scholarly journals Synthesis Of Diaryl Urea Derivatives and Evaluation of Their Antiproliferative Activities in Colon Adenocarcinoma

2022 ◽  
pp. 132318
Author(s):  
Muhammed GÖMEÇ ◽  
Fatih YULAK ◽  
Hayreddin GEZEGEN ◽  
Mustafa ÖZKARACA ◽  
Koray SAYIN ◽  
...  
Keyword(s):  
Colon Adenocarcinoma ◽  
Urea Derivatives ◽  
Antiproliferative Activities

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

Recent advances in Synthesis and Biological Applications of Substituted Ureas

2021 ◽  
Vol 25 ◽  
Author(s):  
Bharatkumar M. Sapkal ◽  
Shamrao T. Disale ◽  
Raghunath B. Toche ◽  
Dhananjay H. More
Keyword(s):  
Protease Inhibitor ◽  
Biological Activities ◽  
Biological Behavior ◽  
Synthetic Approach ◽  
Biological Applications ◽  
Urea Derivatives ◽  
Heterocyclic Molecules ◽  
Hiv 1 ◽  
Antiproliferative Activities ◽  
Substituted Urea

: In the last few decades, substituted urea derivatives have got significant importance due to their wide applications in pharmaceutical, polymer, dyes, and agriculture industries. Urea derivatives are the key starting material for the synthesis of novel bioactive heterocyclic molecules. Substituted urea derivatives are known to possess a wide array of biological activities such as herbicidal, antimicrobial, antimalarial, antivirus, anticancer, antioxidants, antiproliferative, antiatherosclerotic, anti-inflammatory, antibiotic, sedatives, anticonvulsants and acting as HIV-1 protease inhibitor. Herein, the synthetic approach and its herbicidal, anticonvulsant, antimicrobial, and antiproliferative activities are reviewed. This review summarizes the current updates regarding the syntheses and biological behavior of substituted urea.

scholarly journals Antiproliferative evaluation of various aminoquinoline derivatives

2019 ◽  
Vol 69 (4) ◽  
pp. 661-672
Author(s):  
Branka Zorc ◽  
Zrinka Rajić ◽  
Ivana Perković
Keyword(s):  
Cell Lines ◽  
Urea Derivatives ◽  
Sw620 Cell ◽  
Hct 116 ◽  
Adeno Carcinoma ◽  
Low Activity ◽  
Micromolar Range ◽  
Antiproliferative Activities ◽  
Mcf 7

Abstract Four classes of aminoquinoline derivatives were prepared: primaquine ureas 1a–f, primaquine bis-ureas 2a–f, chloroquine fumardiamides 3a–f and mefloquine fumardiamides 4a–f. Their antiproliferative activities against breast adeno-carcinoma (MCF-7), lung carcinoma (H460) and colon carcinoma (HCT 116 and SW620) cell lines were evaluated in vitro, using MTT cell proliferation assay. The results revealed a low activity of primaquine urea and bis-urea derivatives and high activity of all fumardiamides, with IC50 values in low micromolar range against all tested cancer cell lines.

Concise synthesis and biological activity evaluation of novel pyrazinyl-aryl urea derivatives against several cancer cell lines which especially can induce T24 apoptotic and necroptotic cell death

2021 ◽  
Author(s):  
Jia-Nian Chen ◽  
Chu-Ting Chen ◽  
Yue-Zhen He ◽  
Tai-Sheng Qin ◽  
Li Cheng ◽  
...  
Keyword(s):  
Cell Death ◽  
Biological Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Structural Modification ◽  
Cancer Cell Lines ◽  
Urea Derivatives ◽  
Activity Evaluation ◽  
Antiproliferative Activities

Based on structural modification of regorafenib, 28 pyrazinyl-aryl urea derivatives were synthesized and their in vitro antiproliferative activities were evaluated. Six compounds (5-16, 5-17, 5-18, 5-19, 5-22, and 5-23) exhibited...

scholarly journals Antioxidant and antiproliferative activity of Granny Smith apple pomace

2008 ◽  
pp. 201-212 ◽  
Author(s):  
Sladjana Savatovic ◽  
Gordana Cetkovic ◽  
Sonja Djilas ◽  
Vesna Tumbas ◽  
Jasna Canadanovic-Brunet ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Antioxidant Activities ◽  
Colorimetric Assay ◽  
Colon Adenocarcinoma ◽  
Apple Pomace ◽  
Breast Adenocarcinoma ◽  
Diphenyltetrazolium Bromide ◽  
Spin Resonance ◽  
Ht 29 ◽  
Antiproliferative Activities

Granny Smith apple pomace was subjected to evaluation as valuable source of antioxidant and anticancer phytochemicals on the basis of its content in phenolic compounds, antioxidant and antiproliferative activity. The total cotent of phenolics, flavonoids and flavan-3-ols in apple pomace determined spectrophotometrically, was 7.02 mg/g, 0.51 mg/g and 8.80 mg/g. Major phenolics (phenolic acids, flavan-3-ols, flavonoids and dihydrochalcons) in apple pomace were identified and quantified by HPLC. The antioxidant activity of apple pomace on stable 1,1-diphenyl-2-picrylhydrazyl (DPPH) and reactive hydroxyl radicals, was investigated by electron spin resonance (ESR) spectroscopy. The IC50 DPPH and IC50 OH values of Granny Smith apple pomace were 9.51 mg/ml and 29.17 mg/ml, respectively. The antiproliferative activities of apple pomace on cervix epitheloid carcinoma (HeLa), colon adenocarcinoma (HT-29) and breast adenocarcinoma (MCF7) cell lines were determined according to the MTT (3-(4,5-dimethylthiazol-2-yl)- 2,5-diphenyltetrazolium bromide) colorimetric assay. The IC50 HeLa , IC50 HT-29 and IC50 MCF7 values of Granny Smith apple pomace were 26.40 mg/ml, 22.47 mg/ml and 21.26 mg/ml, respectively. The significant correlations between antioxidant activities and antiproliferative activities were established (p<0.05).

In Vitro and in Vivo Comparison of Binding of 99m-Tc-Iabeled Anti-CEA MAb F33-104 with 99m-Tc-labeled Anti-CEA MAb BW431/26

1999 ◽  
Vol 38 (04) ◽  
pp. 115-119
Author(s):  
N. Oriuchi ◽  
S. Sugiyama ◽  
M. Kuroki ◽  
Y. Matsuoka ◽  
S. Tanada ◽  
...  
Keyword(s):  
Nude Mice ◽  
Binding Capacity ◽  
Colon Adenocarcinoma ◽  
Human Colon ◽  
Cell Binding ◽  
Vitro Binding ◽  
Labeling Method ◽  
Human Colon Adenocarcinoma

Summary Aim: The purpose of this study was to assess the potential for radioimmunodetection (RAID) of murine anti-carcinoembryonic antigen (CEA) monoclonal antibody (MAb) F33-104 labeled with technetium-99m (99m-Tc) by a reduction-mediated labeling method. Methods: The binding capacity of 99m-Tc-labeled anti-CEA MAb F33-104 with CEA by means of in vitro procedures such as immunoradiometric assay and cell binding assay and the biodistribution of 99m-Tc-labeled anti-CEA MAb F33-104 in normal nude mice and nude mice bearing human colon adenocarcinoma LS180 tumor were investigated and compared with 99m-Tc-labeled anti-CEA MAb BW431/26. Results: The in vitro binding rate of 99m-Tc-labeled anti-CEA MAb F33-104 with CEA in solution and attached to the cell membrane was significantly higher than 99m-Tclabeled anti-CEA MAb BW431/261 (31.4 ± 0.95% vs. 11.9 ± 0.55% at 100 ng/mL of soluble CEA, 83.5 ± 2.84% vs. 54.0 ± 2.54% at 107 of LS 180 cells). In vivo, accumulation of 99m-Tc-labeled anti-CEA MAb F33-104 was higher at 18 h postinjection than 99m-Tc-labeled anti-CEA MAb BW431/26 (20.1 ± 3.50% ID/g vs. 14.4 ± 3.30% ID/g). 99m-Tcactivity in the kidneys of nude mice bearing tumor was higher at 18 h postinjection than at 3 h (12.8 ± 2.10% ID/g vs. 8.01 ± 2.40% ID/g of 99m-Tc-labeled anti-CEA MAb F33-104, 10.7 ± 1.70% ID/g vs. 8.10 ± 1.75% ID/g of 99m-Tc-labeled anti-CEA MAb BW431/26). Conclusion: 99m-Tc-labeled anti-CEA MAb F33-104 is a potential novel agent for RAID of recurrent colorectal cancer.

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