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

Publisher: Taylor & Francis Country of Publication: England NLM ID: 101150203 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1475-6374 (Electronic) Linking ISSN: 14756366 NLM ISO Abbreviation: J Enzyme Inhib Med Chem Subsets: MEDLINE

Original Publication: Basingstoke, UK : Taylor & Francis, c2002-

Angiogenesis Inhibitors*/pharmacology ; Angiogenesis Inhibitors*/chemistry ; Angiogenesis Inhibitors*/chemical synthesis ; Neovascularization, Pathologic*/drug therapy ; Neovascularization, Pathologic*/metabolism ; Neovascularization, Pathologic*/pathology ; Antineoplastic Agents*/pharmacology ; Antineoplastic Agents*/chemistry ; Antineoplastic Agents*/chemical synthesis ; Small Molecule Libraries*/pharmacology ; Small Molecule Libraries*/chemistry ; Small Molecule Libraries*/chemical synthesis ; Neoplasms*/drug therapy ; Neoplasms*/pathology ; Neoplasms*/blood supply; Humans ; Structure-Activity Relationship ; Molecular Structure ; Cell Proliferation/drug effects ; Animals ; Apoptosis/drug effects ; Drug Screening Assays, Antitumor ; 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.

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Keywords: Anti-cancer; FGFR; HDAC; VEGFR-2; angiogenesis

0 (Angiogenesis Inhibitors)
0 (Antineoplastic Agents)
0 (Small Molecule Libraries)

Date Created: 20251120 Date Completed: 20251120 Latest Revision: 20251123

20251123

PMC12636607

10.1080/14756366.2025.2584811

41263406