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
（-）-Tetrahydrolipstatin 1 was synthesized in three steps and 33.8% overall yield from aldehyde 6 by tandem Mukaiyama-aldol lactonization, which offered a concise, efficient and highly diastereoselective route to thi...（-）-Tetrahydrolipstatin 1 was synthesized in three steps and 33.8% overall yield from aldehyde 6 by tandem Mukaiyama-aldol lactonization, which offered a concise, efficient and highly diastereoselective route to this antiobesity drug. We also presented a resolution method for preparation of the crucial intermediate, β- （t-butyldimethylsilyloxy）tetradecanal.展开更多
A series of novel glyco-gambogic acid（GA） compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma（HCC） cells.All compounds showed much better ...A series of novel glyco-gambogic acid（GA） compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma（HCC） cells.All compounds showed much better aqueous solubility（0.92- 1.89 mg/mL） than GA（0.013 mg/mL）,and displayed potent inhibition on HCC cells（IC_（50）：0.21-12.23μmol/L） and little affects on non-tumor liver cells（IC_（50）：42.56-86.43μmol/L）,suggesting that glyco-GA compounds selectively inhibit HCC proliferation,and may be promising candidates for further intensive study.展开更多
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.
文摘（-）-Tetrahydrolipstatin 1 was synthesized in three steps and 33.8% overall yield from aldehyde 6 by tandem Mukaiyama-aldol lactonization, which offered a concise, efficient and highly diastereoselective route to this antiobesity drug. We also presented a resolution method for preparation of the crucial intermediate, β- （t-butyldimethylsilyloxy）tetradecanal.
基金supported by a grant from the Nature and Science Foundation of Department of Education,Anhui province(No.KJ2010A204)
文摘A series of novel glyco-gambogic acid（GA） compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma（HCC） cells.All compounds showed much better aqueous solubility（0.92- 1.89 mg/mL） than GA（0.013 mg/mL）,and displayed potent inhibition on HCC cells（IC_（50）：0.21-12.23μmol/L） and little affects on non-tumor liver cells（IC_（50）：42.56-86.43μmol/L）,suggesting that glyco-GA compounds selectively inhibit HCC proliferation,and may be promising candidates for further intensive study.
