RESUMO
An efficient method for the synthesis of alkynyl sulfides via a C(sp3)-S bond cleavage of α-bromostyrene sulfonium salts has been developed. This base-promoted nucleophilic ring-opening pathway allows the preparation of diverse alkynyl sulfide compounds using tetramethylene sulfoxide as the sulfur source. The reaction proceeds with good functional group tolerance and could be applied to the late-stage functionalization of bioactive molecules and drugs. Furthermore, the synthetic utility of this method was demonstrated by a one-pot synthesis, scale-up reaction and further modification of various alkynyl sulfide products.
RESUMO
Pancreatic cancer (PC) is one of the most malignant tumors with a dismal survival rate, this is primarily due to inevitable chemoresistance. Dysfunctional tyrosine kinases (TKs) and long non-coding RNAs (lncRNAs) affect the drug resistance and prognosis of PC. Here, we summarize the mechanisms by which TKs or lncRNAs mediate drug resistance and other malignant phenotypes. We also discuss that lncRNAs play oncogenic or tumor suppressor roles and different mechanisms including lncRNA-proteins/microRNAs to mediate drug resistance. Furthermore, we highlight that lncRNAs serve as upstream regulators of TKs mediating drug resistance. Finally, we display the clinical significance of TKs (AXL, EGFR, IGF1R, and MET), clinical trials, and lncRNAs (LINC00460, PVT1, HIF1A-AS1). In the future, TKs and lncRNAs may become diagnostic and prognostic biomarkers or drug targets to overcome the drug resistance of PC.