Design and Synthesis of Potent Ridaifen Analogues: Evaluation as Anticancer, 20S Proteasomal Inhibitors, and Antiebola Virus Agents through In vitro and In Silico Studies.

Ridaifen (RID) analogues are identified as nonpeptide, noncovalent inhibitors of the catalytic subunits of the human 20S proteasome. They demonstrated effectiveness against both multiple myeloma and solid tumors. Herein, the synthesis and biological evaluation of 20 novel RID analogs that exhibit inhibitory effects on the three catalytic subunits of the 20S proteasome are reported.

Manipulating Estrogenic/Anti-Estrogenic Activity of Triphenylethylenes towards Development of Novel Anti-Neoplastic SERMs.

Selective estrogen receptor modulators (SERMs) act as estrogen receptor (ERα) agonists or antagonists depending on the target issue. Tamoxifen (TAM) (a non-steroidal triphenylethylene derivative) was the first SERM approved as anti-estrogen for the treatment of metastatic breast cancer. On the hunt for novel SERMs with potential growth inhibitory activity on breast cancer cell lines yet no potential to induce endometrial carcinoma, we designed and synthesized 28 novel TAM analogs.