Recent progress in the exploitation of anti-cancer small molecules targeting angiogenesis

Angiogenesis is pivotal for cancer growth and metastasis, as tumours rely on new blood vessels to progress and spread. Antiangiogenic drugs represent a crucial therapeutic strategy that combats cancer by both obstructing the development of new blood vessels and disrupting existing tumour-associated vasculature. Recently, significant advancements have been made in antiangiogenic cancer therapies, as evidenced by the extensive literature covered in this review. Numerous novel angiogenesis inhibitors have been reported to exhibit significant efficacy: they not only suppress cancer metastasis and angiogenesis but also induce cancer cell apoptosis via multiple distinct mechanisms. This review comprehensively updates (2014-2025) small molecule angiogenesis inhibitors' design and structure-activity relationship (SAR), integrating latest developments. By systematically analysing the mechanisms of action and distinctive characteristics of these compounds, we aim to offer valuable insights and references to guide the ongoing development of next-generation anti-cancer agents targeting angiogenesis.