Synthesis of novel substituted pyrimidine derivatives bearing a sulfamide group and their in vitro cancer growth inhibition activity

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• 作者：Carole-Anne Lefebvre^a ; ¹ ; Elsa Forcellini^a ; ¹ ; Sophie Boutin^a ; Marie-France Cô ; té ; ^b ; René ; C.-Gaudreault^b ; ^c ; Patrick Mathieu^d ; Patrick Lagü ; e^e ; Jean-Fran&ccedil ; ois Paquin^a ; ^{jean-francois.paquin@chm.ulaval.ca}
• 关键词：Pyrimidine ; Sulfamide ; Anticancer activities ; Structure-activity relationships (SARs) ; Growth inhibition
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：27
• 期：2
• 页码：299-302
• 全文大小：560 K
• 卷排序：27

文摘

The synthesis of two series of novel substituted pyrimidine derivatives bearing a sulfamide group have been described and their in vitro cancer growth inhibition activities have been evaluated against three human tumour cell lines (HT-29, M21, and MCF7). In general, growth inhibition activity has been enhanced by the introduction of a bulky substituent on the aromatic ring with the best compound having GI50 < 6 μM for all the human tumour cell lines. The MCF7 selective compounds were evaluated on four additional human invasive breast ductal carcinoma cell lines (MDA-MB-231, MDA-MB-468, SKBR3, and T47D) and were selective against T47D cell line in all cases except one, suggesting a potential antiestrogen activity.