Selective estrogen receptor downregulators (SERDs) are a novel class of compounds
capable of reducing the ERα protein level and blocking ER activity. Therefore, SERDs are …

Resistance to endocrine therapy in breast carcinogenesis due to the redox regulation of the
signal transduction system by reactive oxygen species (ROS) is the subject of this review …

Resistance to the selective estrogen receptor modulator tamoxifen and to aromatase
inhibitors that lower circulating estradiol occurs in up to 50% of patients, generally leading to …

Almost 70% of breast cancers are estrogen receptor α (ERα) positive. Tamoxifen, a selective
estrogen receptor modulator (SERM), represents the standard of care for many patients; …

The clinical steroidal selective estrogen receptor (ER) degrader (SERD), fulvestrant, is
effective in metastatic breast cancer, but limited by poor pharmacokinetics, prompting the …

The clinical benzothiophene SERM (BT-SERM) raloxifene was compared with estrogens in
protection of primary rat neurons against oxygen-glucose deprivation (OGD). Structure …

Endocrine therapy (ET) is a well-validated strategy for estrogen receptor α positive (ERα+)
breast cancer therapy. Despite the clinical success of current standard of care (SoC) …

Parallel solution-phase methods for the synthesis of a 72-membered benzo [b] thiophene
library are reported. Medicinally interesting, drug-like, methyl sulfone-substituted benzo [b] …

Endocrine-resistant breast cancer is a major clinical obstacle. The use of 17β-estradiol (E2)
has reemerged as a potential treatment option following exhaustive use of tamoxifen or …

A major challenge in cancer research is to discover drugs with high selectivity and minor
side-effects. Tamoxifen has been widely used for more than 30 years in breast cancer …