Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2 was written by Kuriwaki, Ikumi;Kameda, Minoru;Hisamichi, Hiroyuki;Kikuchi, Shigetoshi;Iikubo, Kazuhiko;Kawamoto, Yuichiro;Moritomo, Hiroyuki;Kondoh, Yutaka;Amano, Yasushi;Tateishi, Yukihiro;Echizen, Yuka;Iwai, Yoshinori;Noda, Atsushi;Tomiyama, Hiroshi;Suzuki, Tomoyuki;Hirano, Masaaki. And the article was included in Bioorganic & Medicinal Chemistry in 2020.Reference of 59864-30-1 This article mentions the following:
Fibroblast growth factor receptor 3 (FGFR3) is an attractive therapeutic target for the treatment of bladder cancer. We identified 1,3,5-triazine derivative 18b and pyrimidine derivative 40a as novel structures with potent and highly selective FGFR3 inhibitory activity over vascular endothelial growth factor receptor 2 (VEGFR2) using a structure-based drug design (SBDD) approach. X-ray crystal structure anal. suggests that interactions between 18b and amino acid residues located in the solvent region (Lys476 and Met488), and between 40a and Met529 located in the back pocket of FGFR3 may underlie the potent FGFR3 inhibitory activity and high kinase selectivity over VEGFR2. In the experiment, the researchers used many compounds, for example, 2,6-Dimethoxypyrimidine-4-carboxylic acid (cas: 59864-30-1Reference of 59864-30-1).
2,6-Dimethoxypyrimidine-4-carboxylic acid (cas: 59864-30-1) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Reference of 59864-30-1
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia