Design and Synthesis of (3-Phenylisoxazol-5-yl)methanimine Derivatives as Hepatitis B Virus Inhibitors.

Series of (3-phenylisoxazol-5-yl)methanimine derivatives were synthesized, and evaluated for anti-hepatitis B virus (HBV) activity in vitro. Half of them more effectively inhibited HBsAg than 3TC, and more favor to inhibit secretion of HBeAg than to HBsAg. Part of the compounds with significant inhibition on HBeAg were also effectively inhibit replication of HBV DNA.

Synthesis and bioactive evaluation of -((1-methyl-1-indol-3-yl)methyl)--(3,4,5-trimethoxyphenyl)acetamide derivatives as agents for inhibiting tubulin polymerization.

Based on the inhibitory effect of CA-4 analogues and indoles on tubulin polymerization, we designed and synthesized a series of -((1-methyl-1-indol-3-yl)methyl)-2-(1-pyrazol-1-yl or triazolyl)--(3,4,5-trimethoxyphenyl)acetamides. All the synthesized compounds were evaluated for their antiproliferative activities against HeLa, MCF-7 and HT-29 cancer cell lines, and some of the target compounds demonstrated effective activities towards the three tumour cell lines. Among them, compound 7d exhibited the most potent activities against HeLa (IC = 0.