A series of 1, 4-dihydroindeno-[1,2-c] pyrazole linked oxindole conjugates have been synthesized by using Knoevenagel condensation method and further evaluated for their antiproliferative activity against HeLa, A549 and MDA-MB-231 human cancer cell lines along with HEK-293 (normal human embryonic kidney cells). Among the derivatives, compounds 12a, 12b, and 12d showed excellent cytotoxicity with IC₅₀ values ranging between 1.33 to 4.33 μM. Furthermore, detailed biological assays showed that there was accumulation of mitotic cells in G2/M phase, disruption of microtubule network and increase in the G2/M checkpoint proteins (Cyclin B1 and CDK1). Moreover, compound 12d with IC₅₀ value of 1.33 μM showed significant upregulation of tumor suppressor proteins like p53, p21 and pro-apoptotic Bax. The molecular docking analysis demonstrated that these congeners occupy the colchicine binding pocket of the tubulin.

使用Knoevenagel缩合方法合成了一系列1，4-二氢茚并-[1,2- c ]吡唑连接的羟吲哚共轭物，并进一步评估了它们对HeLa，A549和MDA-MB-231人癌细胞系的抗增殖活性HEK-293（正常人胚胎肾细胞）。在衍生物中，化合物12a，12b和12d显示出优异的细胞毒性，IC ₅₀值在1.33至4.33μM之间 。此外，详细的生物学分析表明，在G2 / M期有丝分裂细胞的积累，微管网络的破坏和G2 / M检查点蛋白（Cyclin B1和CDK1）的增加。此外，带IC的化合物12d₅₀值1.33μM 显示出明显的肿瘤抑制蛋白上调，如p53，p21和促凋亡Bax。分子对接分析表明，这些同类物占据了微管蛋白的秋水仙碱结合口袋。