A Facile Ugi/Ullmann Cascade Reaction to Access Fused Indazolo-Quinoxaline Derivatives with Potent Anticancer Activity-Reference-Cited by-同舟云学术

A Facile Ugi/Ullmann Cascade Reaction to Access Fused Indazolo-Quinoxaline Derivatives with Potent Anticancer Activity

Published:2024-01-17 Issue:2 Volume:29 Page:464
ISSN:1420-3049
Container-title:Molecules
language:en
Short-container-title:Molecules

Author:

Li Yong¹²^ORCID,He Liujun¹^ORCID,Qin Hongxia¹,Liu Yao¹,Yang Binxin¹,Xu Zhigang¹^ORCID,Yang Donglin¹^ORCID

Affiliation:

1. College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, Chongqing University of Arts and Sciences, Chongqing 402160, China

2. School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China

Abstract

A facile methodology for the construction of a complex heterocycle indazolo-fused quinoxalinone has been developed via an Ugi four-component reaction (U-4CR) followed by an intramolecular Ullmann reaction. The expeditious process features an operationally simple approach, time efficiency, and a broad substrate scope. Biological activity was evaluated and demonstrated that compound 6e inhibits human colon cancer cell HCT116 proliferation with an IC50 of 2.1 μM, suggesting potential applications for developing a drug lead in medicinal chemistry.

Funder

Science and Technology Research Program of Chongqing Municipal Education Commission

Natural Science Foundation of Chongqing Science and Technology Bureau

Scientific Research Foundation of the Chongqing University of Arts and Sciences

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

Link

https://www.mdpi.com/1420-3049/29/2/464/pdf

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