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DOAJ Open Access 2021

Synthesis and Biological Evaluation of Spirocyclic Chromane Derivatives as a Potential Treatment of Prostate Cancer

Li Feng Shujia Yu Hai Wang Shengwei Yang Xue Li +4 lainnya
Lihat Sumber DOI

Abstrak

As a significant co-activator involved in cell cycle and cell growth, differentiation and development, p300/CBP has shown extraordinary potential target in cancer therapy. Herein we designed new compounds from the lead compound A-485 based on molecular dynamic simulations. A series of new spirocyclic chroman derivatives was prepared, characterized and proven to be a potential treatment of prostate cancer. The most potent compound <b>B16</b> inhibited the proliferation of enzalutamide-resistant 22Rv1 cells with an IC<sub>50</sub> value of 96 nM. Furthermore, compounds <b>B16</b>–<b>P2</b> displayed favorable overall pharmacokinetic profiles, and better tumor growth inhibition than A-485 in an in vivo xenograft model.

Topik & Kata Kunci

Organic chemistry

Penulis (9)

L

Li Feng

S

Shujia Yu

H

Hai Wang

S

Shengwei Yang

X

Xue Li

H

Hongjuan Dai

L

Liwen Zhao

C

Cheng Jiang

Y

Yazhou Wang

Format Sitasi

APA MLA BibTeX
Feng, L., Yu, S., Wang, H., Yang, S., Li, X., Dai, H. et al. (2021). Synthesis and Biological Evaluation of Spirocyclic Chromane Derivatives as a Potential Treatment of Prostate Cancer. https://doi.org/10.3390/molecules26113162

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Informasi Jurnal
Tahun Terbit
2021
Sumber Database
DOAJ
DOI
10.3390/molecules26113162
Akses
Open Access ✓