Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors

被引：9

作者：

Zhou, Yumei ^{[1
,2
,3
,4
]}

Cui, Huaqing ^{[3
,4
]}

Yu, Xiaoming ^{[3
,4
]}

Peng, Tao ^{[2
]}

Wang, Gang ^{[2
]}

Wen, Xiaoxue ^{[2
]}

Sun, Yunbo ^{[2
]}

Liu, Shuchen ^{[2
]}

Zhang, Shouguo ^{[2
]}

Hu, Liming ^{[1
]}

Wang, Lin ^{[1
,2
]}

机构：

[1] Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China

[2] Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China

[3] Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China

[4] Peking Union Med Coll, Beijing 100050, Peoples R China

来源：

MOLECULES | 2017年 / 22卷 / 08期

基金：

中国国家自然科学基金;

关键词：

benzofuran; sulfoxide; sulfone; selective SIRT2 inhibitor; PROTEIN DEACETYLASES; MOLECULAR DOCKING; IN-VITRO; 4-(2-HYDROXYARYL)-1,2,3-THIADIAZOLES; SUPPRESSOR; SIRTUINS;

D O I：

10.3390/molecules22081348

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of benzofuran derivatives were designed and synthesized, and their inhibitory activites were measured against the SIRT1-3. The enzymatic assay showed that all the compounds showed certain anti-SIRT2 activity and selective over SIRT1 and SIRT3 with IC50 (half maximal inhibitory concentration) values at the micromolar level. The preliminary structure-activity relationships were analyzed and the binding features of compound 7e (IC50 3.81 mu M) was predicted using the CDOCKER program. The results of this research could provide informative guidance for further optimizing benzofuran derivatives as potent SIRT2 inhibitors.

引用

页数：12

共 50 条

[41] Discovery of Novel Thiazole-Based SIRT2 Inhibitors as Anticancer Agents: Molecular Modeling, Chemical Synthesis and Biological Assays
Piacente, Francesco
Guccione, Giorgia
Scarano, Naomi
Lunaccio, Dario
Miro, Caterina
Abbotto, Elena
Salis, Annalisa
Tasso, Bruno
Dentice, Monica
Bruzzone, Santina
Cichero, Elena
Millo, Enrico
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2024, 25 (20)
[42] Recent advances in the development of histone deacylase SIRT2 inhibitors
Yang, Wenyu
Chen, Wei
Su, Huilin
Li, Rong
Song, Chen
Wang, Zhouyu
Yang, Lingling
RSC ADVANCES, 2020, 10 (61) : 37382 - 37390
[43] Discovery of Selective SIRT2 Inhibitors as Therapeutic Agents in B-Cell Lymphoma and Other Malignancies
Chowdhury, Sarwat
Sripathy, Smitha
Webster, Alyssa A.
Park, Angela
Lao, Uyen
Hsu, Joanne H.
Loe, Taylor
Bedalov, Antonio
Simon, Julian A.
MOLECULES, 2020, 25 (03):
[44] Novel small molecule SIRT2 inhibitors induce cell death in leukemic cell lines
Tomohiro Kozako
Paolo Mellini
Takeo Ohsugi
Akiyoshi Aikawa
Yu-ichiro Uchida
Shin-ichiro Honda
Takayoshi Suzuki
BMC Cancer, 18
[45] Novel benzofuran-based sulphonamides as selective carbonic anhydrases IX and XII inhibitors: synthesis and in vitro biological evaluation
Abdelrahman, Mohamed A.
Eldehna, Wagdy M.
Nocentini, Alessio
Ibrahim, Hany S.
Almahli, Hadia
Abdel-Aziz, Hatem A.
Abou-Seri, Sahar M.
Supuran, Claudiu T.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2020, 35 (01) : 298 - 305
[46] NOVEL 1,2,4-OXADIAZOLE DERIVATIVES AS SELECTIVE BUTYRYLCHOLINESTERASE INHIBITORS: DESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION
Nazari, Maryam
Rezaee, Elham
Hariri, Roshanak
Akbarzadeh, Tahmineh
Tabatabai, Sayyed Abbas
EXCLI JOURNAL, 2021, 20 : 907 - 921
[47] Novel Group of Imidazole Derivatives as Atypical Selective Cyclooxygenase-2 Inhibitors: Design, Synthesis and Biological Evaluation
Kiani, Azin
Rezaee, Elham
Tabatabai, Sayyed Abbas
IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH, 2018, 17 : 78 - 86
[48] Novel benzofuran derivatives: synthesis and antitumor activity
Othman, Dina I.
Abdelal, Ali M. M.
El-Sayed, Magda A.
El Bialy, Serry A. A.
HETEROCYCLIC COMMUNICATIONS, 2013, 19 (01) : 29 - 35
[49] Synthesis and cytotoxicity of novel benzofuran neolignan derivatives
Fan, Hua-Fang
Ren, Ying-Mei
Wu, Xiu-Ling
Wang, Qiu-An
JOURNAL OF CHEMICAL RESEARCH, 2010, (04) : 233 - 235
[50] Synthesis and antimicrobial evaluation of new benzofuran derivatives
Jiang, Xizhen
Liu, Wenlu
Zhang, Wei
Jiang, Faqin
Gao, Zhe
Zhuang, Hao
Fu, Lei
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2011, 46 (08) : 3526 - 3530

← 1 2 3 4 5 →