Biomaterials Center, Korea Institute of Science and Technology, Cheongryang, Seoul, Republic of Korea.
Arch Pharm (Weinheim). 2011 Mar;344(3):197-204. doi: 10.1002/ardp.201000057. Epub 2010 Dec 27.
Synthesis of a new series of 1H-pyrazole-1-carboxamide derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with sorafenib. Among all of these derivatives, compound IIe which has N-methylpiperazinyl and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line.
本文描述了一系列新型 1H-吡唑-1-甲酰胺衍生物的合成。测试了它们对 A375 人黑色素瘤细胞系的抗增殖活性,并研究了取代基对二芳基吡唑骨架的影响。药理结果表明,与索拉非尼相比,大多数新合成的化合物对 A375 表现出中等活性。在所有这些衍生物中,具有 N-甲基哌嗪基和酚基部分的化合物 IIe 对 A375 人黑色素瘤细胞系表现出最强的抗增殖活性。