Organofluorine compounds in artificial blood circulation systems

Novel thiazole derivatives incorporating phenyl sulphonyl moiety as potent BRAFV600E kinase inhibitors targeting melanoma

“…Prompted by the role of fluorine atom in enhancing the biological activity of previously reported fluorinated compounds, 49,50 p -fluorophenacyl sulfone 16 was reacted with thiosemicarbazide 2 in ethanolic solution containing HCl to obtain the corresponding thiosemicarbazone derivative 17 (Scheme 5). The reaction of the latter with p -methoxyphenacyl bromide 18 afforded the corresponding fluorinated thiazole product 19 , as depicted in Scheme 5.…”

“…In a similar manner, the reactivity of thiosemicarbazone 3 toward C-1-(ethoxycarbonyl)-N-4-arylhydrazonoyl chlorides 8a-c was investigated. Thus, the reaction of ( 3 Prompted by the role of uorine atom in enhancing the biological activity of previously reported uorinated compounds, 49,50 p-uorophenacyl sulfone 16 was reacted with thiosemicarbazide 2 in ethanolic solution containing HCl to obtain the corresponding thiosemicarbazone derivative 17 As presented in Table 1 and Fig. 6, all the tested compounds effectively inhibited the kinase activity of the B-RAFV600E enzyme with IC 50 values at the nanomolar level in the range from 23.1 to 205 nM, which is equated to the reference drug dabrafenib (IC 50 ¼ 47.2 AE 2.5 nM).…”

Fluorinated Protein and Peptide Materials for Biomedical Applications

“…Applications of these versatile fluorinated materials have primarily been proposed in the biomedical space as fluorination imbues materials with honed target selectivity [ 1 ], strengthened binding affinity [ 2 ], enriched metabolic stability, and prolonged circulation times [ 3 ]. While the introduction of singular fluorine atoms appears to instill these desired properties in large proteins such as antibodies [ 72 ], a higher number of fluorinated moieties distributed throughout lengthy sequences tend to be necessary to observe a more pronounced effect.…”

“…Heralded as a miracle element, fluorine has earned its reputation as one of the most popular heteroatoms in modern chemical design due to its ability to furnish molecules with desirable physiochemical properties, such as honed target selectivity [ 1 ], strengthened binding affinity [ 2 ], enriched metabolic stability, and prolonged circulation times [ 3 ]. The past decade has witnessed the explosive emergence of fluorinated small molecules and nanomaterials in nearly every major commercial industry market, ranging from blockbuster pharmaceuticals like atorvastatin (Lipitor) to non-stick cookware, liquid crystalline displays to fluorinated anesthetics, refrigerants to toothpaste [ 4 ].…”

Fluoropolymer Nanoparticles Synthesized via Reversible-Deactivation Radical Polymerizations and Their Applications

“…Polymeric nanoparticles (PNPs) play an important role in nanomaterials due to their interesting physical and chemical properties caused by high relative surface area, quantum size effects, and characteristics brought from polymers (e.g., mechanical strength, chemical structure, polarity, and solubility). − Fluorinated polymeric nanoparticles (FPNPs) combine attributes of both PNPs and unique properties of fluoropolymers, such as outstanding chemical and temperature stability, high hydrophobicity, low surface energy, low refractive index, and others, and have stimulated massive interest in both academia and industries. − However, fluoropolymers are not available from natural sources. As a result, people have developed various synthetic approaches to obtain FPNPs, leading to fluorinated materials of many applications in coatings, paintings, additives, electronics, photonics, and so forth during past decades. ,, …”