Synthesis, antiviral, cytotoxic and cytostatic evaluation of N 1-(phosphonoalkyl)uracil derivatives
作者:Dorota Rygielska-Tokarska、Graciela Andrei、Dominique Schols、Robert Snoeck、Iwona E. Głowacka
DOI:10.1007/s00706-016-1701-2
日期:2016.6
closure. Under standard conditions (NCS; NBS; I2/CAN) all N 1-(phosphonoalkyl)uracils were transformed into the respective 5-halogeno derivatives to be later benzoylated at N3. All compounds were evaluated in vitro for activity against a broad variety of DNA and RNA viruses. One compound was slightly active against human cytomegalovirus in HEL cell cultures (EC50 = 45 μM) while another showed weak activity
摘要一系列N 1 -(膦酰基烷基)尿嘧啶由ω -氨基烷基膦酸酯和 ( E )-3-乙氧基丙烯酰基异氰酸酯按两步反应顺序制备,然后进行尿嘧啶闭环。在标准条件下(NCS;NBS;I 2 /CAN),所有N 1 -(膦酰基烷基)尿嘧啶都转化为各自的 5-卤代衍生物,随后在 N3 处苯甲酰化。所有化合物都在体外评估了对多种 DNA 和 RNA 病毒的活性。一种化合物在 HEL 细胞培养物中对人巨细胞病毒有轻微活性(EC 50 = 45 μM),而另一种化合物对水痘带状疱疹病毒(TK +VZV 菌株 OKA 和 TK - VZV 菌株 07-1),EC 50 = 43 和 53 µM,分别。此外,几种化合物在低于 200 μM 的浓度下对人宫颈癌细胞 (HeLa) 的增殖具有明显的抑制作用。 图形概要