RT Journal Article SR Electronic T1 Inhibition of Endothelial Cell Proliferation by per-O-acetylated Mannose Conjugates JF Anticancer Research JO Anticancer Res FD International Institute of Anticancer Research SP 1331 OP 1335 VO 27 IS 3A A1 ZARIC, VIOLETA A1 DOYLE, DEARBHLA A1 MURPHY, PAUL V. A1 O'BOYLE, KATHY M. YR 2007 UL http://ar.iiarjournals.org/content/27/3A/1331.abstract AB Background: The inhibition of angiogenesis, defined as the process of new blood vessel formation, represents a promising strategy for treating cancer. Materials and Methods: The inhibitory properties of two N-(per-O-acetylated-β-D- mannopyranosyl)-thiophene-2-carboxamides derivatives (AMTCs, [1],[2]), N-(2,3,4,6-tetra-O-ethoxycarbonyl-β-D-mannopyranosyl)-thiophene-2-carboxamide [3] and of 2,3,4,6-tetra-O-acetyl-β-D-mannopyranosyl-acetamide [4] on the growth of bovine aortic endothelial cells (BAECs) induced by basic fibroblast growth factor (bFGF) were assessed using a [3H]thymidine incorporation assay. The cellular uptake of AMTCs and the non-acetylated homologue (MTC) into BAEC were compared using mass spectrometry analysis of cell lysates. Results: AMTCs [1],[2]), at 80 μM, reversed the increase of [3H]thymidine incorporation induced by bFGF, suggesting that these compounds inhibited bFGF-induced proliferative response in BAECs. The acetamide [4] was inactive showing the importance of the thiophene carboxamide for biological activity. The results of a study of AMTC uptake into BAEC suggest that AMTC is rapidly converted to its non-acetylated counterpart. Conclusion: The promising results obtained with AMTCs as inhibitors of BAEC growth could lead to the development of novel angiogenesis inhibitors. Copyright© 2007 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved