Kiran Y B, Devendranath Reddy C, Gunasekar D, Suresh Reddy C, Leon Annette, Barbosa Luiz C A
Department of Chemistry, Sri Venkateswara University, Tirupati 517502, Andhra Pradesh, India.
Eur J Med Chem. 2008 Apr;43(4):885-92. doi: 10.1016/j.ejmech.2007.05.014. Epub 2007 Jun 7.
Novel bis-heterocyclic bisphosphonates/phosphonamidates were synthesized utilizing the Pudovick reaction. The employment of Nb(2)O(5) as catalyst was found to increase the yields and purity of the bisbenzoxazaphosphine derivatives (13a-h). Their anticancer activity studies in vitro, on three human tumor cell lines NCI-H460 (lung large cell), MCF-7 (breast adenocarcinoma), and SF-268 (central nervous system glioblastoma), showed that bis-[3-(3-chloro-4-fluorophenyl)-2-oxo-3,4-dihydro-2H-2lambda(5)-benzo[e][1,3,2]oxazaphosphinin-2-yl]arylmethanes (13a-h) and [(4-chlorophenyl)-(hydroxyamidophosphinoyl)-methyl]phosphonic acid (14) exhibited significant anticancer activity.
利用普多维克反应合成了新型双杂环双膦酸酯/磷酰胺酯。发现使用五氧化二铌作为催化剂可提高双苯并恶唑磷衍生物（13a - h）的产率和纯度。它们对三种人类肿瘤细胞系NCI - H460（肺大细胞）、MCF - 7（乳腺腺癌）和SF - 268（中枢神经系统胶质母细胞瘤）的体外抗癌活性研究表明，双-[3-(3 - 氯 - 4 - 氟苯基)-2 - 氧代 - 3,4 - 二氢 - 2H - 2λ(5)-苯并[e][1,3,2]恶唑磷杂环戊二烯 - 2 - 基]芳基甲烷（13a - h）和[(4 - 氯苯基)-(羟基氨基磷酰基)-甲基]膦酸（14）表现出显著的抗癌活性。
