School of Medicine, Xi'an Jiaotong University, Xi'an, Shaanxi Province, P.R. China.
Mini Rev Med Chem. 2011 Oct;11(11):920-46. doi: 10.2174/138955711797068355.
Angiogenesis is required for invasive tumor growth and metastasis and constitutes an important point in the control of cancer progression. Its inhibition may be a valuable approach to cancer therapy. Antiangiogenic agents are designed to attack the tumor vasculature and cut off the tumor's supply of nutrients. Systemic blockade of angiogenesis has been recently approved for the treatment of several types of human cancers. Antiangiogenic therapy presents various advantages as compared to conventional treatment. Vascular endothelial growth factor (VEGF) is considered to be one of the most important regulators of angiogenesis and a key target in anticancer treatment. VEGF binding to its receptor (VEGFR) leads to cell proliferation and new vascular formation by tyrosine kinase (TK) pathway. VEGF/VEGFR pathway is becoming attractive target for anticancer drug design. It is believed to be important in the control of angiogenesis. Antiangiogenic therapy based on inhibition of VEGFR was reported to be powerful clinical strategies. In this review, the authors describe the existing literature regarding VEGFR inhibitors in the last few years. We attempt to cover all essential publications on the medicinal chemistry in terms of chemical structure, pharmacological profile and structure-activity relationships.
血管生成对于侵袭性肿瘤的生长和转移是必需的，并且是控制癌症进展的重要方面。抑制血管生成可能是癌症治疗的一种有价值的方法。抗血管生成药物旨在攻击肿瘤血管，并切断肿瘤的营养供应。最近已经批准了全身性阻断血管生成用于治疗几种类型的人类癌症。与传统治疗相比，抗血管生成治疗具有多种优势。血管内皮生长因子（VEGF）被认为是血管生成最重要的调节剂之一，也是抗癌治疗的关键靶点。VEGF 与其受体（VEGFR）结合通过酪氨酸激酶（TK）途径导致细胞增殖和新血管形成。VEGF/VEGFR 途径正成为抗癌药物设计的有吸引力的靶点。它被认为在控制血管生成中很重要。基于抑制 VEGFR 的抗血管生成治疗被报道为强大的临床策略。在这篇综述中，作者描述了过去几年中关于 VEGFR 抑制剂的现有文献。我们试图涵盖药物化学方面的所有重要出版物，包括化学结构、药理学特征和构效关系。
