title: Synthesis of novel substituted pyrimidine derivatives bearing a sulfamide group and their in vitro cancer growth inhibition activity.
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<6μM 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.
authors.affiliation: PROTEO, Département de chimie, Université Laval, Québec, QC G1V 0A6, Canada.
authors.forename: Carole-Anne
authors.initials: CA
authors.lastname: Lefebvre
authors.affiliation: PROTEO, Département de chimie, Université Laval, Québec, QC G1V 0A6, Canada.
authors.forename: Elsa
authors.initials: E
authors.lastname: Forcellini
authors.affiliation: PROTEO, Département de chimie, Université Laval, Québec, QC G1V 0A6, Canada.
authors.forename: Sophie
authors.initials: S
authors.lastname: Boutin
authors.affiliation: CHU de Québec Research Centre, Oncology Division, Hôpital Saint-François d'Assise, Québec, QC G1L 3L5, Canada.
authors.forename: Marie-France
authors.initials: MF
authors.lastname: Côté
authors.affiliation: CHU de Québec Research Centre, Oncology Division, Hôpital Saint-François d'Assise, Québec, QC G1L 3L5, Canada; Department of Molecular Medicine, Faculty of Medicine, Université Laval, Québec, QC G1V 0A6, Canada.
authors.forename: René
authors.initials: R
authors.lastname: C-Gaudreault
authors.affiliation: Laboratory of Cardiovascular Pathobiology, Quebec Heart and Lung Institute/Research Center, Department of Surgery, Université Laval, QC G1V-4G5, Canada.
authors.forename: Patrick
authors.initials: P
authors.lastname: Mathieu
authors.affiliation: PROTEO, IBIS, Département de biochimie, de microbiologie et de bio-informatique, Université Laval, Québec, QC G1V 0A6, Canada.
authors.forename: Patrick
authors.initials: P
authors.lastname: Lagüe
authors.affiliation: PROTEO, Département de chimie, Université Laval, Québec, QC G1V 0A6, Canada. Electronic address: jean-francois.paquin@chm.ulaval.ca.
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Paquin
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011743:Pyrimidines; D013449:Sulfonamides; C030986:pyrimidine
keywords: Anticancer activities; Growth inhibition; Pyrimidine; Structure-activity relationships (SARs); Sulfamide