Synthesis of new diarylamides with pyrimidinyl pyridine scaffold and evaluation of their anti-proliferative effect on cancer cell lines

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• 作者：Ahmed Z. Abdelazem^a ; ^b ; ^d ; ^{aznagi2003@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; Mohammad M. Al-Sanea^a ; ^b ; ^e ; Hyun-Mee Park^c ; So Ha Lee^a ; ^b
• 关键词：Synthesis ; Anti-proliferative effect ; Pyrimidinyl pyridine ; Diarylamide ; Melanoma
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 February 2016
• 年：2016
• 卷：26
• 期：4
• 页码：1301-1304
• 全文大小：2147 K

文摘

A new series of diarylamides, having a pyrimidinyl pyridine scaffold, was designed and synthesized. The target compounds were synthesized in three steps. A selected group from the target compounds was tested over a panel of 60 cancer cell lines at a single dose concentration of 10 μM, and the most active compound, 5j, was further tested in a five-dose testing mode to determine its IC₅₀ value over the 60 cell lines. In single-dose testing mode, compound 5j showed the highest growth inhibition against the NCI-60 cancer cell lines, while other tested compounds showed a weak to moderate inhibitory activity against a range of different cancer cell lines. In five-dose testing mode, compound 5j showed strong inhibitory activity in micro molar range against many cancer cell lines. Its major activity was against melanoma cancer cell lines. Therefore, compound 5j is a promising hit compound targeting this severe form of cancer.