Discovery of a potent, orally available furopyridine derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor,Bioorganic & Medicinal Chemistry Letters

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Discovery of a potent, orally available furopyridine derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2024-06-12 , DOI: 10.1016/j.bmcl.2024.129848
Shuichi Hagihara ₁ , Kouhei Ishizawa ₁ , Manami Kikuchi ₁ , Yuko Kawano ₁ , Akiko Nishidate ₁ , Fumi Matsumoto ₁ , Naohiro Hashimoto ₁ , Chiduko Sasaki ₁ , Ikuko Miyaguchi ₁ , Okimasa Okada ₁ , Tomoya Akashi ₁ , Shinji Nakayama ₁ , Yuko Ogasawara ₁ , Junichi Endo ₁

Affiliation

We explored novel immunosuppressive agents with immune tolerance using a phenotypic drug discovery strategy, focusing on costimulatory molecules in T cells, and obtained triazolothienodiazepine derivatives. Their mechanism of action is to inhibit the bromodomain and extra-terminal domain (BET) family, as we have previously reported. Selective inhibition of the first bromodomain (BD1) of the BET family is expected to exert antitumor and immunosuppressive effects, similar to BET inhibitors.

中文翻译：

发现一种有效的口服呋喃吡啶衍生物作为新型选择性溴结构域和末端外结构域 (BET) 第一溴结构域 (BD1) 抑制剂

我们采用表型药物发现策略，重点关注T细胞中的共刺激分子，探索具有免疫耐受性的新型免疫抑制剂，并获得了三唑并噻吩并二氮杂卓衍生物。正如我们之前报道的，它们的作用机制是抑制溴结构域和末端外结构域 (BET) 家族。选择性抑制 BET 家族的第一个溴结构域 (BD1) 预计将发挥抗肿瘤和免疫抑制作用，类似于 BET 抑制剂。

更新日期：2024-06-12

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