Synthesis of a novel fused pyrrolodiazepine-based library with anti-cancer activity

TETRAHEDRON LETTERS

卷:59

Article

Malik, Neha¹  Iyamu, Iredia D.¹  Scheidt, Karl A.^1,2,3,4  Schiltz, Gary E.^1,3,4 

[1] Northwestern Univ, Ctr Mol Innovat & Drug Discovery, Evanston, IL 60208 USA

[2] Northwestern Univ, Dept Chem, 2145 Sheridan Rd, Evanston, IL 60208 USA

[3] Northwestern Univ, Dept Pharmacol, Chicago, IL 60611 USA

[4] Northwestern Univ, Feinberg Sch Med, Robert H Lurie Comprehens Canc Ctr, Chicago, IL 60611 USA

关键词: Library;    Diazepine;    Mannich reaction;    Cancer;   

DOI  :  10.1016/j.tetlet.2018.03.021

来源: Elsevier

【 摘 要 】

Development of drugs for new and persistent diseases will increasingly rely on the expansion of accessible chemical space to allow exploration of novel molecular targets. Here we report the synthesis of a library of novel fused heterobicyclic small molecules based on the 1,4-diazepine and 2,4-pyrrolidinedione scaffolds. Key chemical transformations included a Mannich-type condensation and chemoselective N-acylation reactions. Screening shows anti-cancer activity of several library compounds which suggests translational potential of this novel chemical scaffold. (C) 2018 Elsevier Ltd. All rights reserved.

【 授权许可】

Free