Pharmaceutical Organic Chemistry Department, Cairo University, Cairo, 11562, Egypt.
Arch Pharm Res. 2010 Jun;33(6):813-9. doi: 10.1007/s12272-010-0603-9. Epub 2010 Jul 6.
Several triazenoindazoles 3a-e and triazinopyrazolopyridines 6a-i were prepared through the reaction of the corresponding 3-amino-4-chloroindazole and 3-aminopyrazolopyridine diazonium salts 2 and 5 with a number of secondary amines. All compounds were evaluated for their in vitro cytotoxic activity on three cell lines, HepG2, MCF7, and HeLa. Most compounds inhibited cell growth with IC(50) less than 0.1 microM. Compound 6d was the most potent, with an IC(50) of 0.03 microM against HepG2 and 0.05 microM against MCF7 and HeLa cells.
通过将相应的 3-氨基-4-氯吲唑和 3-氨基吡唑并吡啶重氮盐 2 和 5 与多种仲胺反应，制备了几种三唑并吲唑 3a-e 和三嗪并吡唑吡啶 6a-i。所有化合物均在三种细胞系 HepG2、MCF7 和 HeLa 上评估了其体外细胞毒性活性。大多数化合物的 IC50 小于 0.1 μM，抑制细胞生长。化合物 6d 对 HepG2 的 IC50 为 0.03 μM，对 MCF7 和 HeLa 的 IC50 为 0.05 μM，活性最强。
