A series of novel uracil and 5-fluorouracil-l-yl-acetic acid-colchicine derivatives（6a--6n） was synthe- sized via coupling and 5-fluorouracil（5-FU） with C-10 analogues of colchicine. The antitumor activities of th...A series of novel uracil and 5-fluorouracil-l-yl-acetic acid-colchicine derivatives（6a--6n） was synthe- sized via coupling and 5-fluorouracil（5-FU） with C-10 analogues of colchicine. The antitumor activities of the target compounds against human hepatocellular earcinoma（BEL7402） cells, human ovary carcinoma（A2780） cells, human lung adenocarcinoma（A549） cells and human breast carcinoma（MCF7） cells were tested in vitro, and the structure-activity relationship（SAR） of the compounds was also studied. The bioassay results demonstrate that most of the tested compounds display significant activity and particularly, compounds 6a, 6e, 6h and 61 show more potent cytotoxic activities than 5-fluorouracil and colchicine. The results show that the new derivatives of colchicine are potential suppressors on human cancer.展开更多
1,3-bis[5-(4-ethyoxycarbonyl)phenyl-10,15,20-tri(4-chlorophenyl)porphyrin]-5-fluorouracil(A),1-[5-(4-ethoxycarbonyl)phenyl-10,15,20-tri(4-chlorophenyl)porphyrin]-5-fluorouracil(B) are synthesized.Their structures are ...1,3-bis[5-(4-ethyoxycarbonyl)phenyl-10,15,20-tri(4-chlorophenyl)porphyrin]-5-fluorouracil(A),1-[5-(4-ethoxycarbonyl)phenyl-10,15,20-tri(4-chlorophenyl)porphyrin]-5-fluorouracil(B) are synthesized.Their structures are characterized by UV-Vis,IR,1HNMR and MS.The synthesis and separation conditions of the target compounds are studied.The results show that the yield is higher when DMF is used as the solvent at 115 ℃ for 11 h.The products are separated via column chroma to graphy with silica gel(200-300) separation is more satisfactory as the eluent when the column is 3 cm in diameter and 12 cm in height.展开更多
文摘[目的]评价5氟脲嘧啶(5-F luorourac il,5Fu)关节腔注射治疗兔膝骨性关节炎(osteoarthritis,OA)的疗效。[方法]24只兔子制成骨关节炎模型随机分成OA组、5Fu组和对照组,OA组立即处死,5Fu组按5Fu 2mg/kg关节腔注射,每周1次连续4次,对照组注射等量生理盐水,最后1次治疗后1周处死。观察3组滑膜组织的光镜、电镜改变及软骨的光镜、MMP-1免疫组化改变,比较软骨M ank in s评分及关节液中IL-1的浓度。[结果]5Fu组可见软骨破坏减轻,滑膜炎症明显抑制,M ank in s评分明显改善(P<0.01);关节液IL-1浓度降低(P<0.05),关节软骨中MMP-1表达减弱。[结论]5Fu关节腔内注射能抑制滑膜炎症,缓解软骨的破坏。
文摘A series of novel uracil and 5-fluorouracil-l-yl-acetic acid-colchicine derivatives（6a--6n） was synthe- sized via coupling and 5-fluorouracil（5-FU） with C-10 analogues of colchicine. The antitumor activities of the target compounds against human hepatocellular earcinoma（BEL7402） cells, human ovary carcinoma（A2780） cells, human lung adenocarcinoma（A549） cells and human breast carcinoma（MCF7） cells were tested in vitro, and the structure-activity relationship（SAR） of the compounds was also studied. The bioassay results demonstrate that most of the tested compounds display significant activity and particularly, compounds 6a, 6e, 6h and 61 show more potent cytotoxic activities than 5-fluorouracil and colchicine. The results show that the new derivatives of colchicine are potential suppressors on human cancer.
文摘1,3-bis[5-(4-ethyoxycarbonyl)phenyl-10,15,20-tri(4-chlorophenyl)porphyrin]-5-fluorouracil(A),1-[5-(4-ethoxycarbonyl)phenyl-10,15,20-tri(4-chlorophenyl)porphyrin]-5-fluorouracil(B) are synthesized.Their structures are characterized by UV-Vis,IR,1HNMR and MS.The synthesis and separation conditions of the target compounds are studied.The results show that the yield is higher when DMF is used as the solvent at 115 ℃ for 11 h.The products are separated via column chroma to graphy with silica gel(200-300) separation is more satisfactory as the eluent when the column is 3 cm in diameter and 12 cm in height.
