1428533-11-2Relevant academic research and scientific papers
Synthesis and evaluation of nicotinamide derivative as anti-angiogenic agents
Choi, Hye-Eun,Choi, Jung-Hye,Lee, Jae Yeol,Kim, Je Hak,Kim, Ji Han,Lee, Joon Kwang,Kim, Gyu Il,Park, Yong,Chi, Yong Ha,Paik, Soo Heui,Lee, Joo Han,Lee, Kyung-Tae
, p. 2083 - 2088 (2013/04/23)
Previously, we have found that BRN-103, a nicotinamide derivative, inhibits vascular endothelial growth factor (VEGF)-mediated angiogenesis signaling in human endothelial cells. During our continuous efforts to identify more potent anti-angiogenic agents, we synthesized various nicotinamide derivatives and evaluated their anti-angiogenic effects. We found that 2-{1-[1-(6-chloro-5- fluoropyrimidin-4-yl)ethyl]piperidin-4-ylamino}-N-(3-chlorophenyl) pyridine-3-carboxamide (BRN-250) significantly inhibited human umbilical vascular endothelial cells (HUVECs) proliferation, migration, tube formation, and microvessel growth in a concentration range of 10-100 nM. Furthermore, BRN-250 inhibited the VEGF-induced phosphorylation and intracellular tyrosine kinase activity of VEGF receptor 2 (VEGFR2) and the activation of its downstream AKT pathway. Taken together, these findings suggest that BRN-250 be considered a potential lead compound for cancer therapy.
