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Synthesis and in vitro antiproliferative activity of new 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea scaffold-based compounds

A new series of 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea derivatives were synthesized and subjected to in vitro antiproliferative screening against National Cancer Institute (NCI)-60 human cancer cell lines of nine different cancer types. Fourteen compounds 5a-n were synthesized with three different...

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Main Authors: Al-Sanea, Mohammad M., Ali Khan, Mohammed Safwan, Abdelazem, Ahmed Z., Lee, So Ha, Mok, Pooi Ling, Gamal, Mohammed, Shaker, Mohamed E., Afzal, Muhammad, Youssif, Bahaa G. M., Omar, Nesreen Nabil
Format: Article
Language:English
Published: MDPI 2018
Online Access:http://psasir.upm.edu.my/id/eprint/74054/1/Synthesis%20and%20In%20vitro%20antiproliferative%20activity%20of%20new%201-phenyl-3-%284-%28pyridin-3-yl%29phenyl%29urea%20scaffold-based%20compounds.pdf
http://psasir.upm.edu.my/id/eprint/74054/
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spelling my.upm.eprints.740542020-04-28T03:33:52Z http://psasir.upm.edu.my/id/eprint/74054/ Synthesis and in vitro antiproliferative activity of new 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea scaffold-based compounds Al-Sanea, Mohammad M. Ali Khan, Mohammed Safwan Abdelazem, Ahmed Z. Lee, So Ha Mok, Pooi Ling Gamal, Mohammed Shaker, Mohamed E. Afzal, Muhammad Youssif, Bahaa G. M. Omar, Nesreen Nabil A new series of 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea derivatives were synthesized and subjected to in vitro antiproliferative screening against National Cancer Institute (NCI)-60 human cancer cell lines of nine different cancer types. Fourteen compounds 5a-n were synthesized with three different solvent exposure moieties (4-hydroxylmethylpiperidinyl and trimethoxyphenyloxy and 4-hydroxyethylpiperazine) attached to the core structure. Substituents with different π and σ values were added on the terminal phenyl group. Compounds 5a-e with a 4-hydroxymethylpiperidine moiety showed broad-spectrum antiproliferative activity with higher mean percentage inhibition values over the 60-cell line panel at 10 µM concentration. Compound 5a elicited lethal rather than inhibition effects on SK-MEL-5 melanoma cell line, 786-0, A498, RXF 393 renal cancer cell lines, and MDA-MB-468 breast cancer cell line. Two compounds, 5a and 5d showed promising mean growth inhibitions and thus were further tested at five-dose mode to determine median inhibitory concentration (IC50) values. The data revealed that urea compounds 5a and 5d are the most active derivatives, with significant efficacies and superior potencies than paclitaxel in 21 different cancer cell lines belonging particularly to renal cancer and melanoma cell lines. Moreover, 5a and 5d had superior potencies than gefitinib in 38 and 34 cancer cell lines, respectively, particularly colon cancer, breast cancer and melanoma cell lines. MDPI 2018 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/74054/1/Synthesis%20and%20In%20vitro%20antiproliferative%20activity%20of%20new%201-phenyl-3-%284-%28pyridin-3-yl%29phenyl%29urea%20scaffold-based%20compounds.pdf Al-Sanea, Mohammad M. and Ali Khan, Mohammed Safwan and Abdelazem, Ahmed Z. and Lee, So Ha and Mok, Pooi Ling and Gamal, Mohammed and Shaker, Mohamed E. and Afzal, Muhammad and Youssif, Bahaa G. M. and Omar, Nesreen Nabil (2018) Synthesis and in vitro antiproliferative activity of new 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea scaffold-based compounds. Molecules, 23 (297). pp. 1-13. ISSN 1420-3049; ESSN: 1420-3049 10.3390/molecules23020297.
institution Universiti Putra Malaysia
building UPM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Putra Malaysia
content_source UPM Institutional Repository
url_provider http://psasir.upm.edu.my/
language English
description A new series of 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea derivatives were synthesized and subjected to in vitro antiproliferative screening against National Cancer Institute (NCI)-60 human cancer cell lines of nine different cancer types. Fourteen compounds 5a-n were synthesized with three different solvent exposure moieties (4-hydroxylmethylpiperidinyl and trimethoxyphenyloxy and 4-hydroxyethylpiperazine) attached to the core structure. Substituents with different π and σ values were added on the terminal phenyl group. Compounds 5a-e with a 4-hydroxymethylpiperidine moiety showed broad-spectrum antiproliferative activity with higher mean percentage inhibition values over the 60-cell line panel at 10 µM concentration. Compound 5a elicited lethal rather than inhibition effects on SK-MEL-5 melanoma cell line, 786-0, A498, RXF 393 renal cancer cell lines, and MDA-MB-468 breast cancer cell line. Two compounds, 5a and 5d showed promising mean growth inhibitions and thus were further tested at five-dose mode to determine median inhibitory concentration (IC50) values. The data revealed that urea compounds 5a and 5d are the most active derivatives, with significant efficacies and superior potencies than paclitaxel in 21 different cancer cell lines belonging particularly to renal cancer and melanoma cell lines. Moreover, 5a and 5d had superior potencies than gefitinib in 38 and 34 cancer cell lines, respectively, particularly colon cancer, breast cancer and melanoma cell lines.
format Article
author Al-Sanea, Mohammad M.
Ali Khan, Mohammed Safwan
Abdelazem, Ahmed Z.
Lee, So Ha
Mok, Pooi Ling
Gamal, Mohammed
Shaker, Mohamed E.
Afzal, Muhammad
Youssif, Bahaa G. M.
Omar, Nesreen Nabil
spellingShingle Al-Sanea, Mohammad M.
Ali Khan, Mohammed Safwan
Abdelazem, Ahmed Z.
Lee, So Ha
Mok, Pooi Ling
Gamal, Mohammed
Shaker, Mohamed E.
Afzal, Muhammad
Youssif, Bahaa G. M.
Omar, Nesreen Nabil
Synthesis and in vitro antiproliferative activity of new 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea scaffold-based compounds
author_facet Al-Sanea, Mohammad M.
Ali Khan, Mohammed Safwan
Abdelazem, Ahmed Z.
Lee, So Ha
Mok, Pooi Ling
Gamal, Mohammed
Shaker, Mohamed E.
Afzal, Muhammad
Youssif, Bahaa G. M.
Omar, Nesreen Nabil
author_sort Al-Sanea, Mohammad M.
title Synthesis and in vitro antiproliferative activity of new 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea scaffold-based compounds
title_short Synthesis and in vitro antiproliferative activity of new 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea scaffold-based compounds
title_full Synthesis and in vitro antiproliferative activity of new 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea scaffold-based compounds
title_fullStr Synthesis and in vitro antiproliferative activity of new 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea scaffold-based compounds
title_full_unstemmed Synthesis and in vitro antiproliferative activity of new 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea scaffold-based compounds
title_sort synthesis and in vitro antiproliferative activity of new 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea scaffold-based compounds
publisher MDPI
publishDate 2018
url http://psasir.upm.edu.my/id/eprint/74054/1/Synthesis%20and%20In%20vitro%20antiproliferative%20activity%20of%20new%201-phenyl-3-%284-%28pyridin-3-yl%29phenyl%29urea%20scaffold-based%20compounds.pdf
http://psasir.upm.edu.my/id/eprint/74054/
_version_ 1665896005317427200
score 13.211869

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