- Discovery of a new series of naphthamides as potent VEGFR-2 kinase inhibitors
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Inhibition of VEGFR-2 signaling pathway has already become one of the most promising approaches for the treatment of cancer. In this study, we describe the design, synthesis, and biological evaluation of a new series of naphthamides as potent inhibitors of VEGFR-2. Among these compounds, 14c exhibited high VEGFR-2 inhibitory potency in both enzymatic and HUVEC cellular proliferation assays, with IC50 values of 1.5 and 0.9 nM, respectively. Kinase selectivity profiling revealed that 14c was a multitargeted inhibitor, and it also exhibited good potency against VEGFR-1, PDGFR-β, and RET. Furthermore, 14c effectively blocked tube formation of HUVEC at nanomolar level. Overall, 14c might be a promising candidate for the treatment of cancer.
- Lv, Yongcong,Li, Mengyuan,Liu, Ting,Tong, Linjiang,Peng, Ting,Wei, Lixin,Ding, Jian,Xie, Hua,Duan, Wenhu
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p. 592 - 597
(2014/06/09)
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- Imidazo[1,2-a]pyridines: Orally active positive allosteric modulators of the metabotropic glutamate 2 receptor
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Advanced leads of an imidazopyridine series of positive allosteric modulators of the metabotropic glutamate 2 (mGlu2) receptor are reported. The optimization of in vitro ADMET and in vivo pharmacokinetic properties led to the identification of 27o. With g
- Trabanco, Andrés A.,Tresadern, Gary,MacDonald, Gregor J.,Vega, Juan Antonio,De Lucas, Ana Isabel,Matesanz, Encarnación,García, Aránzazu,Linares, María Lourdes,Alonso De Diego, Sergio A.,Alonso, José Manuel,Oehlrich, Daniel,Ahnaou, Abdelah,Drinkenburg, Wilhelmus,MacKie, Claire,Andrés, José Ignacio,Lavreysen, Hilde,Cid, José María
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experimental part
p. 2688 - 2701
(2012/06/01)
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