Chin. J. Org. Chem. ›› 2010, Vol. 30 ›› Issue (9): 1395-1399. Previous Articles     Next Articles

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新雌激素衍生物的合成及抗辐射升白生物活性

周则卫*,沈秀,唐卫生,吴小霞,高建芳,巩伟民   

  1. (中国医学科学院中国协和医科大学 放射医学研究所 天津 300192)
  • 收稿日期:2009-03-30 修回日期:2010-03-02 发布日期:2010-04-20
  • 通讯作者: 周则卫 E-mail:zhouzewei666@yahoo.com.cn
  • 基金资助:

    其他

Synthesis of Novel Estrogen Derivatives & Biological Activities of Anti-radiation Promotion White Blood Cells

(Institute of Radiation Medicine, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin 300192)   

  • Received:2009-03-30 Revised:2010-03-02 Published:2010-04-20
  • Contact: ZHOU Ze-Wei E-mail:zhouzewei666@yahoo.com.cn

Four novel estrogen derivatives were synthesized by a one-step reaction with 17α-ethynylestradiol and 17β-estradiol as the initial materials, reacted with allyl bromide and isopentenyl bromide, respec-tively, obtained 17α-ethynylestradiol-3-allyl ether (ES-1), 17β-estradiol-3-allyl ether (ES-2), 17α-ethyny- lestradiol-3-isopentenyl ether (ES-3) and 17β-estradiol-3-isopentenyl ether (ES-4), in yields of 92.2%, 73.7%, 65.9% and 67.6%. And the structures of products were conformed by 1H NMR, 13C NMR, MS, IR techniques and elemental analysis. The four compounds are novel estrogens without paper reported. The initial research of biological activities on anti-radiation promotion white blood cells (WBC) were carried out, and the results suggested that the four compounds possess certain protective effects to 6.5Gy 137Cs γ-rays damages on lowered WBC and haematogenesis system function, promotion WBC effect of ES-3 with obvious preponderance was best in the four products. The effect of promotion WBC for three dosages of ES-3 administered mice, treated by statistics with very obvious difference (P<0.001) vs. control mice.

Key words: estrogen, derivative, synthesis, anti-irradiation, promotion white blood cell (WBC)

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