Discovery of Novel Tricyclic Thiazepine Derivatives as Anti-Drug-Resistant Cancer Agents by Combining Diversity-Oriented Synthesis and Converging Screening Approach
An efficient discovery strategy by combining diversity-oriented synthesis and converging cellular screening is described. By a three-round screening process, we identified novel tricyclic pyrido[2,3-b][1,4]benzothiazepines showing potent inhibitory activity against paclitaxel-resistant cell line H460TaxR (EC50 50 > 100 μM against normal human fibroblasts). The most active hits also exhibited drug-like properties suitable for further preclinical research. This redeployment of antidepressing compounds for anticancer applications provides promising future prospects for treating drug-resistant tumors with fewer side effects.
Nucleophilic substitutions at the pyridine ring. Conformational preference of the products and kinetics of the reactions of 2-chloro-3-nitro- and 2-chloro-5-nitro-pyridines with arenethiolates
The reactions of 2-chloro-3-nitropyridine 1 and 2-chloro-5-nitropyridine 2 with arenethiolates 3a-i result in arylthio-dechlorination to give 2-arylthio-3-nitropyridines 4a-i and 2-arylthio-5-nitropyridines 5a-i. A 1H NMR study and AM1 calculat
Hamed, Ezzat A.,El-Bardan, Ali A.,Saad, Esmat F.,Gohar, Gamal A.,Hassan, Ghada M.
p. 2415 - 2421
(2007/10/03)
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