Synthesis and Biological Evaluation of 2-(5-Nitrofuranyl)vinyl-8-hydroxyquinoline Analogues as Antit

来源 :第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会 | 被引量 : 0次 | 上传用户:liongliong426
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  Androgens influence normal prostate growth and prostate cancer(PC)mainly throughandrogen receptor(AR).Thereby,androgen ablation therapy is effective for most PC patients.However,the influence of androgen receptor gradually decreases.Eventually,PC will becomeandrogen-independent prostate cancer(AIPC).At this stage,PC will relapse intohormone-refractory or turn out to be androgen-independent.Unfortunately,no effectivechemotherapies are available for this stage.Recently,2-(5-nitrofuranyl)vinyl-8-hydroxyquinoline(HZY-2023) has already shown very strong effectagainst PC-3 cell line.Previous investigation indicates that the conjugation system isimportant to their biological activity.Based on this lead compound,series analogues withmodification at olefin group were prepared and subjected to biological activity.Meanwhile,simulation technique was also used to propose a rational mechanism to the observed result.The result will be discussed in detail.
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