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Molecules 2018, 23(6), 1459;

Pyridine-Ureas as Potential Anticancer Agents: Synthesis and In Vitro Biological Evaluation

Chemistry Department, Faculty of Sciences, University of Sharjah, Sharjah 27272, UAE
Department of Chemistry, Chemistry Research Laboratory, University of Oxford, 12 Mansfield Road, Oxford OX1 3TA, UK
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Egyptian Russian University, Badr City, Cairo 11829, Egypt
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kafrelsheikh University, Kafrelsheikh 33516, Egypt
Department of Applied Organic Chemistry, National Research Center, Dokki, Cairo 12622, Egypt
Author to whom correspondence should be addressed.
Academic Editors: Simona Collina and Mariarosaria Miloso
Received: 23 May 2018 / Revised: 12 June 2018 / Accepted: 12 June 2018 / Published: 15 June 2018
(This article belongs to the Special Issue Recent Advances in Anticancer Drugs)
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In our endeavor towards the development of effective anticancer agents, a novel series of pyridine-ureas 8an were synthesized. All the newly prepared derivatives were evaluated in vitro for their growth inhibitory activity towards the proliferation of breast cancer MCF-7 cell line. Compounds 8e and 8n were found to be the most active congeners against MCF-7 cells (IC50 = 0.22 and 1.88 µM after 48 h treatment; 0.11 and 0.80 µM after 72 h treatment, respectively) with increased activity compared to the reference drug doxorubicin (IC50 = 1.93 µM). Moreover, eight selected pyridines 8b, 8d, 8e, 8i, 8j and 8ln were evaluated for their in vitro anticancer activity according to the US-NCI protocol. Pyridines 8b and 8e proved to be the most effective anticancer agents in the NCI assay with mean inhibition = 43 and 49%, respectively. Both 8b and 8e exhibited anti-proliferative activity against all tested cancer cell lines from all subpanels growth inhibition (GI for 8b; 12–78%, GI for 8e; 15–91%). Pyridines 8b and 8e were screened in vitro for their inhibitory activity against VEGFR-2. Both compounds inhibited VEGFR-2 at micromolar IC50 values 5.0 ± 1.91 and 3.93 ± 0.73 µM, respectively. The most active pyridines were filtered according to the Lipinski and Veber rules and all of them passed these filters. Finally, several ADME descriptors were predicted for the active pyridines through a theoretical kinetic study. View Full-Text
Keywords: pyridine-urea; breast cancer; anticancer; VEGFR-2; synthesis; ADME pyridine-urea; breast cancer; anticancer; VEGFR-2; synthesis; ADME

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El-Naggar, M.; Almahli, H.; Ibrahim, H.S.; Eldehna, W.M.; Abdel-Aziz, H.A. Pyridine-Ureas as Potential Anticancer Agents: Synthesis and In Vitro Biological Evaluation. Molecules 2018, 23, 1459.

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