血管生成在肿瘤的形成和进展中起着重要作用，用于供应营养和转移。因此，本文设计了一系列新颖的二氢-吲哚衍生物，并通过与秋水仙碱结合，作为微管聚合抑制剂，展示了对新生血管形成的抗血管生成活性。通过结构-活性关系研究，发现化合物12d是最有效的衍生物之一，对四种癌细胞线的抗增殖活性具有IC50值在0.028-0.087 µM之间。化合物12d在体外与微管上的秋水仙碱结合，并抑制了微管的聚合。此外，化合物12d引发细胞周期在G2/M期的停滞，促进细胞凋亡，抑制肿瘤转移和血管生成。最后，体内实验证明，化合物12d可以防止肿瘤形成，抑制肿瘤增殖和血管生成，而无明显毒性。综上所述，所有这些发现表明化合物12d是一种值得进一步研究的新颖微管聚合抑制剂。

Angiogenesis plays an important role in tumour generation and progression, which is used to supply nutrients and metastasis. Herein, a series of novel dihydro-1H-indene derivatives were designed and evaluated as tubulin polymerisation inhibitors by binding to colchicine site, exhibiting anti-angiogenic activities against new vessel forming. Through structure-activity relationships study, compound 12d was found to be the most potent derivative possessing the antiproliferative activity against four cancer lines with IC50 values among 0.028-0.087 µM. Compound 12d bound to colchicine site on tubulin and inhibited tubulin polymerisation in vitro. In addition, compound 12d induced cell cycle arrest at G2/M phase, stimulated cell apoptosis, inhibited tumour metastasis and angiogenesis. Finally, the results of in vivo assay suggested that compound 12d could prevent tumour generation, inhibit tumour proliferation and angiogenesis without obvious toxicity. Collectively, all these findings suggested that compound 12d is a novel tubulin polymerisation inhibitor deserving further research.