Antiangiogenic agent 2

Antiangiogenic agent 2 (compound 3b) 是一种有效的胸苷磷酸化酶 (thymidine phosphorylase) 抑制剂 (IC50: 39.71 μM)，表现出抗血管生成作用。

JNJ-10198409 是相对选择性的、ATP 竞争性的、具有口服活性的血小板衍生生长因子受体酪氨酸激酶抑制剂，其IC50=2 nM。它对PDGFR-β激酶 (IC50=4.2 nM) 和PDGFR-α激酶 (IC50=45 nM) 有较好的抑制作用。它是双重机制的抗血管生成和肿瘤细胞的抗增殖剂。

Rubusoside 是天然的增溶剂及甜味剂，具有良好的抗血管新生和抗过敏药的特性。

Apricoxib, also known as Benzenesulfonamide 42(4ethoxyphenyl)4methyl1Hpyrrol1yl, is an orally bioavailable nonsteroidal anti-inflammatory agent (NSAID) with potential antiangiogenic and antineoplastic activities. Apricoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), thereby inhibiting the conversion of arachidonic acid into prostaglandins. Apricoxib-mediated inhibition of COX-2 may induce tumor cell apoptosis and inhibit tumor cell proliferation and tumor angiogenesis. COX-related metabolic pathways may represent crucial regulators of cellular proliferation and angiogenesis.

Apatinib, also known as Rivoceranib and YN-968D1, is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. The free-base form is also known as Rivoceranib. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.

Azurin p28 peptide是一种具有肿瘤穿透能力和抗肿瘤活性的肽。它通过与p53结合形成p28:p53复合物，从而降低p53在蛋白酶体中的降解，进而诱导细胞凋亡(apoptosis)或使细胞周期停滞。此外，Azurin p28 peptide通过抑制VEGFR-2、FAK和Akt的磷酸化表现出抗血管生成效果，抑制p53阳性肿瘤的生长。

(Z)-Orantinib ((Z)-SU6668) 是一种有效，选择性，具有口服活性和 ATP 竞争性的 Flk‐1/KDR，PDGFRβ和 FGFR1抑制剂，IC50值分别为 2.1，0.008 和 1.2 μM。(Z)-Orantinib 是有效的抗血管生成和抗肿瘤剂，可诱导已形成的肿瘤消退。