2. Academic Validation
  3. Design, synthesis, and biological evaluation of 2-(naphthalen-1-yloxy)-N-phenylacetamide derivatives as TRPM4 inhibitors for the treatment of prostate cancer

Design, synthesis, and biological evaluation of 2-(naphthalen-1-yloxy)-N-phenylacetamide derivatives as TRPM4 inhibitors for the treatment of prostate cancer

  • Bioorg Med Chem. 2024 Jan 15:98:117584. doi: 10.1016/j.bmc.2023.117584.
Le Niu 1,  Huina Liu 2,  Xiaomei Li 2,  Lin Wang 3,  Hui Hua 2,  Qiaofeng Cao 3,  Qiuping Xiang 2,  Ting Cai 4,  Dongsheng Zhu 5
Affiliations

Affiliations

  • 1 Guoke Ningbo Life Science and Health Industry Research Institute, Ningbo No.2 Hospital, Ningbo, 315010, China; Department of Urology, the Second Affiliated Hospital of Nanjing Medical University, and Department of Medicinal Chemistry, School of Pharmacy, Nanjing Medical University, Nanjing, 211166, China.
  • 2 Guoke Ningbo Life Science and Health Industry Research Institute, Ningbo No.2 Hospital, Ningbo, 315010, China.
  • 3 Department of Urology, the Second Affiliated Hospital of Nanjing Medical University, and Department of Medicinal Chemistry, School of Pharmacy, Nanjing Medical University, Nanjing, 211166, China.
  • 4 Guoke Ningbo Life Science and Health Industry Research Institute, Ningbo No.2 Hospital, Ningbo, 315010, China. Electronic address: tingcai@ucas.ac.cn.
  • 5 Department of Urology, the Second Affiliated Hospital of Nanjing Medical University, and Department of Medicinal Chemistry, School of Pharmacy, Nanjing Medical University, Nanjing, 211166, China. Electronic address: zhuds@njmu.edu.cn.
PMID: 38168629 DOI: 10.1016/j.bmc.2023.117584
Abstract

Transient receptor potential melastatin 4 (TRPM4) is considered to be a potential target for Cancer and Other human diseases. Herein, a series of 2-(naphthalen-1-yloxy)-N-phenylacetamide derivatives were designed and synthesized as new TRPM4 inhibitors, aiming to improve cellular potency. One of the most promising compounds, 7d (ZX08903), displayed promising antiproliferative activity against prostate Cancer cell lines. 7d also suppressed colony formation and the expression of Androgen Receptor (AR) protein in prostate Cancer cells. Furthermore, 7d can concentration-dependently induce cell Apoptosis in prostate Cancer cells. Collectively, these findings indicated that compound 7d may serve as a promising lead compound for further Anticancer drug development.

Keywords

Cellular potency; Drug design; Prostate cancer; TRPM4.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z