以2-硝基苯磺酰氯为起始原料,经多步反应合成了12种新型1,1-二氧代-4H-苯并[1,2,4]-噻二嗪类衍生物,产物收率高,水溶性好,并经1H NMR、13C NMR、MS-ESI和元素分析法确证结构.用MTT法测试了这类衍生物对肝癌细胞HepG-2生长的抑制作用,结果显示目标化合物能不同程度地抑制肿瘤细胞生长,其中7-氨甲基-3-环丙基-1,1-二氧代-4H-苯并[1,2,4]-噻二嗪(7c)对肝癌细胞HepG-2的抗性显著,最高抑制率达到79.3％.
参考文献
| [1] | Boverie S;Antoine MH;Somers F;Becker B;Sebille S;Ouedraogo R;Counerotte S;Pirotte B;Lebrun P;de Tullio P.Effect on K-ATP channel activation properties and tissue selectivity of the nature of the substituent in the 7-and the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides[J].Journal of Medicinal Chemistry,200510(10):3492-3503. |
| [2] | Shaw AN;Tedesco R;Bambal R.Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase.[J].Bioorganic and Medicinal Chemistry Letters,200915(15):4350-4353. |
| [3] | de Tullio P.;Somers F.;Boverie S.;Lacan F.;Delarge J.;Pirotte B..Study of the ring closure reaction of o-aminoarylsulfonamides with 1,1 '-thiocarbonyldiimidazole.[J].Tetrahedron,199819(19):4935-4942. |
| [4] | Flemming E. Nielsen;Thora B. Bodvarsdottir;Anne Worsaae;Peter MacKay;Carsten E. Stidsen;Harrie C. M. Boonen;Lone Pridal;Per O. G. Arkhammar;Philip Wahl;Lars Ynddal.6-Chloro-3-alkylamino-4H-thieno[3,2-e-1,2,4-thiadiazine 1,1-Dioxide Derivatives Potently and Selectively Activate ATP Sensitive Potassium Channels of Pancreatic β-Cells[J].Journal of Medicinal Chemistry,200219(19):4171-4187. |
| [5] | Chen, X.;Zhu, C.;Guo, F.;Qiu, X.;Yang, Y.;Zhang, S.;He, M.;Parveen, S.;Jing, C.;Li, Y.;Ma, B..Acetic acid derivatives of 3,4-dihydro-2 H-1,2,4-benzothiadiazine 1,1-dioxide as a novel class of potent aldose reductase inhibitors[J].Journal of Medicinal Chemistry,201023(23):8330-8344. |
| [6] | 杨雷;范良华;赵丹丹;戚斌斌;甘春芳;崔建国;黄燕敏.22-降-豆甾-22-含氮化合物的合成及抗肿瘤活性[J].应用化学,2015(3):273-277. |
| [7] | 关松磊;胡秀丽;刘忠英;宋凤瑞;刘志强.姜黄素联合顺铂对卵巢癌细胞COC1的体外抗肿瘤作用[J].应用化学,2011(9):1022-1027. |
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