DESIGN AND SYNTHESIS OF 1,3,5-TRIAZINE DERIVATIVES AS NOVEL INVERSE AGONISTS OF NUCLEAR RETINOIC ACID RECEPTOR-RELATED ORPHAN RECEPTOR-gamma

作者：Kaitoh Kazuma; Toyama Hirozumi; Hashimoto Yuichi; Fujii Shinya^*

来源：Heterocycles, 2017, 95(1): 547-556.

DOI：10.3987/COM-16-S(S)16

1,3,5-Triazine structure is a versatile chemical species for development of functional molecules, including biologically active compounds. We report herein the design, synthesis and biological evaluation of novel inverse agonists of nuclear retinoic acid receptor-related orphan receptor-gamma (ROR gamma), in which the 2-anilino-1,3,5-triazine moiety was used as a scaffold for structural development. Among the synthesized compounds, 13b exhibited potent and selective inverse agonistic activity toward RORy, being more potent than the lead compound T0901317 (7). The results suggest that the 2-anilino-1,3,5-triazine moiety is a useful scaffold for development of inhibitory ligands of nuclear receptors.

• 出版日期2017-1-25