杨幼春, 张水泉. 肿瘤化学治疗的研究——溴乙酰己烷雌酚(HL-286)的合成J. 药学学报, 1981, 16(12): 937-939.
引用本文: 杨幼春, 张水泉. 肿瘤化学治疗的研究——溴乙酰己烷雌酚(HL-286)的合成J. 药学学报, 1981, 16(12): 937-939.
Yang Youchun, Zhang Shuiquan. A STUDY ON ANTITUMOR CHEMOTHERAPEUTIC AGENTS——SYNTHESIS OF HEXOESTROL DIBROMOACETATE (HL-286)J. Acta Pharmaceutica Sinica, 1981, 16(12): 937-939.
Citation: Yang Youchun, Zhang Shuiquan. A STUDY ON ANTITUMOR CHEMOTHERAPEUTIC AGENTS——SYNTHESIS OF HEXOESTROL DIBROMOACETATE (HL-286)J. Acta Pharmaceutica Sinica, 1981, 16(12): 937-939.

肿瘤化学治疗的研究——溴乙酰己烷雌酚(HL-286)的合成

A STUDY ON ANTITUMOR CHEMOTHERAPEUTIC AGENTS——SYNTHESIS OF HEXOESTROL DIBROMOACETATE (HL-286)

  • Abstract: Hexoestrol dibromoacetate (HL-286) -meso 3,4-bis- (P-bromoacetoxyphenyl)-n-hexane (Ⅴ), a novel compound of non-steroid oestrogen was synthesized. According to known methods, compounds Ⅱ~Ⅳ was synthesized.Compound Ⅴ was synthesized from Ⅳ by condensation with bromoacetyl bromide in 8.2% overall yield. This compound was shown to have potent inhibitory action on mice tumour S-180,S-37 and U-14.Preliminary clinical trials on 78 patients with prostate cancer showed promising results. Hexoestrol dibromoacetate has been recommended for clinical.

     

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