NU 2018-007

INVENTORS

• Karl Scheidt*
• Gary Schiltz

ABSTRACT

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. Some compounds have particular efficacy against lung cancer cells in vitro.

APPLICATIONS

• Novel chemical compositions
• Utility in drug discovery as bioactive molecules
• Actvity as anti-cancer agents

ADVANTAGES

• New molecular structures with new mechansims of actions
• Compound have highly drug-like chemical and biophysical properties
• New therapies for cancers are in continual need

IP STATUS

Issued US Patent No. 11,225,483

PUBLICATION

Malik N, Iyamu I, Scheidt K and Schiltz G (2018) Synthesis of a novel fused pyrrolodiazepine-based library with anti-cancer activity.  Tetrahedron Letters. 59: 1513-1516. https://doi.org/10.1016/j.tetlet.2018.03.021