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Novel pyrrol-2(3H)-ones and pyridazin-3(2H)-ones carrying quinoline scaffold as anti-proliferative tubulin polymerization inhibitors

Publication date:

October 2018


Source:Bioorganic Chemistry, Volume 80

Author(s): Mahmoud S. Abdelbaset, Gamal El-Din A. Abuo-Rahma, Mostafa H. Abdelrahman, Mohamed Ramadan, Bahaa G.M. Youssif, Syed Nasir Abbas Bukhari, Mamdouh F.A. Mohamed, Mohamed Abdel-Aziz

A novel quinolinyl pyrrolone and quinolinyl pyridazinone derivatives has been synthesized and characterized using different spectroscopic and elemental analysis techniques. Most of the target compounds displayed promising antiproliferative activity; In general, the pyrrolone derivatives 4a-f exhibited higher antiproliferative activity than their corresponding pyridazinone. The pyrrolone 4f showed outstanding antiproliferative activity with moderate selectivity against CNS and renal cancer with selectivity ratio of 3.49 and 3.56, respectively. Compound 4e and 5d experienced tubulin polymerization inhibitory activity comparable to that of vincristine while 4c, 4e and 4d showed good BRAF kinase inhibition compared to Erlotinib. Docking of compound 4e into colchicine binding site and biological assay results revealed that these compounds act mainly through tubulin polymerization inhibitory mechanism and can exhibit pre G1 apoptosis and cell cycle arrest at G2/M phase.
Graphical abstract




Autoren:   Author(s): Mahmoud S. Abdelbaset, Gamal El-Din A. Abuo-Rahma, Mostafa H. Abdelrahman, Mohamed Ramadan, Bahaa G.M. Youssif, Syed Nasir Abbas Bukhari, Mamdouh F.A. Mohamed, Mohamed Abdel-Aziz
Journal:   Bioorganic Chemistry
Band:   80
Jahrgang:   2018
Seiten:   151
DOI:   10.1016/j.bioorg.2018.06.003
Erscheinungsdatum:   25.06.2018
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