38652-23-2Relevant academic research and scientific papers
Synthesis and antitumor activity of novel pyridino[2,3-d]pyrimidine urea derivatives
Chen, Dongmei,Chen, Yumei,Yang, Di,Zheng, Zhaopeng,Zhou, Zhixu
, p. 1628 - 1636 (2021/05/19)
A series of novel N-(3-((6-bromopyrido[2,3-d]pyrimidin-4-yl)oxy)phenyl)pyrrolidine-1-carboxamide and 1-(3-((6-bromopyrido[2,3-d]pyrimidin-4-yl)oxy)phenyl)-3-propylurea derivatives were synthesized. Their antitumor activities against human breast carcinoma cells (MCF-7) and human colon cancer cells (HCT-116) in vitro were evaluated, using sorafenib as a positive control drug. Anticancer bioassays indicated that several compounds exhibited appreciable anticancer activity against MCF-7 and HCT-116 cells. Particularly, compounds 9g and 8b demonstrated the most significant inhibitory effect against HCT-116 and MCF-7 cells, with inhibition ratios of 25.56% and 26.46%, respectively. Additionally, the synthesized pyridine[2,3-d]pyrimidine derivatives containing a urea group moieties exhibited antitumor activities against MCF-7 and HCT-116 cells in vitro.
Design, synthesis, and biological evaluation of novel benzo[b]thiophene-diaryl urea derivatives as potential anticancer agents
Zarei, Omid,Azimian, Fereshteh,Hamzeh-Mivehroud, Maryam,Shahbazi Mojarrad, Javid,Hemmati, Salar,Dastmalchi, Siavoush
, p. 1438 - 1448 (2020/05/28)
A hybrid pharmacophore approach was applied to design and synthesize a series of benzo[b]thiophene-diaryl urea derivatives 17a–g with potential anticancer effect. In vitro antiproliferative activities of all target compounds were evaluated against HT-29 a
Development of tyrosinase labile protecting groups for amines
Osborn, Helen M. I.,Williams, Nana Aba O.
, p. 3111 - 3113 (2007/10/03)
(Chemical Equation Presented) The development of two novel protecting groups for amines is described. Thus, a range of amines have been converted to ureas, and the deprotection of these upon exposure to mushroom tyrosinase (E.C. 1.14.18.1) has been demonstrated.
Structural refinement of inhibitors of urea-based soluble epoxide hydrolases
Morisseau, Christophe,Goodrow, Marvin H.,Newman, John W.,Wheelock, Craig E.,Dowdy, Deanna L.,Hammock, Bruce D.
, p. 1599 - 1608 (2007/10/03)
The soluble epoxide hydrolase (sEH) is involved in the metabolism of arachidonic, linoleic, and other fatty acid epoxides, endogenous chemical mediators that play an important role in blood pressure regulation and inflammation. 1,3-Disubstituted ureas, carbamates, and amides are new potent and stable inhibitors of sEH. However, the poor solubility of the lead compounds limits their use. Inhibitor structure-activity relationships were investigated to better define the structural requirements for inhibition and to identify points in the molecular topography that could accept polar groups without diminishing inhibition potency. Results indicate that lipophilicity is an important factor controlling inhibitor potency. Polar groups could be incorporated into one of the alkyl groups without loss of activity if they were placed at a sufficient distance from the urea function. The resulting compounds had a 2-fold higher water solubility. These findings will facilitate the rational design and optimization of sEH inhibitors with better physical properties.
