Evaluation of the predictive power of calculation procedure for molecular hydrophobicity of some estradiol derivates

Characterization of lipophilicity and antiproliferative activity of E-2-arylmethylene-1-tetralones and their heteroanalogues

“…In full accordance with it, now the same effect could be obtained with thiochromanon: the k data of thiochromanon (22) was significantly higher than that of the tetralone ( Table 1). The compound with sulphinyl moiety (23) showed much decreased retention parameter as it was expected and incorporation of the sulphonyl derivative (24) was found to cause further decrease in k . Both effect can be explained the stronger polarisability of sulphonyl and sulphinyl group and was demonstrated earlier by our group in reference to aurones and oxidised thioaurones [49].…”

“…Group I (Table 1) is consisting of substituted arylmethylene-tetralones (1-10), heteroaryl-methylene-tetralones (11)(12)(13)(14)(15)(16)(17)(18) and the indanone (20) and benzosuberone (19) derivatives. Group II contains the chromanones and their analogues (21)(22)(23)(24)(25)(26).…”

“…Another possibility is to investigate the influence of lipophilicity on biological activity instead of fragment approach either atom-based (e.g. Crippen's, Viswanadhan's, Broto's method) [23] or molecular lipophilicity potential (MLP) developed by Testa and co-workers [24].…”

Design of Estradiol Loaded PLGA Nanoparticulate Formulations: A Potential Oral Delivery System for Hormone Therapy

“…Estrogens are endogenous substances with a variety of effects on the human body, including growth and maintenance of the female reproductive system and female sex characteristics (1). The primary source of estrogen in normally cycling adult women is the ovarian follicle (2).…”

Use of reversed-phase liquid chromatography for determining the lipophilicity of α-aryl-N-cyclopropylnitrones

“…Nowadays, reversed-phase liquid chromatography (RP-HPLC) is widely used as an alternative technique to the tedious, time-consuming and poorly reproducible shake flask method, since the determined retention parameters (e.g. log k w ) can be correlated with log P and other lipophilicity parameters of compounds [11,12].…”