School of Chemical Sciences and Pharmacy, Central University of Rajasthan, NH-8, Bandarsindri, Ajmer-305817, Rajasthan, India.
Chem Commun (Camb). 2018 Oct 11;54(82):11530-11533. doi: 10.1039/c8cc05845h.
Synthesis of pyrazolo[1,5-c]quinazolines from four easily available precursors is presented through a one-pot tricyclic Pd(ii)/Ag(i) relay catalysis. The bimetallic relay cascade forges five new chemical bonds by concatenating six discrete chemical steps. The relay catalysis enables four-component assembly of pyrazolo[1,5-c]quinazolines that selectively inhibit EGFR, exhibit apoptosis through the ROS-induced mitochondrial-mediated pathway, and arrest the cell cycle at the G1 phase.
通过一锅三组分钯(ii)/银(i)接力催化，从四个易得前体制备吡唑并[1,5-c]喹唑啉。双金属接力级联通过串联六个离散的化学步骤形成五个新的化学键。该接力催化实现了吡唑并[1,5-c]喹唑啉的四组分组装，其选择性抑制 EGFR，通过 ROS 诱导的线粒体介导途径诱导细胞凋亡，并将细胞周期阻滞在 G1 期。
