Design, synthesis and antiproliferative activities of diaryl urea derivatives bearing N-acylhydrazone moiety

2012 ◽  
Vol 23 (8) ◽  
pp. 915-918 ◽  
Author(s):  
Bei Zhang ◽  
Yan Fang Zhao ◽  
Xin Zhai ◽  
Wei Jie Fan ◽  
Jun Ling Ren ◽  
...  
Keyword(s):  
Urea Derivatives ◽  
Design Synthesis ◽  
Antiproliferative Activities

Design, synthesis and antiproliferative activities of novel 5H-pyridazino[4,5-b]indoles

2007 ◽  
Vol 18 (10) ◽  
pp. 1191-1194 ◽  
Author(s):  
Rong Dong Li ◽  
Xin Zhai ◽  
Yan Fang Zhao ◽  
Ping Gong
Keyword(s):  
Design Synthesis ◽  
Antiproliferative Activities

Design, Synthesis and Antiproliferative Activities of Diaryl Thiourea Derivatives as Anticancer Agents

2012 ◽  
Vol 30 (10) ◽  
pp. 2423-2430 ◽  
Author(s):  
Jianwen Yao ◽  
Zuopeng He ◽  
Jing Chen ◽  
Daquan Chen ◽  
Wei Sun ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Design Synthesis ◽  
Thiourea Derivatives ◽  
Antiproliferative Activities

Structure-Based Design, Synthesis and Molecular Modeling Studies of Thiazolyl Urea Derivatives as Novel Anti-Parkinsonian Agents

2012 ◽  
Vol 8 (6) ◽  
pp. 1057-1068
Author(s):  
Faizul Azam ◽  
Medapati Vijaya Vara Prasad ◽  
Neelaveni Thangavel ◽  
Anil Kumar Shrivastava ◽  
Govind Mohan
Keyword(s):  
Molecular Modeling ◽  
Urea Derivatives ◽  
Design Synthesis ◽  
Modeling Studies ◽  
Molecular Modeling Studies

scholarly journals N,N′-Disubstituted thiourea and urea derivatives: design, synthesis, docking studies and biological evaluation against nitric oxide synthase

MedChemComm ◽  
2016 ◽  
Vol 7 (4) ◽  
pp. 667-678 ◽  
Author(s):  
Mariem Chayah ◽  
M. Encarnación Camacho ◽  
M. Dora Carrión ◽  
Miguel A. Gallo ◽  
Miguel Romero ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Urea Derivatives ◽  
Design Synthesis ◽  
Inos Inhibitors ◽  
Oxide Synthase

N,N′-Disubstituted thioureas and ureas as nNOS and iNOS inhibitors were synthesized. Thiourea 4g was the best inhibitor without eNOS inhibition.

scholarly journals Design, synthesis and evaluation of belinostat analogs as histone deacetylase inhibitors

2019 ◽  
Vol 11 (21) ◽  
pp. 2765-2778
Author(s):  
Jie-Huan Zhang ◽  
Madhusoodanan Mottamal ◽  
Hai-Shan Jin ◽  
Shanchun Guo ◽  
Yan Gu ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Active Compound ◽  
Histone Deacetylase Inhibitors ◽  
Hdac Inhibitors ◽  
Antitumor Therapy ◽  
Design Synthesis ◽  
Inhibitory Activities ◽  
Antiproliferative Activities

Aim: Histone deacetylase (HDAC) is an attractive target for antitumor therapy. Therefore, the development of novel HDAC inhibitors is warranted. Materials & methods: A series of HDAC inhibitors based on N-hydroxycinnamamide fragment was designed as the clinically used belinostat analog using amide as the connecting unit. All target compounds were evaluated for their in vitro HDAC inhibitory activities and some selected compounds were tested for their antiproliferative activities. Conclusion: Among them, compound 7e showed an IC50 value of 11.5 nM in inhibiting the HDAC in a pan-HDAC assay, being the most active compound of the series.

scholarly journals Chloroquine Urea Derivatives: Synthesis and Antitumor Activity in Vitro

2018 ◽  
Vol 68 (4) ◽  
pp. 471-483 ◽  
Author(s):  
Kristina Pavić ◽  
Zrinka Rajić ◽  
Zvonimir Mlinarić ◽  
Lidija Uzelac ◽  
Marijeta Kralj ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Urea Derivatives ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Lead Compounds ◽  
Insight Into

Abstract In the current paper, we describe the design, synthesis and antiproliferative screening of novel chloroquine derivatives with a quinoline core linked to a hydroxy or halogen amine through a flexible aminobutyl chain and urea spacer. Synthetic pathway leading to chloroquine urea derivatives 4-10 includes two crucial steps: i) synthesis of chloroquine benzotriazolide 3 and ii) formation of urea derivatives through the reaction of compound 3 with the corresponding amine. Testing of antiproliferative activity against four human cancer cell lines revealed that chloroquine urea derivatives 9 and 10 with aromatic moieties show activity at micromolar concentrations. Therefore, these molecules represent interesting lead compounds that might provide an insight into the design of new anticancer agents.

Design, synthesis, and biological evaluation of tetrahydroisoquinoline-based diaryl urea derivatives for suppressing VEGFR-2 signaling

2019 ◽  
Vol 30 (5) ◽  
pp. 508-516 ◽  
Author(s):  
Yuanzheng Huang ◽  
Yang Zhang ◽  
Jiaming Li ◽  
Xiaodong Ma ◽  
Mengqi Hu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Urea Derivatives ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis, molecular docking and cytotoxic activity of novel urea derivatives of 2-amino-3-carbomethoxythiophene

2020 ◽  
Vol 132 (1) ◽  
Author(s):  
Venugopalarao Vikram ◽  
Srinivasa R Penumutchu ◽  
Raviraj Vankayala ◽  
Suresh Thangudu ◽  
Karteek Rao Amperayani ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Cytotoxic Activity ◽  
Urea Derivatives ◽  
Design Synthesis ◽  
Derivatives Of

Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents

2014 ◽  
Vol 77 ◽  
pp. 351-360 ◽  
Author(s):  
Chenshu Lu ◽  
Ke Tang ◽  
Yan Li ◽  
Peng Li ◽  
Ziyun Lin ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Urea Derivatives ◽  
Design Synthesis ◽  
Potential Antitumor
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