Lead optimization represents the tedious process of fine-tuning lead compounds from biologically active hits to suitable drug candidates for clinical trials. By chemically modifying a hit structure, an improved compound can be obtained in terms activity, selectivity, and pharmacokinetic ADME (absorption, distribution, metabolism, excretion) properties. The carboxylic acid moiety is known crucia...

Estrogens are a broad class of compounds which exert many physiological effects. In addition to gonadal and peripheral endogenous estrogen production, humans can be exposed to exogenous estrogenic compounds (xenoestrogens) from medicinal, dietary and environmental sources. These compounds can exert effects similar to that of 17 -estradiol (E2) through estrogen receptor (ER)-mediated mechanisms,...

The identification of new bioactive compounds derived from medicinal plants with significant therapeutic properties has attracted considerable interest in recent years. Such is the case of the Tripterygium wilfordii (TW), an herb used in Chinese medicine. Clinical trials performed so far using its root extracts have shown impressive therapeutic properties but also revealed substantial gastroint...