About: ABSTRACT: A series of N (1)-(phosphonoalkyl)uracils was prepared in a two-step reaction sequence from ω-aminoalkylphosphonates and (E)-3-ethoxyacryloyl isocyanate followed by the uracil ring closure. Under standard conditions (NCS; NBS; I(2)/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 (EC(50) = 45 μM) while another showed weak activity against varicella-zoster virus (TK(+) VZV strain OKA and TK(−) VZV strain 07-1) with EC(50) = 43 and 53 µM, respectively. In addition, several compounds exhibited noticeable inhibitory effects on the proliferation of human cervical carcinoma cells (HeLa) at a concentration lower than 200 μM. GRAPHICAL ABSTRACT: [Image: see text]   Goto Sponge  NotDistinct  Permalink

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  • ABSTRACT: A series of N (1)-(phosphonoalkyl)uracils was prepared in a two-step reaction sequence from ω-aminoalkylphosphonates and (E)-3-ethoxyacryloyl isocyanate followed by the uracil ring closure. Under standard conditions (NCS; NBS; I(2)/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 (EC(50) = 45 μM) while another showed weak activity against varicella-zoster virus (TK(+) VZV strain OKA and TK(−) VZV strain 07-1) with EC(50) = 43 and 53 µM, respectively. In addition, several compounds exhibited noticeable inhibitory effects on the proliferation of human cervical carcinoma cells (HeLa) at a concentration lower than 200 μM. GRAPHICAL ABSTRACT: [Image: see text]
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  • Virology
  • Physical chemistry
  • Varicelloviruses
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