Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors was written by Wang, Yuming;Li, Lijun;Fan, Jun;Dai, Yang;Jiang, Alan;Geng, Meiyu;Ai, Jing;Duan, Wenhu. And the article was included in Journal of Medicinal Chemistry in 2018.Safety of 2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine This article mentions the following:
Fibroblast growth factor receptors (FGFR1-4) are promising therapeutic targets in many cancers. With the resurgence of interest in irreversible inhibitors, efforts have been directed to the discovery of irreversible FGFR inhibitors. Currently, several selective irreversible inhibitors are being evaluated in clin. trials that could covalently target a conserved cysteine in the P-loop of FGFR. In this article, the authors used a structure-guided approach that is rationalized by a computer-aided simulation to discover the novel and irreversible pan-FGFR inhibitor, 9g ((S)-1-(3-(4-amino-5-(7-methoxy-5-methylbenzo[b]thien-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)pyrrolidin-1-yl)prop-2-en-1-one), which provided superior FGFR in vitro activities and decent selectivity over VEGFR2 (vascular endothelia growth factor receptor 2). In in vivo studies, 9g displayed clear antitumor activities in NCI-H1581 and SNU-16 xenograft mice models. Addnl., the diluting method confirmed the irreversible binding of 9g to FGFR. In the experiment, the researchers used many compounds, for example, 2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine (cas: 1012785-51-1Safety of 2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine).
2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine (cas: 1012785-51-1) belongs to iodide derivatives. Organic iodides are organic compounds containing a carbon-iodine (C-I) bond. The carbon-iodine bond is weaker than other carbon-halogen bonds due to the poor electronegative nature of the iodine atom. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond.Safety of 2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com