5,7—二羟基—3‘,4’—二甲氧基及3‘,5—二羟基—4’,7—二甲氧基 …

以橙皮甙为原料经选择性甲基化及水解两步分别以较好收率半合成了５,７－二羟基３’,４‘－二甲氧基－及３’,５－二羟基－４’,７－二甲氧基黄烷酮,该工艺原料易得,工艺简单,收率高。     

3‘—当归酰氧基—4’—乙酰氧基—3‘,4’—双氢邪蒿内酯对麻醉犬短时…

静脉输入３＇－当归酰氧基－４＇－乙酰氧基－３＇－４＇－双氢邪蒿内酯３０ｍｉｎ对１５ｍｉｎ闭塞犬左前降枝伴３ｈ再灌注后心肌收缩功能的影响被研究。用超声微测距法测定心肌节段收缩长度表明：该药迅速改善心肌收缩功能不良，再灌后５ｍｉｎ即使ＳＳ％恢复到用药前的４１±５１％，对血流动力学无明显影响。     

4—（4“—（2”,2“,6”,6“—四甲基哌啶氮氧自由基）...

The antitumor activity of GP-7, a new spin-labeled epipodophyllotoxin, was studied by liquid scintillation spectrometry. There were many similarities between GP-7 and etoposide. Both GP-7 and etoposide inhibited the incorporation of [3H]TdR, [3H]UR, and [3H]Leu into DNA, RNA, and protein synthesis in leukemia 7712 cells. The inhibition correlated with drug concentration and duration. IC50 of GP-7 and etoposide on DNA synthesis at 24 h were 0.21 and 0.37 micrograms.ml-1, respectively. The inhibition of GP-7 or etoposide on DNA synthesis retained even after the drug were washed out for 3 h. GP-7 and etoposide caused DNA single-strand breaks, with a well concentration-response relationship. These data suggest that the inhibition of DNA synthesis by GP-7 or etoposide is likely due to the damage of DNA template and breaking of single-strand DNA.     

2,6—哌嗪二酮类抗肿瘤药物的研究1—取代苯基—4—（2‘,3’—二乙酰…

本文设计合成了１１个１－取代苯基－４－（２’，３’－二乙酰氧基－５’－甲氧羰基苄基）－２，６－哌嗪二酮类化合物，并经过小鼠白血病细胞Ｐ３８８、小鼠肝癌细胞Ｈｅｐ和人体胃癌细胞ＳＧＣ７９０１的体外实验表明，化合物９ｊ对Ｐ３８８白血病细胞有较强的抑制作用，化合物９ｄ对Ｈｅｐ肝癌细胞有较强的抑制作用，本文还考察了超声波辐射时间对Ｍａｎｎｉｃｈ反应的影响。     

2—ASG —3—（3‘,5’—双吗啉甲基—4‘—羟基）—苯甲酰吲哚（HWL—12）逆转肿…

AIM: To explore the reversal of multidrug resistance (MDR) by indole derivative HWL-12. METHODS: Cytotoxicity was determined by tetrazolium (MTT) assay. The function of P-gp was examined by Fura 2-AM assay. Cellular accumulation of doxorubicin (Dox) was measured by fluorescence spectrophotometry. RESULTS: HWL-12 10 mumol.L-1 markedly increased Fura-2 accumulation and was 17.2-fold reversal of MDR in MCF-7/ADR cells. The cellular Dox accumulation in MDR cells was increased in the presence of HWL-12 on the MCF-7/ADR cells. No effect was observed for Dox accumulation in the presence of high Ca2+ (addition of CaCl2) or low Ca2+ (addition of egtazic acid). CONCLUSION: HWL-12 has a potent MDR reversal action which was associated with the increase of cellular Dox accumulation in MDR cells and not related with calcium ion concentration.     

（1‘R,2S,2’S）—2—（2—甲基—2—溴甲基—3—亚甲基）环戊基丙酸的合成

以商业易得的（＋）－内向３－溴莰酮－２为手性源合成了光学活性的（１’Ｒ,２Ｓ,２‘Ｓ）－２－（２－溴甲基－２－甲基－３－亚甲基）环戊基丙酸。     

由2，4，6—三硝基甲苯高选择性合成2—氨基—4，6—二硝基甲苯（1）、2，6—二氨基—4—硝基甲苯（2）或2，4，6—三氨基甲苯（3）

伯胺在无水 DMF中 ,与 CO2 、卤代烷、Cs2 CO3、TBAI反应 ,得 N ,N -二烷基氨基甲酸酯 ,3例收率 80 %～ 87%。如反应前后阶段加不同卤代烷 ,则得到不同烷基取代的氨基甲酸酯 ,11例收率 5 6 %～ 92 %。由伯胺和卤代烷制备N-烷基氨基甲酸酯@谭璨     

N^4—烷基—5—甲基—2‘—脱氧胞苷的合成

3‘,5‘-O-二苯甲酰胸苷在三氯氧磷存在的条件下与1,2,4-三唑缩合可得到1-（3‘,5‘-O-二苯甲酰-β-D-呋喃核糖）-4-（1,2,4-三唑-1-基）-5-甲基-嘧啶-2-（1H）-酮,再用不同的胺取代核苷C4上的三唑基团可制备一系列全新的N^4-烷基取代的5-甲基胞苷。方法简便,收率高。