Shivarama Holla B, Veerendra B, Shivananda M K, Poojary Boja
Department of P.G. Studies and Research in Chemistry, Mangalore University, Mangalagangotri, 574199, India.
Eur J Med Chem. 2003 Jul-Aug;38(7-8):759-67. doi: 10.1016/s0223-5234(03)00128-4.
A series of 3-substituted 4-[5-(4-methoxy-2-nitrophenyl)-2-furfurylidene] amino-5-mercapto-1,2,4-triazoles (3) were synthesized. Aminomethylation of compounds 3 with formaldehyde and various secondary amines furnished Mannich bases 4 and 5. These compounds were characterized on the basis of IR, 1H-NMR, mass spectral data and elemental analysis. The newly synthesized compounds were screened for their anticancer activity against a panel of 60 cell lines derived from seven cancer types namely, lung, colon, melanoma, renal, ovarian, CNS and leukemia. Some of the compounds were slightly more potent.
合成了一系列3-取代的4-[5-(4-甲氧基-2-硝基苯基)-2-糠叉基]氨基-5-巯基-1,2,4-三唑(3)。化合物3与甲醛和各种仲胺进行氨甲基化反应得到曼尼希碱4和5。这些化合物通过红外光谱、1H-核磁共振、质谱数据和元素分析进行表征。对新合成的化合物针对一组来自七种癌症类型（即肺癌、结肠癌、黑色素瘤、肾癌、卵巢癌、中枢神经系统癌和白血病）的60种细胞系进行了抗癌活性筛选。其中一些化合物的活性略强。
