Maximizing ER-α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927 was written by Kahraman, Mehmet;Govek, Steven P.;Nagasawa, Johnny Y.;Lai, Andiliy;Bonnefous, Celine;Douglas, Karensa;Sensintaffar, John;Liu, Nhin;Lee, KyoungJin;Aparicio, Anna;Kaufman, Josh;Qian, Jing;Shao, Gang;Prudente, Rene;Joseph, James D.;Darimont, Beatrice;Brigham, Daniel;Heyman, Richard;Rix, Peter J.;Hager, Jeffrey H.;Smith, Nicholas D.. And the article was included in ACS Medicinal Chemistry Letters in 2019.Application In Synthesis of 2-(3-Methoxyphenyl)acetyl chloride This article mentions the following:
The further optimization of ER-α degradation efficacy of a series of ER modulators by refining side-chain substitution led to efficacious selective estrogen receptor degraders (SERDs). A fluoromethyl azetidine group was found to be preferred and resulted in the identification of bis-phenol chromene 17ha. In a tamoxifen-resistant breast cancer xenograft model, 17ha (ER-α degradation efficacy = 97%) demonstrated tumor regression, together with robust reduction of intratumoral ER-α levels. However, despite superior oral exposure, 5a (ER-α degradation efficacy = 91%) had inferior activity. This result suggests that optimizing ER-α degradation efficacy leads to compounds with robust effects in a model of tamoxifen-resistant breast cancer. Compound 17ha (GDC-0927) was evaluated in clin. trials in women with metastatic estrogen receptor-pos. breast cancer. In the experiment, the researchers used many compounds, for example, 2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0Application In Synthesis of 2-(3-Methoxyphenyl)acetyl chloride).
2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Application In Synthesis of 2-(3-Methoxyphenyl)acetyl chloride
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics