作为潜在肿瘤抑制剂的单官能和双官能α-亚甲基内酯系统的合成。

Synthesis of mono- and bifunctional alpha-methylene lactone systems as potential tumor inhibitors.

作者信息

Grieco P A, Noguez J A, Masaki Y, Hiroi Y, Nishizawa M, Rosowsky A, Oppenheim S, Lazarus H

出版信息

J Med Chem. 1977 Jan;20(1):71-6. doi: 10.1021/jm00211a014.

Abstract

Synthetic nono- and bifunctional alpha-methylene lactone derivatives including deoxyvernolepin and kihydrodeoxyvernolepin were tested as inhibitors of the growth of CCRF-CEM human lymphoblastic leukemia cells in culture. The range of ID-50 values for compounds 1-7 (ca. 10(-5)-10(-6)M) was roughly comparable to the doses observed earlier in the CCRF-CEM cell system with synthetic alpha-methylene-gamma-butyrolactones. Of significance is that dihydrodeoxyvernolepin and deoxyvernolepin were at least an order of magnitude more active than natural vernolepin.

摘要

合成的单官能团和双官能团α-亚甲基内酯衍生物，包括脱氧斑鸠菊素和二氢脱氧斑鸠菊素，作为CCRF-CEM人淋巴细胞白血病细胞在培养中的生长抑制剂进行了测试。化合物1-7的半数抑制浓度（ID-50）值范围（约10^(-5)-10^(-6)M）与早期在CCRF-CEM细胞系统中使用合成α-亚甲基-γ-丁内酯观察到的剂量大致相当。重要的是，二氢脱氧斑鸠菊素和脱氧斑鸠菊素的活性至少比天然斑鸠菊素高一个数量级。