Lung cancer is the major cause of cancer-related mortality, accountingfor over one quarter of cancer deaths. Lung cancers are generally divided into two main categories： SCLC （small cell lung cancer） and NSCLC （no...Lung cancer is the major cause of cancer-related mortality, accountingfor over one quarter of cancer deaths. Lung cancers are generally divided into two main categories： SCLC （small cell lung cancer） and NSCLC （non-small cell lung cancer）. NSCLC accounts for approximately 85% of all lung cancers. ALK （anaplastic largecell kinase） gene rearrangements are identified and targeted resulting in promising response rates for NSCLC in early studies. Ceritinib is a second-generation ALK inhibitor that has demonstrated activity in crizotinib （the first-generation ALK inhibitor）-resistant patients. In this paper, the synthesis, pharmacodynamics, pharmacokinetics, therapeutic trials, adverse events and drug-drug interactions are briefly overviewed in order to make more scholars, medical workers and patients have a more clear and comprehensive recognition on this drug.展开更多
A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS spectra.All the new compounds were screened for their antimicrobial activities in vitro by a twofold serial ...A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS spectra.All the new compounds were screened for their antimicrobial activities in vitro by a twofold serial dilution technique.The bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles were comparably or even more strongly antibacterial and antifungal than the reference drugs Chloromycin,Norfloxacin,and Fluconazole.The combination of2,4-difluorobenzyl benzimidazole derivative 5l and its hydrochloride 7 respectively with the antibacterials Chloromycin,Norfloxacin,and the antifungal Fluconazole was more sensitive to methicillin-resistant MRSA and Fluconazole-insensitive A.flavus.In addition,the interaction of compound 5l with calf thymus DNA demonstrated that this compound could effectively intercalate into DNA to form a compound 5l-DNA complex that might block DNA replication and thereby exert good antimicrobial activity.展开更多
文摘Lung cancer is the major cause of cancer-related mortality, accountingfor over one quarter of cancer deaths. Lung cancers are generally divided into two main categories： SCLC （small cell lung cancer） and NSCLC （non-small cell lung cancer）. NSCLC accounts for approximately 85% of all lung cancers. ALK （anaplastic largecell kinase） gene rearrangements are identified and targeted resulting in promising response rates for NSCLC in early studies. Ceritinib is a second-generation ALK inhibitor that has demonstrated activity in crizotinib （the first-generation ALK inhibitor）-resistant patients. In this paper, the synthesis, pharmacodynamics, pharmacokinetics, therapeutic trials, adverse events and drug-drug interactions are briefly overviewed in order to make more scholars, medical workers and patients have a more clear and comprehensive recognition on this drug.
基金supported by the National Natural Science Foundation of China (21172181,21372186)the Research Fellowship for International Young Scientists from the International (Regional) Cooperation and Exchange Program (81250110554,81350110338,81350110523)+1 种基金the key program from Natural Science Foundation of Chongqing (CSTC2012- jjB10026)the Specialized Research Fund for the Doctoral Program of Higher Education of China (20110182110007)
文摘A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS spectra.All the new compounds were screened for their antimicrobial activities in vitro by a twofold serial dilution technique.The bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles were comparably or even more strongly antibacterial and antifungal than the reference drugs Chloromycin,Norfloxacin,and Fluconazole.The combination of2,4-difluorobenzyl benzimidazole derivative 5l and its hydrochloride 7 respectively with the antibacterials Chloromycin,Norfloxacin,and the antifungal Fluconazole was more sensitive to methicillin-resistant MRSA and Fluconazole-insensitive A.flavus.In addition,the interaction of compound 5l with calf thymus DNA demonstrated that this compound could effectively intercalate into DNA to form a compound 5l-DNA complex that might block DNA replication and thereby exert good antimicrobial activity.
