1285561-73-0Relevant academic research and scientific papers
Metronidazole aryloxy, carboxy and azole derivatives: Synthesis, anti-tumor activity, QSAR, molecular docking and dynamics studies
Faghih-Mirzaei, Ehsan,Sabouri, Salehe,Zeidabadinejad, Leila,AbdolahRamazani, Salman,Abaszadeh, Mehdi,Khodadadi, Arash,Shamsadinipour, Mohadeseh,Jafari, Mandana,Pirhadi, Somayeh
, p. 305 - 314 (2019)
A series of novel metronidazole aryloxy, carboxy and azole derivatives has been synthesized and their cytotoxic activities on three cancer cell lines were evaluated by MTT assay. Compounds 4m, 4l and 4d showed the most potent cytotoxic activity (IC50s less than 100 μg/mL). Apoptosis was also detected for these compounds by flow cytometry. Docking studies were performed in order to propose the probable target protein. In the next step, molecular dynamics simulation was carried out on the proposed target protein, focal adhesion kinase (FAK, PDB code: 2ETM), bound to compound 4m. As, 4m showed a potent cytotoxic activity and an acceptable apoptotic effect, it can be a potential anticancer candidate that may work through inhibition of FAK.
Synthesis of arrays using low molecular weight MPEG-assisted mitsunobu reaction
Figlus, Marek,Wellaway, Natalie,Cooper, Anthony W. J.,Sollis, Steven L.,Hartley, Richard C.
experimental part, p. 280 - 285 (2011/06/25)
Triphenylphosphine tagged with a short poly(ethyleneglycol)-ω- monomethyl ether chain (light MPEG, 10-16 ethylenoxy units, MTPP-G2) and an MPEG-tagged version of diethyl azodicarboxylate (MDEAD) have been used to prepare a 20 member library of esters, ethers, and sulfonamides, with cLogP?s in the range of 1.4-5.7 on a 0.1 mmol scale. Removal of MPEG-tagged side products was achieved by MPEG-assisted solid-phase extraction (MSPE) on prepacked silica columns to give the products in good yield and high purity.
