Opening book details…
Can I read Identification of novel 3-aryl-1-aminoisoquinolines-based KRASG12C inhibitors: Rational drug design and expedient construction by C H functionalization/annulation on EtoBox?
Identification of novel 3-aryl-1-aminoisoquinolines-based KRASG12C inhibitors: Rational drug design and expedient construction by C H functionalization/annulation by Zirong Gong; Yu Zhao; Buyi Xu; Zhou Yang; Boquan Ren; Han Yang; Chengfu Zeng; Renqiang Chen; Yan-Jun Xu; Qing Li is a Chemistry article available to read on EtoBox.
What is Identification of novel 3-aryl-1-aminoisoquinolines-based KRASG12C inhibitors: Rational drug design and expedient construction by C H functionalization/annulation about?
Developing a synthetic methodology to expediently construct a specific drug scaffold with the desired biological activity remains challenging. Herein, we describe a work on rational application of a synthetic methodology in the synthesis of KRAS G12C inhibitors. Novel KRAS G12C inhibitors were initially designed with 1-amino-3-aryl isoquinoline scaffold using structure-based drug design strategy. A ruthenium-catalyzed direct mono -C -H functionalization/annulation cascade reaction of amidines and sulfoxonium ylides was then developed with high versatility of substrates and good tolerance for polar functional groups. By using this reaction, the target compounds 1-amino-3-aryl isoquinolines were facilely prepared. Further in vitro tests led to identification of two novel lead compounds with KRAS G12C inhibitory activity.
Who reads Identification of novel 3-aryl-1-aminoisoquinolines-based KRASG12C inhibitors: Rational drug design and expedient construction by C H functionalization/annulation?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Zirong Gong; Yu Zhao; Buyi Xu; Zhou Yang; Boquan Ren; Han Yang; Chengfu Zeng; Renqiang Chen; Yan-Jun Xu; Qing Li
- Publisher
- Elsevier BV
- Published
- 2024
- Language
- EN
- Field
- Chemistry (Physical Sciences)