Kojima, Tomohiro; Ogawa, Takumi; Kitao, Souichiro; Sato, Manabu; Oda, Akifumi; Ohta, Kiminori; Endo, Yasuyuki published the artcile< Estrogenic activity of bis(4-hydroxyphenyl)methanes with cyclic hydrophobic structure>, Reference of 112-63-0, the main research area is preparation hydroxyphenylmethane estrogenic antitumor neoplasm; Carborane; Estrogen receptor; Partial agonist; SERM.
Monoalkylated bis(4-hydroxyphenyl)methanes are reported to show weak binding affinity for estrogen receptor (ER). The authors hypothesized that introduction of appropriately located hydrophobic substituents in these compounds would increase the binding affinity. Indeed, the authors found that bis(4-hydroxyphenyl)methane bearing a 3,3-dimethylcyclohexyl group I shows potent ERα binding affinity, comparable to that of estradiol. Bulkier substituents could be introduced at the 3,3-position without decreasing the affinity. However, the position of the substituents was critical: the 4,4-dimethylcyclohexyl derivative showed very weak binding affinity. The compounds with high ER-binding affinity showed predominantly agonistic activity, together with weak antagonistic activity at high concentration, in cell proliferation assay with human breast cancer cell line MCF-7. Further structure-function studies of these compounds and their derivatives might lead to the development of more selective and potent estrogen receptor modulators.
Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics