@article{162efbc8c4f74c1c96e2733c3b1cbe79,
title = "Synthesis of Constrained Heterocycles Employing Two Post-Ugi Cyclization Methods for Rapid Library Generation with In Cellulo Activity",
abstract = "Benzimidazoles and quinoxalinones are present in the core of many pharmacologically relevant compounds. Several combinatorial methods have been developed to attach ring systems to both scaffolds for derivatization at select positions. Herein, we describe the development of novel constrained heterocyclic compounds attached to the N1 position of both benzimidazole and quinoxalinone scaffolds. Utilizing robust post-Ugi cyclization methods, including the Ugi-deprotection-cyclization (UDC) methodology, allows for efficient access to a new area of chemical space. Additionally, molecular modeling and in cellulo screening was employed to therapeutically validate the compounds formed with this method.",
keywords = "Heterocycle Formation, MDM2/MDMX, Multicomponent Reaction, Post-Ugi Modifications, Ugi Condensation",
author = "Nicholas McConnell and Zhigang Xu and Vishnu Kumarasamy and Daekyu Sun and Brendan Frett and Li, {Hong Yu}",
note = "Funding Information: This work was supported by a training grant from The National Institutes of Health (T32 GM008804), the NCI Predoctoral to Postdoctoral Fellow Transition Award (F99 CA212480-02), University of Arizona startup funding, the Yuma Friends of Arizona Health Sciences Young Investigator Research Award, and by an Institutional Development Award (IDeA) from the National Institute of General Medical Sciences from the National Institutes Funding Information: of Health under grant number “P20 GM109005”. We would like to acknowledge the Biological Chemistry Program (BCP) at the University of Arizona for their continued scholarship support.",
year = "2017",
month = dec,
day = "11",
doi = "10.1002/slct.201702179",
language = "English (US)",
volume = "2",
pages = "11821--11825",
journal = "ChemistrySelect",
issn = "2365-6549",
publisher = "Wiley-Blackwell Publishing Ltd",
number = "35",
}