1639-44-7Relevant articles and documents
Synthesis and antiproliferative activity of 17-[1′,2′,3′]-selenadiazolylpregnenolone compounds
Cui, Jianguo,Pang, Liping,Wei, Meizhen,Gan, Chunfang,Liu, Dandan,Yuan, Haiyan,Huang, Yanmin
, p. 151 - 158 (2018)
Using pregnenolone as a starting material, some 3-substituted 17-[1′,2′,3′]-selenadiazolylpregnenolone derivatives were synthesized, and their structures were characterized by IR, NMR and HRMS. The in vitro antitumor activity of the compounds was assayed
Synthesis, Structural Elucidation, and Biological Evaluation of NSC12, an Orally Available Fibroblast Growth Factor (FGF) Ligand Trap for the Treatment of FGF-Dependent Lung Tumors
Castelli, Riccardo,Giacomini, Arianna,Anselmi, Mattia,Bozza, Nicole,Vacondio, Federica,Rivara, Silvia,Matarazzo, Sara,Presta, Marco,Mor, Marco,Ronca, Roberto
, p. 4651 - 4663 (2016/06/13)
NSC12 is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity. It was identified by virtual screening from a NCI small molecule library, but no data were available about its synthesis, stereochemistry, and physicochemical properties. We report here a synthetic route that allowed us to characterize and unambiguously identify the structure of the active compound by a combination of NMR spectroscopy and in silico conformational analysis. The synthetic protocol allowed us to sustain experiments aimed at assessing its therapeutic potential for the treatment of FGF-dependent lung cancers. A crucial step in the synthesis generated a couple of diastereoisomers, with only one able to act as a FGF trap molecule and to inhibit FGF-dependent receptor activation, cell proliferation, and tumor growth when tested in vitro and in vivo on murine and human lung cancer cells.
