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Design, Synthesis, and Evaluation of ω‐(Isothiocyanato)alkylphosphinates and Phosphine Oxides as Antiproliferative Agents
ChemMedChem ( IF 3.6 ) Pub Date : 2017-12-06 , DOI: 10.1002/cmdc.201700619 Łukasz Janczewski 1 , Mateusz Psurski 2 , Marta Świtalska 2 , Anna Gajda 1 , Tomasz M. Goszczyński 2 , Józef Oleksyszyn 3 , Joanna Wietrzyk 2 , Tadeusz Gajda 1
ChemMedChem ( IF 3.6 ) Pub Date : 2017-12-06 , DOI: 10.1002/cmdc.201700619 Łukasz Janczewski 1 , Mateusz Psurski 2 , Marta Świtalska 2 , Anna Gajda 1 , Tomasz M. Goszczyński 2 , Józef Oleksyszyn 3 , Joanna Wietrzyk 2 , Tadeusz Gajda 1
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A series of 21 novel, structurally diverse ω‐(isothiocyanato)alkylphosphinates and phosphine oxides (ITCs) were designed and synthesized in moderate to good yields. The synthesized compounds were evaluated for in vitro antiproliferative activity using LoVo and LoVo/DX cancer cell lines. The biological activity of the synthesized compounds was higher than that of natural isothiocyanates such as benzyl isothiocyanate or sulforaphane. The antiproliferative activity of selected ITCs was also tested on selected cancer cell lines: A549, MESSA and MESSA/DX‐5, HL60 and HL60MX2, BALB/3T3, and 4T1. These compounds were assessed for their mechanism of action as inducers of cell‐cycle arrest and apoptosis. Ethyl (6‐isothiocyanatohexyl)(phenyl)phosphinate (71) was tested in vivo on the 4T1 cell line and demonstrated moderate antitumor activity, similar to that benzyl isothiocyanate and cyclophosphamide.
中文翻译：
抗增殖剂ω-（异硫氰酸根合）烷基次膦酸酯和氧化膦的设计，合成和评价
设计并合成了一系列21种新颖的，结构多样的ω-（异硫氰酸根合）烷基次膦酸酯和氧化膦（ITC），并以中等至良好的产率合成。使用LoVo和LoVo / DX癌细胞系评估了合成的化合物的体外抗增殖活性。合成的化合物的生物活性高于天然异硫氰酸酯，例如异硫氰酸苄酯或萝卜硫烷。还对选定的癌细胞系：A549，MESSA和MESSA / DX-5，HL60和HL60MX2，BALB / 3T3和4T1测试了选定的ITC的抗增殖活性。对这些化合物作为细胞周期停滞和凋亡诱导剂的作用机理进行了评估。（6-异硫氰基己基）（苯基）次膦酸乙酯（71）在4T1细胞系上进行了体内测试，并显示出适度的抗肿瘤活性，类似于异硫氰酸苄酯和环磷酰胺。
更新日期：2017-12-06
中文翻译：
抗增殖剂ω-（异硫氰酸根合）烷基次膦酸酯和氧化膦的设计，合成和评价
设计并合成了一系列21种新颖的，结构多样的ω-（异硫氰酸根合）烷基次膦酸酯和氧化膦（ITC），并以中等至良好的产率合成。使用LoVo和LoVo / DX癌细胞系评估了合成的化合物的体外抗增殖活性。合成的化合物的生物活性高于天然异硫氰酸酯，例如异硫氰酸苄酯或萝卜硫烷。还对选定的癌细胞系：A549，MESSA和MESSA / DX-5，HL60和HL60MX2，BALB / 3T3和4T1测试了选定的ITC的抗增殖活性。对这些化合物作为细胞周期停滞和凋亡诱导剂的作用机理进行了评估。（6-异硫氰基己基）（苯基）次膦酸乙酯（71）在4T1细胞系上进行了体内测试，并显示出适度的抗肿瘤活性，类似于异硫氰酸苄酯和环磷酰胺。
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