分别以2-甲基-5-硝基苯甲酸、2-氯-5-硝基苯甲酸为原料,经羧基氯化、Friedel-Crafts酰基化、羰基还原、硝基还原和还原胺化反应合成了4种新型的1,2-O-异丙叉基-5-芳氨基代-α-呋喃葡萄糖衍生物.利用IR、NMR和HRMS等技术手段对反应所及中间体及目标化合物进行了结构测定和表征,并采用MTT法将目标化合物对3种人体肿瘤细胞的抗肿瘤活性进行了初步评价.结果表明,目标化合物1a1对肿瘤细胞的生长抑制作用优于其它3种目标化合物,特别是对A431细胞表现出更明显的生长抑制活性(IC50:(6.54±1.34) μmol/L).
参考文献
| [1] | Shang,H.;Chen,H.;Zhao,D.;Tang,X.;Liu,Y.;Pan,L.;Cheng,M..Synthesis and biological evaluation of 4α/4β-imidazolyl podophyllotoxin analogues as antitumor agents[J].Archiv der Pharmazie,20121(1):43-48. |
| [2] | 尚海;潘莉;杨澍;陈虹;程卯生.微管蛋白抑制剂的研究进展[J].药学学报,2010(9):1078-1088. |
| [3] | 李耀武;周有骏;朱驹;郑灿辉;陈军;盛春泉;吕加国;唐辉;栗亚男;张珏.作用于秋水仙碱位点的微管蛋白抑制剂的结合模式研究与结构模型的构建[J].化学学报,2008(14):1735-1739. |
| [4] | 任晓岚;汪鑫;李志裕;尤启冬.表皮生长因子受体（EGFR）酪氨酸激酶抑制剂的研究进展[J].中国新药杂志,2005(7):821-826. |
| [5] | Laskin JJ;Sandler AB.Epidermal growth factor receptor: a promising target in solid tumours.[J].Cancer Treatment Reviews,20041(1):1-17. |
| [6] | Vlahovic G;Crawford J.Activation of tyrosine kinases in cancer.[J].The oncologist,20036(6):531-538. |
| [7] | Ravaud A;Hawkins R;Gardner JP;von-der-Maase H;Zantl N;Harper P;Rolland F;Audhuy B;Machiels JP;Petavy F;Gore M;Schoffski P;El-Hariry I.Lapatinib versus hormone therapy in patients with advanced renal cell carcinoma: a randomized phase III clinical trial.[J].Journal of Clinical Oncology,200814(14):2285-2291. |
| [8] | Sato,T.;Watanabe,H.;Tsuganezawa,K.;Yuki,H.;Mikuni,J.;Yoshikawa,S.;Kukimoto-Niino,M.;Fujimoto,T.;Terazawa,Y.;Wakiyama,M.;Kojima,H.;Okabe,T.;Nagano,T.;Shirouzu,M.;Yokoyama,S.;Tanaka,A.;Honma,T..Identification of novel drug-resistant EGFR mutant inhibitors by in silico screening using comprehensive assessments of protein structures[J].Bioorganic and medicinal chemistry,201212(12):3756-3767. |
| [9] | Morphy, R.Selectively Nonselective Kinase Inhibition: Striking the Right Balance[J].Journal of Medicinal Chemistry,20104(4):1413-1437. |
| [10] | 高宏亮;王留昌;徐宏江;张喜全;刘仁杰;李宝林.4-苯胺喹唑啉类化合物的合成与抗癌活性初步研究[J].化学通报（印刷版）,2014(10):974-979. |
| [11] | Gong, S.W.;He, H.F.;Zhao, Ch.Q.;Liu, L.J.;Cui, Q.X..Convenient deoxygenation of aromatic ketones by silica-supported chitosan schiff base palladium catalyst[J].Synthetic Communications,20124/6(4/6):574-581. |
| [12] | Zuidema, D.R.;Williams, S.L.;Wert, K.J.;Bosma, K.J.;Smith, A.L.;Mebane, R.C..Deoxygenation of aromatic ketones using transfer hydrogenolysis with Raney nickel in 2-propanol[J].Synthetic Communications,201119/21(19/21):2927-2931. |
| [13] | Federica Zaccheria;Nicoletta Ravasio;Mauro Ercoli;Pietro Allegrini.Heterogeneous Cu-catalysts for the reductive deoxygenation of aromatic ketones without additives[J].Tetrahedron letters: The International Journal for the Rapid Publication of Preliminary Communications in Organic Chemistry,200545(45):7743-7745. |
| [14] | 孙键;李娇毅;张喜全;顾红梅;杨玲;李宝林.抗肿瘤药物吉非替尼的合成方法研究[J].化学研究与应用,2013(8):1180-1184. |
上一张
下一张
上一张
下一张
计量
- 下载量()
- 访问量()
文章评分
- 您的评分：
-
10%
-
20%
-
30%
-
40%
-
50%