Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity

Longjun Ma; Yan Zhou; Dehua Yang; Ming Wei Wang; Wei Lu; Jiyu Jin

doi:10.3390/molecules27185867

Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity

Longjun Ma
, Yan Zhou
, Dehua Yang
, Ming Wei Wang^*
, Wei Lu^*
, Jiyu Jin^*

^*此作品的通讯作者

化学与分子工程学院

Lanzhou Jiaotong University
East China Normal University
CAS - Shanghai Institute of Materia Medica

科研成果: 期刊稿件 › 文章 › 同行评审

4 引用（Scopus）

摘要

Hydroxymethylthiohydantoin, hydroxymethylthiohydantoin, and hydantoin, containing a pyridine group, were synthesized to study their androgen receptor antagonistic activities. Among them, compounds 6a/6c/7g/19a/19b exhibited excellent androgen receptor antagonistic activity, which was consistent with or even superior to enzalutamide. In addition, compounds 19a and 19b exhibited better antiproliferative activity than enzalutamide in prostate cancer cells. The results show that compound 19a has great potential as a new AR antagonist.

源语言	英语
文章编号	5867
期刊	Molecules
卷	27
期	18
DOI	https://doi.org/10.3390/molecules27185867
出版状态	已出版 - 9月 2022

联合国可持续发展目标

此成果有助于实现下列可持续发展目标：

可持续发展目标 3 良好健康与福祉

访问文件

10.3390/molecules27185867

其它文件与链接

链接到 Scopus 的出版物

引用此

@article{700d249da0304079b0c7a7c4dad808dc,

title = "Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity",

abstract = "Hydroxymethylthiohydantoin, hydroxymethylthiohydantoin, and hydantoin, containing a pyridine group, were synthesized to study their androgen receptor antagonistic activities. Among them, compounds 6a/6c/7g/19a/19b exhibited excellent androgen receptor antagonistic activity, which was consistent with or even superior to enzalutamide. In addition, compounds 19a and 19b exhibited better antiproliferative activity than enzalutamide in prostate cancer cells. The results show that compound 19a has great potential as a new AR antagonist.",

keywords = "androgen receptor, antagonist, antiproliferative, enzalutamide, hydantoin analogs",

author = "Longjun Ma and Yan Zhou and Dehua Yang and Wang, \{Ming Wei\} and Wei Lu and Jiyu Jin",

note = "Publisher Copyright: {\textcopyright} 2022 by the authors.",

year = "2022",

month = sep,

doi = "10.3390/molecules27185867",

language = "英语",

volume = "27",

journal = "Molecules",

issn = "1420-3049",

publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",

number = "18",

}

TY - JOUR

T1 - Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity

AU - Ma, Longjun

AU - Zhou, Yan

AU - Yang, Dehua

AU - Wang, Ming Wei

AU - Lu, Wei

AU - Jin, Jiyu

PY - 2022/9

Y1 - 2022/9

N2 - Hydroxymethylthiohydantoin, hydroxymethylthiohydantoin, and hydantoin, containing a pyridine group, were synthesized to study their androgen receptor antagonistic activities. Among them, compounds 6a/6c/7g/19a/19b exhibited excellent androgen receptor antagonistic activity, which was consistent with or even superior to enzalutamide. In addition, compounds 19a and 19b exhibited better antiproliferative activity than enzalutamide in prostate cancer cells. The results show that compound 19a has great potential as a new AR antagonist.

AB - Hydroxymethylthiohydantoin, hydroxymethylthiohydantoin, and hydantoin, containing a pyridine group, were synthesized to study their androgen receptor antagonistic activities. Among them, compounds 6a/6c/7g/19a/19b exhibited excellent androgen receptor antagonistic activity, which was consistent with or even superior to enzalutamide. In addition, compounds 19a and 19b exhibited better antiproliferative activity than enzalutamide in prostate cancer cells. The results show that compound 19a has great potential as a new AR antagonist.

KW - androgen receptor

KW - antagonist

KW - antiproliferative

KW - enzalutamide

KW - hydantoin analogs

UR - https://www.scopus.com/pages/publications/85138409283

U2 - 10.3390/molecules27185867

DO - 10.3390/molecules27185867

M3 - 文章

C2 - 36144603

AN - SCOPUS:85138409283

SN - 1420-3049

VL - 27

JO - Molecules

JF - Molecules

IS - 18

M1 - 5867

ER -

Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity

摘要

联合国可持续发展目标

访问文件

其它文件与链接

指纹

引用此