Novel furoxan-based nitric oxide-releasing derivatives 6a-p of hydroxylcinnamic acids were synthesized by coupling the carboxyl group of hydroxylcinnamic acids with furoxan through various alkylol amines.Compounds 6a,...Novel furoxan-based nitric oxide-releasing derivatives 6a-p of hydroxylcinnamic acids were synthesized by coupling the carboxyl group of hydroxylcinnamic acids with furoxan through various alkylol amines.Compounds 6a,e-i and m-p displayed more potent anti-tumor activities superior to control 5-fluorouracil（5-FU） in most cancer cells tested.Furthermore,6f could selectively inhibit tumor cells,but not non-tumor cell proliferation.This inhibition was attributed to high levels of NO released in cancer cells and potentially synergistic effect of NO donor moieties and the bioactivity of hydroxylcinnamic acids.展开更多
New pyrimidine nucleoside derivatives with nitric oxide（NO） donor were systematically synthesized.The antivirus activities of these nucleoside analogues against vesicular stomatitis virus（VSV） in Wish cell were ev...New pyrimidine nucleoside derivatives with nitric oxide（NO） donor were systematically synthesized.The antivirus activities of these nucleoside analogues against vesicular stomatitis virus（VSV） in Wish cell were evaluated.It was demonstrated that most of compounds had stronger antiviral acitivity than acyclovir,while their toxicities were similar or lower to acyclovir.展开更多
Two novel energetic compounds, 3,4-bis（1＇,2＇,4＇-triazole-3＇-yl）furoxan （BTAF） and 3,4-bis（1＇-nitro-l＇,2＇,4＇-tri- azole-3＇-yl）furoxan （BNTAF）, were prepared and their structures were characterized by I...Two novel energetic compounds, 3,4-bis（1＇,2＇,4＇-triazole-3＇-yl）furoxan （BTAF） and 3,4-bis（1＇-nitro-l＇,2＇,4＇-tri- azole-3＇-yl）furoxan （BNTAF）, were prepared and their structures were characterized by IR, ^1H NMR, ^13C NMR, MS techniques and elemental analysis. The properties of BTAF and BNTAF were estimated. The predicted per- formance data of BTAF are as follows： density （measured） is 1.75 g/cm3, nitrogen content 50.9%, detonation veloc- ity 7277 m/s, detonation pressure 20.1 GPa and enthalpy of formation ＋419.7 kJ/mol. The predicted performance data of BNTAF are as follows： density is 1.84 g/cm3, nitrogen content 45.2%, enthalpy of formation ＋841.5 kJ/mol, detonation velocity 8490 rn/s and detonation pressure 32.4 GPa. The main themal properties of BTAF and BNTAF were analyzed by DSC and TG techniques, the results show that BTAF melts with concomitant decompo- sition at 188.8℃, the melting point of BNTAF is at 99.2 ℃ and its first decomposition temperature is 139.2 ℃.展开更多
A series of furoxan-based nitric oxide-releasing matrine derivatives(10a-f) were synthesized.The biological evaluation showed that compounds 10a,10b,10e and 10f had stronger cytotoxic activities than 5-fluorouracil ag...A series of furoxan-based nitric oxide-releasing matrine derivatives(10a-f) were synthesized.The biological evaluation showed that compounds 10a,10b,10e and 10f had stronger cytotoxic activities than 5-fluorouracil against human hepatoma cells(HepG2) in vitro.展开更多
A series of novel nitric oxide-donating sixalkoxyl biphenyl derivatives （14a-1） were synthesized by coupling furoxan with alkoxyl biphenyl skeleton using amino acids as the spacers, and their cytotoxicity against He...A series of novel nitric oxide-donating sixalkoxyl biphenyl derivatives （14a-1） were synthesized by coupling furoxan with alkoxyl biphenyl skeleton using amino acids as the spacers, and their cytotoxicity against HepG2 cells in vitro were evaluated by MTT method. It was found that 14c, 14d, 14f, 14i, 14j and 14k showed more potent cytotoxic activities than control 5-fluorouracil. NO release assay of target compounds indicated that the maximum amount of NO released by most active compounds 14c and 14j was about 6 × 10^-2 μmol/L, whereas 14a and 14h with very weak activity only released NO of 1 × 10^-2 μmol/L.展开更多
文摘Novel furoxan-based nitric oxide-releasing derivatives 6a-p of hydroxylcinnamic acids were synthesized by coupling the carboxyl group of hydroxylcinnamic acids with furoxan through various alkylol amines.Compounds 6a,e-i and m-p displayed more potent anti-tumor activities superior to control 5-fluorouracil（5-FU） in most cancer cells tested.Furthermore,6f could selectively inhibit tumor cells,but not non-tumor cell proliferation.This inhibition was attributed to high levels of NO released in cancer cells and potentially synergistic effect of NO donor moieties and the bioactivity of hydroxylcinnamic acids.
基金the National Natural Science Foundation of China(No.30572240)
文摘New pyrimidine nucleoside derivatives with nitric oxide（NO） donor were systematically synthesized.The antivirus activities of these nucleoside analogues against vesicular stomatitis virus（VSV） in Wish cell were evaluated.It was demonstrated that most of compounds had stronger antiviral acitivity than acyclovir,while their toxicities were similar or lower to acyclovir.
文摘Two novel energetic compounds, 3,4-bis（1＇,2＇,4＇-triazole-3＇-yl）furoxan （BTAF） and 3,4-bis（1＇-nitro-l＇,2＇,4＇-tri- azole-3＇-yl）furoxan （BNTAF）, were prepared and their structures were characterized by IR, ^1H NMR, ^13C NMR, MS techniques and elemental analysis. The properties of BTAF and BNTAF were estimated. The predicted per- formance data of BTAF are as follows： density （measured） is 1.75 g/cm3, nitrogen content 50.9%, detonation veloc- ity 7277 m/s, detonation pressure 20.1 GPa and enthalpy of formation ＋419.7 kJ/mol. The predicted performance data of BNTAF are as follows： density is 1.84 g/cm3, nitrogen content 45.2%, enthalpy of formation ＋841.5 kJ/mol, detonation velocity 8490 rn/s and detonation pressure 32.4 GPa. The main themal properties of BTAF and BNTAF were analyzed by DSC and TG techniques, the results show that BTAF melts with concomitant decompo- sition at 188.8℃, the melting point of BNTAF is at 99.2 ℃ and its first decomposition temperature is 139.2 ℃.
文摘A series of furoxan-based nitric oxide-releasing matrine derivatives(10a-f) were synthesized.The biological evaluation showed that compounds 10a,10b,10e and 10f had stronger cytotoxic activities than 5-fluorouracil against human hepatoma cells(HepG2) in vitro.
文摘A series of novel nitric oxide-donating sixalkoxyl biphenyl derivatives （14a-1） were synthesized by coupling furoxan with alkoxyl biphenyl skeleton using amino acids as the spacers, and their cytotoxicity against HepG2 cells in vitro were evaluated by MTT method. It was found that 14c, 14d, 14f, 14i, 14j and 14k showed more potent cytotoxic activities than control 5-fluorouracil. NO release assay of target compounds indicated that the maximum amount of NO released by most active compounds 14c and 14j was about 6 × 10^-2 μmol/L, whereas 14a and 14h with very weak activity only released NO of 1 × 10^-2 μmol/L.
