- Novel N-phenyl dichloroacetamide derivatives as anticancer reagents: Design, synthesis and biological evaluation
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A current study shows that sodium dichloroacetate (DCA) can induce cancer cell apoptosis and inhibit tumor growth, but its cytotoxic activity is low (IC50 > 1000 μM for A549). In this paper, a variety of DCA derivatives were synthesized, and their cytotoxic activities were evaluated. The result showed that the N-phenyl-2,2-dichloroacetamide analogues had satisfactory potencies. Among them, N-(3-iodophenyl)-2,2-dichloroacetamide (3e), an optimized lead compound, has an IC50 against A549 as low as 4.76 μM. Furthermore, it can induce cancer cell apoptosis and has a low toxicity in mice (LD50 = 1117 mg/kg). N-phenyl-2,2-dichloroacetamide analogues has higher cytotoxic activity and N-(3-iodophenyl)-2,2-dichloroacetamide (3e) is an optimized lead compound.
- Yang, Yongchong,Shang, Peihua,Cheng, Changmei,Wang, Dongchun,Yang, Ping,Zhang, Feng,Li, Tianwen,Lu, Aijun,Zhao, Yufen
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experimental part
p. 4300 - 4306
(2010/10/02)
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- SUBSTITUTED DIPHENYL ISOXAZOLES, PYRAZOLES AND OXADIAZOLES USEFUL FOR TREATING HCV INFECTION
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The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.
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- HETEROCYCLIC COMPOUNDS AND HYDRO ISOMERS THEREOF
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The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.
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- Substituted diphenyl heterocycles useful for treating HCV infection
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The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV re
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