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<p>Evaluation of <em>in vitro </em>and <em>in vivo </em>Cytotoxic Activities and Kinase Inhibition of Newly Synthesized Cyclo (<em>N<sup>α</sup></em>-Dinicotinoyl)-Bis-[(L-Valinyl)-L-Lysine Methyl Ester]</p>

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Title Statement <p>Evaluation of <em>in vitro </em>and <em>in vivo </em>Cytotoxic Activities and Kinase Inhibition of Newly Synthesized Cyclo (<em>N<sup>α</sup></em>-Dinicotinoyl)-Bis-[(L-Valinyl)-L-Lysine Methyl Ester]</p>
 
Added Entry - Uncontrolled Name Amr, A E; Pharmaceutical Chemistry Department, College of Pharmacy, Drug Exploration & Development Chair (DEDC), King Saud University, Riyadh 11451, Saudi Arabia. Applied Organic Chemistry Department, National Research Center, Cairo, Dokki 12622, Egypt.
Al –Omar, M A; Applied Organic Chemistry Department, National Research Center, Cairo, Dokki 12622, Egypt.
Elsayed, E A; Bioproducts Research Chair, Zoology Department, College of Science, King Saud University, Riyadh 11451, Kingdom of Saudi Arabia Natural and Microbial Products Department, National Research Centre, Dokki, Cairo 12311, Egypt
Azab, Mohammad E.; Synthetic Organic Lab, Chemistry Department, Faculty of Science, Ain Shams University, Abbassia, Cairo 11566, Egypt
Sabry, Nermien M.; Applied Organic Chemistry Department, National Research Center, Cairo, Dokki 12622, Egypt.
 
Uncontrolled Index Term in vitro cytotoxicity, in vivo antiprostate, Macrocyclic tripeptidopyridine ester, VEGFR-2 kinase activity
 
Summary, etc. <p>Cancer is a major risk disease affecting human survival. The pharmaceutical companies are continuing searching for new drug candidates with promising anticancer activities, and reduced side effects. The current work aimed at synthesized a new tripeptide with potential pharmacological properties. L-Valine methyl ester was used to prepare cyclo (<em>N<sup>α</sup></em>-dinicotinoyl)-bis-[(L-valinyl)-L-lysine methyl ester. The new compound revealed promising <em>in vitro</em> cytotoxic activities against different neuroblastoma, cervical carcinoma, fibrosarcoma as well as hepatocellular carcinomas. Furthermore, we also found that the obtained IC<sub>50</sub> of the compound decreased by about 50% during its <em>in vivo </em>anti-prostate cancer evaluation. Furthermore, the mechanism of action studies proposes that the new prepared derivative affects cancer cells trough the inhibition of VEGFR-2 kinase enzyme.</p>
 
Publication, Distribution, Etc. Journal of Scientific & Industrial Research
2022-11-19 05:33:33
 
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http://op.niscair.res.in/index.php/JSIR/article/view/68647
 
Data Source Entry Journal of Scientific & Industrial Research; ##issue.vol## 79, ##issue.no## 3 (2020): Journal of Scientific & Industrial Research
 
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