Voronov Ilya I, Martynenko Vyacheslav M, Chernyak Alexander V, Balzarini Jan, Schols Dominique, Troshin Pavel A
Institute for Problems of Chemical Physics of RAS, Semenov Prospect 1, Chernogolovka, 142432, Russia.
Rega Institute for Medical Research, Minderbroedersstraat 10, B-3000, Leuven, Belgium.
Chem Biodivers. 2018 Nov;15(11):e1800293. doi: 10.1002/cbdv.201800293. Epub 2018 Oct 29.
We have synthesized a series of water-soluble polycarboxylic derivatives of [60]fullerene with a gradually changed polarity by combining three to five polar (ionic) malonate addends with two to zero hydrophobic dichlorobenzene units and explored their antiviral activity. It has been shown that decreasing the number of the ionogenic carboxylic groups in the molecules enhanced their antiviral activity against HIV-1 and suppressed their action against HIV-2. The obtained results implied that the charged states and hydrophobicity of the water-soluble polycarboxylic fullerene derivatives affect significantly their biological properties.
我们通过将三到五个极性（离子型）丙二酸加成物与两到零个疏水性二氯苯单元相结合，合成了一系列极性逐渐变化的[60]富勒烯水溶性多羧酸衍生物，并研究了它们的抗病毒活性。结果表明，分子中离子ogenic羧基数量的减少增强了它们对HIV-1的抗病毒活性，并抑制了它们对HIV-2的作用。所得结果表明，水溶性多羧酸富勒烯衍生物的带电状态和疏水性对其生物学性质有显著影响。
