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在寻找能够提高治疗指数和降低毒性的蒽环类化合物的过程中。在氨基糖的4’位置用卤素替代的卤化蒽环化合物最近业已合成,其中4’-碘-4’-脱氧阿霉素(IDX)有明显的抗实验性肿瘤的作用。体外实验中,IDX对一组人和鼠的瘤细胞株的作用比阿霉素(DX)强。体内实验时,IDX的抗瘤谱与母体药物相似。IDX对小鼠的心脏毒性亦比DX小。在目前的研究中,我们通过一种体外测定法比较了IDX和DX在人体结肠一直肠癌活体检查样品的作用。这种测定法已证明具有瘤种特异性以及预测临床疗效的可靠性,并已被应用于第Ⅱ期的体外研究。
In looking for the treatment index and reduce the toxicity of anthracyclines in the process. Halogenated anthracycline compounds have recently been synthesized at the 4 ’position of the amino sugar, with 4’-iodo-4’-deoxy doxorubicin (IDX) having a clear anti-experimental tumor effect. In vitro, IDX exerted a stronger effect on doxorubicin (DX) against a panel of human and murine tumor cell lines. In vivo experiments, IDX anti-tumor spectrum and the parent drug similar. IDX is also less toxic to mice than DX. In the present study, we compared the role of IDX and DX in biopsy samples of human colorectal cancer by an in vitro assay. This assay has demonstrated tumor-specific specificity and predicts the reliability of clinical efficacy and has been used in Phase II in vitro studies.