西北药学杂志
西北藥學雜誌
서북약학잡지
2011年
4期
288-291
,共4页
甾体骨架%噻唑烷二酮%脑文阁缩合%仿生合成%抗肿瘤
甾體骨架%噻唑烷二酮%腦文閣縮閤%倣生閤成%抗腫瘤
치체골가%새서완이동%뇌문각축합%방생합성%항종류
steroid%thiazolidinedione%knoevenagel condensation%biomimetic reduction%anti-neoplastics
目的 合成17-取代甾体衍生物,寻找具有抗肿瘤活性的先导化合物.方法 通过骨架迁跃的方法设计了一种结构新型的17-噻唑烷酮取代甾体生物缀合物,目标化合物由商业易得的原料经三步有效反应合成得到,其中涉及到一步生物催化的仿生合成.结果 所得目标化合物和中间体未见文献报道,所有新化合物的化学结构经IR,1H-NMR,13C-NMR,MS 和元素分析等波谱解析验证.结论 该噻唑烷酮-甾体生物缀合物具有一定的类药性,且合成方法简单,值得进一步的结构修饰和开发.
目的 閤成17-取代甾體衍生物,尋找具有抗腫瘤活性的先導化閤物.方法 通過骨架遷躍的方法設計瞭一種結構新型的17-噻唑烷酮取代甾體生物綴閤物,目標化閤物由商業易得的原料經三步有效反應閤成得到,其中涉及到一步生物催化的倣生閤成.結果 所得目標化閤物和中間體未見文獻報道,所有新化閤物的化學結構經IR,1H-NMR,13C-NMR,MS 和元素分析等波譜解析驗證.結論 該噻唑烷酮-甾體生物綴閤物具有一定的類藥性,且閤成方法簡單,值得進一步的結構脩飾和開髮.
목적 합성17-취대치체연생물,심조구유항종류활성적선도화합물.방법 통과골가천약적방법설계료일충결구신형적17-새서완동취대치체생물철합물,목표화합물유상업역득적원료경삼보유효반응합성득도,기중섭급도일보생물최화적방생합성.결과 소득목표화합물화중간체미견문헌보도,소유신화합물적화학결구경IR,1H-NMR,13C-NMR,MS 화원소분석등파보해석험증.결론 해새서완동-치체생물철합물구유일정적류약성,차합성방법간단,치득진일보적결구수식화개발.
Objective To obtain new 17-substituted steroidal derivatives as the possible anti-neoplastic drug candidates.Methods 17-(1,3-thiazolidinedione-5-yl)-steroidal bioconjugate was designed by the method of scaffold hopping and was synthesized from commercially available material via three efficient steps including one biomimetic step of reaction.Result Both the intermediate and target molecule were reported for the first time.The structures of the all these new compounds have been verified by spectral analysis,such as IR,1H-NMR,13C-NMR,MS and elemental analysis.Conclusion The synthetic method and drug-like properties of the target compound might be promising for further development.
