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Synthesis and antitumor evaluation of fluoroquinolone C3 fused heterocycles(Ⅱ):From triazolothiadiazines to pyrazolotriazoles

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Chinese Chemical Letters 2011年第7期22卷 804-806页

作者： Guo Qiang Hu Li Li Hou Yong Yang Lei Yi Song Qiang Xie Guo Qiang Wang Nan Nan Duan Tie Yao Chao Xiao Yi Wen Wen Long Huang Institute of Chemistry & Biology Henan University Kaifeng 475001 China China Pharmaceutical University Nanjing 210009 China

To further expand an effective modified route for the shift from an antibacterial fluoroquinolone （FQ） to an antitumor FQ, two series of title compounds based on an isostere of the FQ C3 carboxylic group with two fused heterocyclic rings, [ 1,2,4]triazolo[3,4- b][1,3,4]thiadiazine and pyrazolo[5,1-c][1,2,4]triazole, respectively, were designed and synthesized starting from the current antibacterial FQs, and their in vitro antitumor activity against L1210, CHO cell lines were evaluated via their respective IC50 values.

关键词： Fluoroquinolone Triazolothiadiazine Pyrazolotriazole antitumor evaluation

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Synthesis and antitumor evaluation of C3/C3 fluoroquinolone dimers(Ⅰ):Tethered with a fused heterocyclic s-triazolo[2,1-b][1,3,4]thiadiazole

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Chinese Chemical Letters 2010年第6期21卷 -页

作者： Guo Institute of Chemistry & Biology Henan UniversityKaifeng 475001China China Pharmaceutical University Nanjing 210009China

Five C3/C3 fluoroquinolone dimers tethered with a fused heterocyclic ring of s-triazolo[2,1-b][1,3,4]thiadiazole derived from antibacterial quinoiones were synthesized and characterized,and their in vitro antitumor ac... 详细信息

关键词： Fluoroquinolone Dirtier antitumor evaluation

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Synthesis and antitumor evaluation of C3/C3 fluoroquinolone dimers(Ⅰ):Tethered with a fused heterocyclic s-triazolo[2,1-b][1,3,4]thiadiazole

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Chinese Chemical Letters 2010年第6期 661-663页

作者： Guo Qiang Hu~(a,*),Zhong Quan Zhang~a,Song Qiang Xie~a,Wen Long Huang~b a Institute of Chemistry & Biology,Henan University,Kaifeng 475001,China b China Pharmaceutical University,Nanjing 210009,China

关键词： Fluoroquinolone Dimer antitumor evaluation

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Synthesis and antitumor and antibacterial evaluation of fluoroquinolone derivatives(Ⅲ):Mono- and bis-Schiff-bases

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Chinese Chemical Letters 2012年第5期23卷 515-517页

作者： Guo Qiang Hu Xiao Kui Wu Guo Qiang Wang Nan Nan Duan Xiao Yi Wen Tie Yao Cao Yin Jun Wang Wei Song Qiang Xie Wen Long Huang Institute of Chemistry&Biology Henan UniversityKaifeng 475001China China Pharmaceutical University Nanjing 210009China

To further explore an efficient modified route for the shift from an antibacterial fluoroquinolone to an antitumor one,mono-Schiff bases 6a-6h related to ciprofloxacin C3 carbonylhydrazone and bis-Schiff bases 4a-4h corresponding to C3/C7 carbonylhydrazone/hydrazone attached on a skeleton of ciprofloquinolone were designed and synthesized,and their in vitro antitumor activity against CHO,HL60,L1210 cells and antibacterial activity against Staphylococcus aureus and Escherichia coli were also reported.

关键词： Fluoroquinolone Schiff base antitumor evaluation

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Design, synthesis and antitumor activity of C3/C3 bis-fluoroquonolones cross-linked with [1,2,4]triazolo[3,4-b] [1,3,4]thiadiazole

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Acta Pharmaceutica Sinica B 2011年第3期1卷 172-177页

作者： Guo-qiang Hu Yong Yang Lei Yi Guo-qiang Wang Nan-nan Duan Xiao-yi Wen Tie-yao Cao Song-qiang Xie Wen-Long Huang Institute of Chemistry&Biology Henan UniversityKaifeng 475001China Center of Drug Discovery China Pharmaceutical UniversityNanjing 210009China

To contribute to the development of an efficient method for the conversion of antibacterial fluoroquinolones to antitumor fluoroquinolones,a series of C3/C3 bis-fluoroquinolone fused heterocycles cross-linked with a[1,2,4]-triazolo[3,4-b][1,3,4]-thiadiazole core as a common bioisostere of two carboxylic acid groups was designed and synthesized as their hydrochloride *** were characterized by elemental analysis and spectral data and their in vitro antitumor activity against L1210,CHO and HL60 cell lines was screened by determination of their IC50 values in the methylthiazole trazolium(MTT)*** compounds were highly potent against the HL60 cell line and represent promising lead compounds for future development.

关键词： Fluoroquinolone Triazolothiadiazole Synthesis antitumor evaluation

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