An easy method to achieve a fluorinated graphene oxide-silica nanohybrid (GOSF) is presented. Graphene oxide (GO) was synthesized by Hummer's modified method, the GO-silica nanohybrid (GOS) was obtained via Fischer esterification, the fluorinated moiety (3-pentadecafluoroheptyl-5-perfluorophenyl-1,2,4-oxadiazole) was introduced by nucleophilic substitution operated by the hydroxyl functionalities onto the GOS surface. Full characterization of the new materials confirmed the formation of covalent bonds between the graphene oxide/silica hybrid matrix and the fluorinated moieties. The proposed methodology offers an easy way to get fluorinated carbon/silica hybrid nanomaterials avoiding the harsh reaction conditions usually involved in the preparation of fluorinated materials, and allowing the selective immobilization of specific fluorotails. Moreover, performed oxygen uptake and release kinetics showed that the introduction of fluorinated moieties increases the oxygen exchange, making the material interesting for prospective applications in the biomedical field, as oxygen delivery system, as filler for biocompatible materials, and in the preparation of membranes for the purification of water.
A new class of
pyrrolo[2′,3′:3,4]cyclohepta[1,2-
d
][1,2]oxazoles was
synthesized for the treatment of hyperproliferative pathologies, including neoplasms.
The new compounds were screened in the 60 human cancer cell lines of the NCI drug screen
and showed potent activity with GI
50
values reaching the nanomolar level,
with mean graph midpoints of 0.08–0.41 μM. All compounds were further
tested on six lymphoma cell lines, and eight showed potent growth inhibitory effects
with IC
50
values lower than 500 nM. Mechanism of action studies showed the
ability of the new [1,2]oxazoles to arrest cells in the G2/M phase in a concentration
dependent manner and to induce apoptosis through the mitochondrial pathway. The most
active compounds inhibited tubulin polymerization, with IC
50
values of
1.9–8.2 μM, and appeared to bind to the colchicine site. The G2/M arrest
was accompanied by apoptosis, mitochondrial depolarization, generation of reactive
oxygen species, and PARP cleavage.
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