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Design, synthesis and pharmacological evaluation of new anticancer fused pentacycles.

机译:新抗癌融合追感的设计,合成与药理评价。

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The quinoline chromophore has long formed the basis for the clinical development of novel antitumour agents. Camptothecin derivatives have already proved their clinical efficacy and compounds such as ascididemin (pyridoacridine family), DHDMC (protoberberine family) have a very promising future. During our search for new cytotoxic molecules, we have designed compounds based on the benzo[c]pyrido[2,3,4-kl]acridine skeleton which combines the structural features of ascididemin and DHDMC. Corresponding compounds were synthesized and evaluated for their cytotoxic activity against human prostatic PC-3 cell lines. Some have shown promising biological activity in inhibiting the growth of cell lines which are resistant to camptothecin.
机译:喹啉色团长期以来一直形成了新型抗肿瘤剂的临床发展的基础。 Camptothecin衍生物已经证明了它们的临床疗效和诸如亚藜(吡啶吖啶家族)的化合物,DHDMC(Protoberberine家族)具有非常有前途的未来。 在我们寻找新的细胞毒性分子期间,我们设计了基于苯并[C]吡啶的化合物[2,3,4- k1]吖啶骨架,其结合了亚啶胺蛋白和DHDMC的结构特征。 合成相应的化合物,并评估其对人前列腺PC-3细胞系的细胞毒性活性。 有些人已经表明了有希望的生物活性,以抑制耐植物素的细胞系的生长。

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