29264-14-0Relevant articles and documents
Design, synthesis, antitumor, and VEGFR-2 inhibition activities of novel 4-anilino-2-vinyl - quinazolines: Molecular modeling studies
Abdel-Aziz, Alaa A.-M.,AlSaif, Nawaf A.,El-Azab, Adel S.,El-Shafey, Hamed W.,Hamdi, Abdelrahman,Othman, Dina I. A.
, (2022/03/14)
The antitumor activity of newly synthesized 4-anilino-2-vinylquinazolines 8a-r was measured comparable to sorafenib as a standard drug. The 2-vinylquinazolines 8a-r were evaluated for their in vitro antitumor activity. The most active antitumor agents were subjected to in vitro VEGFR-2 inhibition and apoptotic inducing assay. Compounds 8 h, 8 l, and 8r showed potential antitumor activities with IC50 values of 4.92–14.37 μM relative to the reference drug, sorafenib (IC50 values of 5.47–9.18 μM). Compound 8 h possessed potential VEGFR-2 inhibitory activity (IC50 = 60.27 nM) compared to standard drug sorafenib (IC50 = 55.43 nM), whereas compound 8 l showed moderate inhibitory activity (IC50 = 93.50 nM). The most active compound, 8 h, exhibited total apoptosis with 36.24% on MCF-7 cells, more than the apoptotic effect provoked by sorafenib (32.46%) and the cell cycle arrested at a G1/S phase. Compound 8 h, a potent VEGFR-2 inhibitor, was docked into the VEGFR-2 binding pocket, where this compound showed binding interaction similar to co-crystallized inhibitor sorafenib.
Desymmetrisation of aromatic diamines and synthesis of non-symmetrical thiourea derivatives by click-mechanochemistry
Strukil, Vjekoslav,Margetic, Davor,Igrc, Marina D.,Eckert-Maksic, Mirjana,Friscic, Tomislav
supporting information, p. 9705 - 9707 (2012/10/29)
ortho- and para-Phenylenediamines were desymmetrised and quantitatively transformed into mono- and bis-(thio)ureas or mixed thiourea-ureas through a one-pot mechanochemical click reaction sequence; mechanochemical desymmetrisation proceeds quantitatively
