Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer was written by Chen, Linrong;Han, Liuquan;Mao, Shujun;Xu, Ping;Xu, Xinxin;Zhao, Ruibo;Wu, Zhihua;Zhong, Kai;Yu, Guangliang;Wang, Xiaolei. And the article was included in European Journal of Medicinal Chemistry in 2021.Formula: C16H22N2O4 This article mentions the following:
Herein the design, synthesis, and biol. evaluation of highly effective proteolysis targeting chimeras (PROTAC) androgen receptor (AR) degraders, such as compound I was reported. It could induce the degradation of AR protein in VCaP cell lines in a time-dependent manner, achieving the IC50 value of less than 0.25μM. The I was 5 times less toxic than EZLA and works with an appropriate half-life (t 1/2) or clearance rate (Cl). Also, it had a significant inhibitory effect on tumor growth in zebrafish transplanted with human prostate cancer (VCaP). Therefore, I provided a further idea of developing novel drugs for prostate cancer. In the experiment, the researchers used many compounds, for example, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4Formula: C16H22N2O4).
4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Formula: C16H22N2O4
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics