Structure-activity relationship of novel (benzoylaminophenoxy)phenol derivatives as anti-prostate cancer agents was written by Kazui, Yuko;Fujii, Shinya;Yamada, Ayumi;Ishigami-Yuasa, Mari;Kagechika, Hiroyuki;Tanatani, Aya. And the article was included in Bioorganic & Medicinal Chemistry in 2018.Application of 103-16-2 The following contents are mentioned in the article:
The androgen receptor (AR) is a ligand-inducible transcription factor belonging to the nuclear receptor superfamily, and is a target mol. for development of drugs to treat prostate cancer. However, AR antagonists in clin. use, such as flutamide (3a) and bicalutamide (4), encounter resistance after several years of hormone therapy, predominantly due to mutations of AR. Thus, although some new-generation AR antagonists have been developed, novel types of AR antagonists are still required to treat drug-resistant prostate cancer. We previously reported a novel (benzoylaminophenoxy)phenol derivative 10a, which is structurally distinct from conventional AR antagonists. Here, we systematically examined the structure-activity relationship of (benzoylaminophenoxy)phenol derivatives on the inhibitory activity on the prostate cancer cell proliferations. We found that the 4-[4-(benzoylamino)phenoxy]phenol backbone is important for anti-prostate cancer activity. Introduction of a small substituent at the 2 position of the central benzene ring (B ring) increases the activity. Among the synthesized compounds, 19a and 19b exhibited the most potent inhibitory activity toward dihydrotestosterone-induced proliferation of several androgen-dependent cell lines, SC-3 (wild-type AR), LNCaP (T877A AR), and 22Rv1 (H874Y AR), but interestingly also inhibited proliferation of AR-independent PC-3 cells. These compounds, which have a different pharmacophore from conventional AR antagonists, are promising drug candidates for the treatment of prostate cancer. This study involved multiple reactions and reactants, such as 4-Benzyloxyphenol (cas: 103-16-2Application of 103-16-2).
4-Benzyloxyphenol (cas: 103-16-2) belongs to ethers. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is γ-valerolactone.Application of 103-16-2
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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem