Synthesis of novel substituted pyrimidine derivatives bearing a sulfamide group and their in vitro cancer growth inhibition activity |
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| Authors: | Carole-Anne Lefebvre Elsa Forcellini Sophie Boutin Marie-France Côté René C.-Gaudreault Patrick Mathieu Patrick Lagüe Jean-François Paquin |
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| Affiliation: | 1. PROTEO, Département de chimie, Université Laval, Québec, QC G1V 0A6, Canada;2. CHU de Québec Research Centre, Oncology Division, Hôpital Saint-François d’Assise, Québec, QC G1L 3L5, Canada;3. Department of Molecular Medicine, Faculty of Medicine, Université Laval, Québec, QC G1V 0A6, Canada;4. Laboratory of Cardiovascular Pathobiology, Quebec Heart and Lung Institute/Research Center, Department of Surgery, Université Laval, QC G1V-4G5, Canada;5. PROTEO, IBIS, Département de biochimie, de microbiologie et de bio-informatique, Université Laval, Québec, QC G1V 0A6, Canada |
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| Abstract: | 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. |
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| Keywords: | Pyrimidine Sulfamide Anticancer activities Structure-activity relationships (SARs) Growth inhibition |
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