869494-92-8Relevant academic research and scientific papers
Microwave-assisted synthesis of certain pyrrolylpyridines, some derived ring systems and their evaluation as anticancer and antioxidant agents
Rostom, Sherif A.F.,Bekhit, Adnan A.
, p. 712 - 722 (2015)
The synthesis of 18 novel pyrrolylpyridines and some derived bi-, tri- and tetracyclic ring systems using both the conventional heating and MW irradiation techniques is described. Fourteen compounds; 2-9, 10-12, 14, 17 and 18 were evaluated for their anti
A facile synthesis of some 3-cyano-1,4,6-trisubstituted-2(1H)-pyridinones and their biological evaluation as anticancer agents
Rostom, Sherif A. F.,Faidallah, Hassan M.,Al-Saadi, Mohammed S.
, p. 1260 - 1272 (2012/05/20)
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 (LC50) 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 (GI50 (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. Springer Science+Business Media, LLC 2010.
