Medicinal Chemistry Research

, volume 33 , issue 11 , pages 2131-2149

Design, synthesis and biological evaluation of novel pyrimidine-phenylsulfonylfuroxan hybrids

Dongling Gu ^{1, 2}

Shihao Wang ^{1, 2}

Zichen Yang ^{1, 2}

Hongjing Chen ^{1, 2}

Jiahui Han ^{1, 2}

Chi Lingling ^{1, 2}

Fuqiang Yu ^{1, 2}

Hao Wang ^{1, 2}

Jiaxin Zheng, ^{1, 3}

Peirong Zhao ^{2, 3, 4}

Hongmin Liu ^{1, 2, 3, 4}

Yu Ke ^{1, 2, 3, 4}

Qiurong Zhang ^{1, 2, 3, 4}

Hide authors affiliations Show authors affiliations: 4 affiliations

School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, China |

Institute of Drug Discovery and Development, Zhengzhou, China |

Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou, China |

⁴

State Key Laboratory of Esophageal Cancer Prevention & Treatment, Zhengzhou, China |

Publication type: Journal Article

Publication date: 2024-10-15

Springer Nature

Medicinal Chemistry Research

scimago Q2

wos Q3

SJR: 0.470

CiteScore: 5.1

Impact factor: 3.1

ISSN: 10542523, 15548120

DOI: 10.1007/s00044-024-03315-y

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Abstract

In this study, a series of novel pyrimidine-phenylsulfonylfuroxan hybrids were designed, synthesized and evaluated for their biological activities. Most of the compounds demonstrated considerable antiproliferative activity against MDA-MB-231 and PC-3 cells. Among them, 21y (IC50 = 0.82 ± 0.08 μM) possessed excellent antiproliferative activity against PC-3 in vitro, significantly superior to the positive control drug 5-FU, which inhibited PC-3 colony formation and migration ability in a dose-dependent manner and blocked the cell cycle at the GO/G1 phase. Furthermore, 21y dramatically induced apoptosis of PC-3 cells via the mitochondrial pathway, the ROS pathway, and the regulation of apoptosis-related proteins. Notably, the high-level NO generated by 21y in PC-3 cells had a synergistic antitumor effect. With these results, compound 21y could act as an antitumor candidate with potential for further studies.

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Gu D. et al. Design, synthesis and biological evaluation of novel pyrimidine-phenylsulfonylfuroxan hybrids // Medicinal Chemistry Research. 2024. Vol. 33. No. 11. pp. 2131-2149.

GOST all authors (up to 50) Copy

Gu D., Wang S., Yang Z., Chen H., Han J., Lingling C., Yu F., Wang H., Zheng, J., Zhao P., Liu H., Ke Yu., Zhang Q. Design, synthesis and biological evaluation of novel pyrimidine-phenylsulfonylfuroxan hybrids // Medicinal Chemistry Research. 2024. Vol. 33. No. 11. pp. 2131-2149.

RIS |

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RIS Copy

TY - JOUR

DO - 10.1007/s00044-024-03315-y

UR - https://link.springer.com/10.1007/s00044-024-03315-y

TI - Design, synthesis and biological evaluation of novel pyrimidine-phenylsulfonylfuroxan hybrids

T2 - Medicinal Chemistry Research

AU - Gu, Dongling

AU - Wang, Shihao

AU - Yang, Zichen

AU - Chen, Hongjing

AU - Han, Jiahui

AU - Lingling, Chi

AU - Yu, Fuqiang

AU - Wang, Hao

AU - Zheng,, Jiaxin

AU - Zhao, Peirong

AU - Liu, Hongmin

AU - Ke, Yu

AU - Zhang, Qiurong

PY - 2024

DA - 2024/10/15

PB - Springer Nature

SP - 2131-2149

IS - 11

VL - 33

SN - 1054-2523

SN - 1554-8120

ER -

BibTex |

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BibTex (up to 50 authors) Copy

@article{2024_Gu,

author = {Dongling Gu and Shihao Wang and Zichen Yang and Hongjing Chen and Jiahui Han and Chi Lingling and Fuqiang Yu and Hao Wang and Jiaxin Zheng, and Peirong Zhao and Hongmin Liu and Yu Ke and Qiurong Zhang},

title = {Design, synthesis and biological evaluation of novel pyrimidine-phenylsulfonylfuroxan hybrids},

journal = {Medicinal Chemistry Research},

year = {2024},

volume = {33},

publisher = {Springer Nature},

month = {oct},

url = {https://link.springer.com/10.1007/s00044-024-03315-y},

number = {11},

pages = {2131--2149},

doi = {10.1007/s00044-024-03315-y}

}

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MLA Copy

Gu, Dongling, et al. “Design, synthesis and biological evaluation of novel pyrimidine-phenylsulfonylfuroxan hybrids.” Medicinal Chemistry Research, vol. 33, no. 11, Oct. 2024, pp. 2131-2149. https://link.springer.com/10.1007/s00044-024-03315-y.

Publisher

Springer Nature

Journal

Medicinal Chemistry Research

scimago Q2

wos Q3

SJR

0.470

CiteScore

5.1

Impact factor

3.1

ISSN

10542523 (Print)

15548120 (Electronic)