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^*

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

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

Research output: Contribution to journal › Article › peer-review

4 Scopus citations

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.

Original language	English
Article number	5867
Journal	Molecules
Volume	27
Issue number	18
DOIs	https://doi.org/10.3390/molecules27185867
State	Published - Sep 2022

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

androgen receptor
antagonist
antiproliferative
enzalutamide
hydantoin analogs

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10.3390/molecules27185867

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@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

Abstract

UN SDGs

Keywords

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