化学研究与应用
化學研究與應用
화학연구여응용
CHEMICAL RESEARCH AND APPLICATION
2015年
5期
665-670
,共6页
戚斌斌%刘亮%赵丹丹%杨雷%甘春芳%黄燕敏%崔建国
慼斌斌%劉亮%趙丹丹%楊雷%甘春芳%黃燕敏%崔建國
척빈빈%류량%조단단%양뢰%감춘방%황연민%최건국
甾酮%甾体腙化合物%甾体芳杂环化合物%抗肿瘤活性
甾酮%甾體腙化閤物%甾體芳雜環化閤物%抗腫瘤活性
치동%치체종화합물%치체방잡배화합물%항종류활성
steroidal ketone%steroidal hydrazones%steroidal aromatic heterocycles%antiproliferative acitivity
甾体类药物由于其特有的生理活性而被广泛应用于各种疾病的治疗。本文采用一锅法及分步合成法,通过胆甾-4-烯-3,6-二酮及22-降-3β-羟基胆甾-5-烯-22醛与水合肼反应,然后进一步与不同的芳香醛反应,合成了5个新的具有不同结构特征的甾体芳杂环腙化合物,合成物经IR、NMR及HRMS进行结构表征。同时对合成物进行了体外抑制肿瘤细胞生长增殖活性测试。
甾體類藥物由于其特有的生理活性而被廣汎應用于各種疾病的治療。本文採用一鍋法及分步閤成法,通過膽甾-4-烯-3,6-二酮及22-降-3β-羥基膽甾-5-烯-22醛與水閤肼反應,然後進一步與不同的芳香醛反應,閤成瞭5箇新的具有不同結構特徵的甾體芳雜環腙化閤物,閤成物經IR、NMR及HRMS進行結構錶徵。同時對閤成物進行瞭體外抑製腫瘤細胞生長增殖活性測試。
치체류약물유우기특유적생리활성이피엄범응용우각충질병적치료。본문채용일과법급분보합성법,통과담치-4-희-3,6-이동급22-강-3β-간기담치-5-희-22철여수합정반응,연후진일보여불동적방향철반응,합성료5개신적구유불동결구특정적치체방잡배종화합물,합성물경IR、NMR급HRMS진행결구표정。동시대합성물진행료체외억제종류세포생장증식활성측시。
The steroidal drugs were widely applied in the cure of various diseases because of their special bioactivity. Using cholest-4-en-3,6-dione and 22-seco-3β-hydroxycholest-5-en-22-al as starting materials,some steroidal aromatic heterocycle hydrazones were synthesized by the reaction with hydrazine hydrate and various aromatic aldehydes. The structures of all compounds were character-ized by IR,NMR and MS. The antiproliferative activity of compounds was evaluated against human gastric cancer(SGC-7901)and human liver cancer(Bel-7404)cells.