Lardic Morgane, Patry Cedric, Duflos Muriel, Guillon Jean, Massip Stephane, Cruzalegui Francisco, Edmonds Thomas, Giraudet Stephanie, Marini Laetitia, Leonce Stephane
Faculty of Pharmacy, Department of Pharmacochemistry, Nantes University, Nantes Atlantique Universities, BioCiT UPRES EA 1155, 1 rue Gaston Veil, Nantes F-44000, France.
J Enzyme Inhib Med Chem. 2006 Jun;21(3):313-25. doi: 10.1080/14756360600741834.
New series of 2(or 3)-arylmethylenenaphtho[2,1-b]furan-3(or 2)-ones were synthesized, characterized and tested for anticancer properties in vitro. The target compounds were prepared by Knoevenagel coupling between the naphthofuranones 3, 28-30 and formyl derivatives. 2-(4-Oxo-1-benzopyran-3-ylmethylene)naphtho[2,1-b]furan-3-one 36 was the most active compound (IC50 (L1210) = 1.6 microM). These compounds were also evaluated, in an independent manner, as inhibitors of Src protein tyrosine kinase, but only minor activity was observed.
合成了一系列新的2（或3）-芳基亚甲基萘并[2,1-b]呋喃-3（或2）-酮，对其进行了表征并测试了体外抗癌特性。目标化合物通过萘并呋喃酮3、28 - 30与甲酰基衍生物之间的Knoevenagel缩合反应制备。2-（4-氧代-1-苯并吡喃-3-基亚甲基）萘并[2,1-b]呋喃-3-酮36是活性最高的化合物（IC50（L1210）= 1.6 microM）。还以独立的方式评估了这些化合物作为Src蛋白酪氨酸激酶抑制剂的活性，但仅观察到轻微活性。
