10141-46-5Relevant articles and documents
Indoline ureas as potential anti-hepatocellular carcinoma agents targeting VEGFR-2: Synthesis, in vitro biological evaluation and molecular docking
Eldehna, Wagdy M.,Fares, Mohamed,Ibrahim, Hany S.,Aly, Mohamed H.,Zada, Suher,Ali, Mamdouh M.,Abou-Seri, Sahar M.,Abdel-Aziz, Hatem A.,Abou El Ella, Dalal A.
, p. 89 - 97 (2015)
In our effort to develop potent and effective agents with anti-proliferative activity towards HepG2 hepatocellular carcinoma cells with potential inhibitory activity against VEGFR-2, a novel series of 1-(4-((2-oxoindolin-3-ylidene)amino)phenyl)-3-arylurea
Bis amide-aromatic-ureas - Highly effective hydro- and organogelator systems
Baker,Acton,Stevens,Hayes
, p. 8303 - 8311 (2014)
A series of hydro- and organo-supergelators have been synthesised via coupling of simple bis aromatic-ureas via alkyl amide linkages. These bis amide-aromatic-ureas exhibited reduced critical gelator concentrations, improved gelator stability, mechanical
One-pot synthesis and transmembrane chloride transport properties of C3-symmetric benzoxazine urea
Roy, Arundhati,Saha, Debasis,Mukherjee, Arnab,Talukdar, Pinaki
, p. 5864 - 5867 (2016)
One-pot synthesis of a C3-symmetric benzoxazine-based tris-urea compound is discussed. 1H NMR titrations indicate a stronger Cl- binding compared that of Br- and I- by the receptor. Effective Cl- transport across liposomal membranes via a Cl-/X- antiport mechanism is confirmed. Theoretical calculation suggests that a few water molecules with N-H, C=O, and the aromatic ring of the receptor create a H-bonded polar cavity where a Cl- is recognized by O-H···Cl- interactions from five bridged water molecules.
NOVEL HYDROGELATOR
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, (2019/08/20)
A novel hydrogelator that contains a monourea compound having a sugar structure, which can be produced by a simple method, includes a compound of the following Formula [1]: (wherein Sg is a sugar group, A is a divalent linking group, and R is a
Design, synthesis and molecular modeling study of certain VEGFR-2 inhibitors based on thienopyrimidne scaffold as cancer targeting agents
Ghith, Amna,Youssef, Khairia M.,Ismail, Nasser S.M.,Abouzid, Khaled A.M.
, p. 111 - 128 (2018/10/24)
Different series of novel thieno [2,3-d]pyrimidine derivative (9a-d,10a-f,l,m and 15a-m) were designed, synthesized and evaluated for their ability to in vitro inhibit VEGFR-2 enzyme. Also, the cytotoxicity of the final compounds was tested against a panel of 60 different human cancer cell lines by NCI. The VEGFR-2 enzyme inhibitory results revealed that compounds 10d, 15d and 15 g are among the most active inhibitors with IC50 values of 2.5, 5.48 and 2.27 μM respectively, while compound 10a remarkably showed the highest cell growth inhibition with mean growth inhibition (GI) percent of 31.57%. It exhibited broad spectrum anti-proliferative activity against several NCI cell lines specifically on human breast cancer (T7-47D) and renal cancer (A498) cell lines of 85.5% and 77.65% inhibition respectively. To investigate the mechanistic aspects underlying the activity, further biological studies like flow cytometry cell cycle together with caspase-3 colorimetric assays were carried on compound 10a. Flow cytometric analysis on both MCV-7 and PC-3 cancer cells revealed that it induced cell-cycle arrest in the G0-G1phase and reinforced apoptosis via activation of caspase-3. Furthermore, molecular modeling studies have been carried out to gain further understanding of the binding mode in the active site of VEGFR-2 enzyme and predict pharmacokinetic properties of all the synthesized inhibitors.