引用本文:
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. Synthesis and antitumor evaluation of fluoroquinolone C3 fused heterocycles (Ⅱ):From triazolothiadiazines to pyrazolotriazoles[J]. Chinese Chemical Letters,
2011, 22(7): 804-806.
doi:
10.1016/j.cclet.2011.01.018
Citation: 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. Synthesis and antitumor evaluation of fluoroquinolone C3 fused heterocycles (Ⅱ):From triazolothiadiazines to pyrazolotriazoles[J]. Chinese Chemical Letters, 2011, 22(7): 804-806. doi: 10.1016/j.cclet.2011.01.018
Citation: 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. Synthesis and antitumor evaluation of fluoroquinolone C3 fused heterocycles (Ⅱ):From triazolothiadiazines to pyrazolotriazoles[J]. Chinese Chemical Letters, 2011, 22(7): 804-806. doi: 10.1016/j.cclet.2011.01.018
Synthesis and antitumor evaluation of fluoroquinolone C3 fused heterocycles (Ⅱ):From triazolothiadiazines to pyrazolotriazoles
摘要:
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, [l,2,4]triazolo[3,4-b][l,3,4]thiadiazine and pyrazolo[5,l-c][l,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.
English
Synthesis and antitumor evaluation of fluoroquinolone C3 fused heterocycles (Ⅱ):From triazolothiadiazines to pyrazolotriazoles
Abstract:
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, [l,2,4]triazolo[3,4-b][l,3,4]thiadiazine and pyrazolo[5,l-c][l,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.
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Key words:
- Heterocyclic compounds
- / Bretschneiderazines
- / Directed lithiation
- / Synthesis
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