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Microwave‐Assisted One‐Pot Synthesis of New α‐Aminophosphonates Using ZnBr2‐SiO2 as a Catalyst under Solvent‐Free Conditions and Their Anticancer Activity
ChemistrySelect ( IF 1.9 ) Pub Date : 2018-09-11 , DOI: 10.1002/slct.201801965 Geetha Chukka 1 , Kesavulu M. Muppuru 2 , Venkanna Banothu 3 , Reddy S. Battu 4 , Uma Addepally 3 , Syam P. Gandavaram 5 , Naga R. Chamarthi 6 , Rao V. B. Mandava 1
ChemistrySelect ( IF 1.9 ) Pub Date : 2018-09-11 , DOI: 10.1002/slct.201801965 Geetha Chukka 1 , Kesavulu M. Muppuru 2 , Venkanna Banothu 3 , Reddy S. Battu 4 , Uma Addepally 3 , Syam P. Gandavaram 5 , Naga R. Chamarthi 6 , Rao V. B. Mandava 1
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Synthesis of a succession of new α‐aminophosphonates 4a‐j was achieved by the one‐pot three‐component Kabachnik‐Fields reaction by reacting equimolar quantities of 4‐morpholinoaniline (1), a variety of aromatic aldehydes 2a‐j and diethyl phosphite (3) using silica‐supported zinc bromide (ZnBr2‐SiO2) as a catalyst in solvent‐free conditions under microwave (MW) irradiation. Products 4a‐j were characterized by IR, 1H, 13C, 31P, NMR and mass spectral data. For these new set of compounds, two‐dimensional structures are drawn, three‐dimensional coordinates are generated and studied for their anti‐cancer activity against breast cancer. To support theoretical findings, experimental studies are performed using breast cancer cell lines. The results of these studies suggested that analogue, 4f has the maximum activity against breast cancer cells (MDA‐MB‐231). Since α‐aminophosphonates are less toxic compared to drugs currently available in the market, this new classes of drugs have very good potential for the treatment of Breast cancer.
中文翻译：
无溶剂条件下以ZnBr2-SiO2为催化剂的微波辅助一锅法合成新的α-氨基膦酸酯及其抗癌活性
新的连续的合成α -aminophosphonates图4a-j中被4-吗啉代苯胺（等摩尔量的反应通过一锅三组分Kabachnik-Fields反应实现1），各种芳族醛的2a-j中和亚磷酸二乙酯（3）在无溶剂条件下，在微波（MW）辐射下，使用二氧化硅负载的溴化锌（ZnBr 2 -SiO 2）作为催化剂。产品4a-j的特征在于IR，1 H，13 C，31P，NMR和质谱数据。对于这些新化合物，绘制了二维结构，生成了三维坐标，并研究了其对乳腺癌的抗癌活性。为了支持理论发现，使用乳腺癌细胞系进行了实验研究。这些研究结果表明，类似物4f对乳腺癌细胞（MDA-MB-231）具有最大的活性。由于与市场上现有的药物相比，α-氨基膦酸盐的毒性较小，因此这类新药具有治疗乳腺癌的巨大潜力。
更新日期：2018-09-11
中文翻译：
无溶剂条件下以ZnBr2-SiO2为催化剂的微波辅助一锅法合成新的α-氨基膦酸酯及其抗癌活性
新的连续的合成α -aminophosphonates图4a-j中被4-吗啉代苯胺（等摩尔量的反应通过一锅三组分Kabachnik-Fields反应实现1），各种芳族醛的2a-j中和亚磷酸二乙酯（3）在无溶剂条件下，在微波（MW）辐射下，使用二氧化硅负载的溴化锌（ZnBr 2 -SiO 2）作为催化剂。产品4a-j的特征在于IR，1 H，13 C，31P，NMR和质谱数据。对于这些新化合物，绘制了二维结构，生成了三维坐标，并研究了其对乳腺癌的抗癌活性。为了支持理论发现，使用乳腺癌细胞系进行了实验研究。这些研究结果表明，类似物4f对乳腺癌细胞（MDA-MB-231）具有最大的活性。由于与市场上现有的药物相比，α-氨基膦酸盐的毒性较小，因此这类新药具有治疗乳腺癌的巨大潜力。
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