Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi, India.
Bioorg Med Chem Lett. 2012 Aug 1;22(15):4934-8. doi: 10.1016/j.bmcl.2012.06.048. Epub 2012 Jun 21.
Structural modification of one of our earlier reported lead molecule (ABNM13) has been carried out to study the effect of different substituents at the N″-position of N-hydroxy-N'-amino guanidines (HAGs) on their anticancer activity. Compounds with electron donating substituents were found to be less active. In contrast, those with electron withdrawing groups were found favorable for anticancer activity. The obtained results provide significant SAR information that may be useful for further drug designing with HAGs.
对我们之前报道的先导分子(ABNM13)之一进行了结构修饰,以研究 N-羟基-N'-氨基胍(HAGs)的 N″-位不同取代基对其抗癌活性的影响。带有供电子取代基的化合物活性较低。相比之下,带有吸电子基团的化合物有利于抗癌活性。所得结果提供了有意义的 SAR 信息,这可能对使用 HAGs 进行进一步药物设计有用。