H-pyrrol-2-yl counter part at positions 6 and 4, respectively. Consequently, he 3-cyano-4-(1-methyl-1H-pyrrol-2-yl)-6-(4- bromophenyl or 3,4-dimethoxyphenyl)-2(1H)-pyridinones 4a and 4b, could be considered as the most active members identified in this investigation as evidenced from their relative higher growth inhibitory (GI 50 (MG-MID) 77.6 and 67.6 μM, respectively) and cytostatic (TGI (MG-MID) 85.1 and 95.5 lM, respectively) activities, when compared with the substituted thiocarbamoyl analog 7b and the icyclic [1,2,4]triazolo[3,4-a]pyridine derivative 12b. |
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ردمد |
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1054-2523 |
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اسم الدورية |
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Medicinal Chemistry Research |
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المجلد |
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20 |
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العدد |
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8 |
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سنة النشر |
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1432 هـ
2011 م |
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نوع المقالة |
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مقالة علمية |
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تاريخ الاضافة على الموقع |
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Saturday, March 17, 2012 |
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الباحثون
| Sherif A F Rostom | Rostom, Sherif A F | باحث | دكتوراه | sherifrostom@yahoo.com |
| حسن مصطفى فيض الله | Faidallah, Hassan Mostafa | باحث | دكتوراه | HFAIDALLAH@kau.edu.sa |
| Mohammed S M Al-Saadi | Al-Saadi, Mohammed S M | باحث | دكتوراه | |
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الرجوع إلى صفحة الأبحاث
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