Electrophile-induced reactions of cross-conjugated enynones in the synthesis of heterocycles
CHEMISTRY OF HETEROCYCLIC COMPOUNDS
Authors: Pankova, Alena S.
Abstract
Being compounds with multiple electrophilic centers, cross-conjugated enynones can be involved in various transformations upon treatment with electrophiles, in particular, Lewis and Bronsted acids, providing a convenient access to acyclic and cyclic compounds. This review covers literature data on electrophile-assisted reactions of substrates with cross-conjugated enynone scaffold toward the synthesis of heterocyclic compounds. The information is arranged according to the type of enynone motif, and chemical transformations of 2-(alkyn-1-yl)alk-2-en-1-ones and alk-1-en-4-yn-3-ones are discussed. The bibliography includes 52 sources.
Synthesis and evaluation of F-18 labeled crizotinib derivative [F-18]FPC as a novel PET probe for imaging c-MET-positive NSCLC tumor
BIOORGANIC & MEDICINAL CHEMISTRY
Authors: Lin, Qingyu; Zhang, Yingying; Fu, Zhequan; Hu, Bingxin; Si, Zhan; Zhao, Yanzhao; Shi, Hongcheng; Cheng, Dengfeng
Abstract
c-MET-positive NSCLC is an important subtype accounting for about 5%similar to 22% of lung cancer. NSCLC patients with activating c-MET are intensively sensitive to c-MET selective receptor tyrosine kinase (RTK) inhibitors, so we aimed to develop a specific PET probe targeting to c-MET-positive NSCLC for potential patients screened by PET/CT. Herein, PET tracer F-18-radiolabeled crizotinib derivative ([F-18]FPC) was successfully achieved through a simple one-step F-18-labeling method. [F-18]FPC PET imaging on c-MET-positive (as well as blocking group) and negative NSCLC models were further evaluated, and results showed that [F-18]FPC was effective as a PET imaging probe that targeted c-MET-positive tumor. Therefore, [F-18]FPC could be a potential PET imaging probe for NSCLC tumor which was sensitive to c-MET-TKIs. By virtue of this property, it will benefit NSCLC patients for c-MET-TKI treatment.