Singh Palwinder, Paul Kamaldeep
Department of Chemistry, Guru Nanak Dev University, Amritsar-143005, India.
Bioorg Med Chem. 2006 Dec 15;14(24):8622-5. doi: 10.1016/j.bmc.2006.08.025. Epub 2006 Sep 1.
All the nine 1,3-dialkylated-pyrimidin-2,4-diones investigated are active against all the 59 human tumor cell lines. Compounds 2, 3, 4, and 6 show significant anti-cancer activities at some specific cell lines while compounds 7 and 9 exhibit anti-cancer activities against more number of cell lines. The structure-activity relationship studies indicate that the presence of piperidine/pyrrolidine at the end of C-6 chain, benzoyl group at C-5, and benzyl groups at N-1, N-3 of the pyrimidine ring increases the anti-cancer activities of these molecules.
所研究的所有九种1,3 - 二烷基化嘧啶 - 2,4 - 二酮对全部59种人类肿瘤细胞系均有活性。化合物2、3、4和6在某些特定细胞系中显示出显著的抗癌活性，而化合物7和9对更多数量的细胞系表现出抗癌活性。构效关系研究表明，嘧啶环C - 6链末端存在哌啶/吡咯烷、C - 5位有苯甲酰基以及N - 1、N - 3位有苄基会增加这些分子的抗癌活性。
