57753-81-8Relevant academic research and scientific papers
Furan-2-carboxamide derivative, a novel microtubule stabilizing agent induces mitotic arrest and potentiates apoptosis in cancer cells
Shwetha,Sudhanva, M. Srinivasa,Jagadeesha,Thimmegowda,Hamse, Vivek K.,Sridhar,Thimmaiah,Ananda Kumar,Shobith, Rangappa,Rangappa
, (2021/02/21)
The vital role played by microtubules in the cell division process, marks them as a potential druggable target to decimate cancer. A novel furan-2-carboxamide based small molecule, is a selective microtubule stabilizing agent (MSA) with IC50 ranging from 4 μM to 8 μM in different cancer cell lines. Inhibition of tubulin polymerization or stabilization of tubulin polymers abrogates chromosomal segregation during cell division, results in cell cycle arrest and leads to cell death due to the delayed repair mechanism. A novel furan-2-carboxamide based small molecule exhibited potent anti-proliferative and anti-metastatic property In-Vitro against the panel of cancer cells. Annexin V-FITC/PI, double staining reveals potent cytotoxic effect of SH09 against HeLa cells. FACS analysis displays induction of G2/M arrest and accumulation of subG1 population of cells upon treatment with SH09. Molecular docking study unveils SH09 binding affinity to the Taxol binding pocket of tubulin proteins and MM-GBSA also confirms strong binding energies of SH09 with tubulin proteins.
T-BuXPhos: A highly efficient ligand for Buchwald-Hartwig coupling in water
Wagner, Patrick,Bollenbach, Maud,Doebelin, Christelle,Bihel, Frederic,Bourguignon, Jean-Jacques,Salome, Christophe,Schmitt, Martine
supporting information, p. 4170 - 4178 (2014/09/29)
An efficient and versatile 'green' catalytic system for the Buchwald-Hartwig cross-coupling reaction in water is reported. In an aqueous micellar medium, the combination of t-BuXPhos with [(cinnamyl)PdCl]2 showed excellent performance for coupling arylbromides or chlorides with a large set of amines, amides, ureas and carbamates. The method is functional-group tolerant, proceeds smoothly (30 to 50 °C) and provides rapid access to the target compounds in good to excellent isolated yields. When applied to the synthesis of a known NaV1.8 modulator, this method led to a significant improvement of the E-factor in comparison with classical organic synthesis. the Partner Organisations 2014.
Use of 5-phenyl-2-furan esters and amides as antiepileptic agents
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, (2008/06/13)
A method of preventing epileptic seizures in a human or mammal subject susceptible to said seizures, comprising systemically administering to said subject a safe and effective amount of a compound of the formula: STR1 wherein (a) X is halo or hydrogen, an
