A new series of indolenines decorated with pyrazolo[3,4-]pyridines were designed and synthesized in up to 96% yield from the acid-catalyzed cyclocondensation of 1,3-dialdehydes with 3-aminopyrazoles. X-ray crystallography on a representative derivative, , revealed two close to planar conformations whereby the -atom of the pyridyl residue was or to the pyrrole- atom in the two independent molecules of the asymmetric unit. The computational and DNA binding data suggest that is a strong DNA intercalator with the results in agreement with its potent cytotoxicity against two colorectal cancer cell lines (HCT 116 and HT-29). In contrast to doxorubicin, compounds - have higher druggability (compliance to more criteria stated in Lipinski’s rule of five and Veber’s rule), higher bioavailability, and better medicinal chemistry properties, indicative of their potential application as chemotherapeutical agents.

中文翻译：

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发现吲哚基吡唑并[3,4-b]吡啶作为针对结直肠癌细胞的有效化疗剂

设计并合成了一系列新的吡唑并[3,4-]吡啶修饰的假吲哚，通过1,3-二醛与3-氨基吡唑的酸催化环缩合反应，产率高达96%。代表性衍生物 的 X 射线晶体学揭示了两种接近平面的构象，其中吡啶基残基的 原子是 或 是不对称单元的两个独立分子中的吡咯原子。计算和 DNA 结合数据表明，它是一种强 DNA 嵌入剂，其结果与其对两种结直肠癌细胞系（HCT 116 和 HT-29）的有效细胞毒性一致。与阿霉素相比，化合物具有更高的成药性（符合利平斯基五法则和韦伯法则中规定的更多标准）、更高的生物利用度和更好的药物化学性质，表明它们作为化疗药物的潜在应用。