Design, synthesis and evaluation of belinostat analogs as histone deacetylase inhibitors

被引：4

作者：

Zhang, Jie-Huan ^{[1
]}

Mottamal, Madhusoodanan ^{[3
,4
]}

Jin, Hai-Shan ^{[1
]}

Guo, Shanchun ^{[3
,4
]}

Gu, Yan ^{[1
]}

Wang, Guangdi ^{[3
,4
]}

Zhao, Li-Ming ^{[1
,2
]}

机构：

[1] Jiangsu Normal Univ, Sch Chem & Mat Sci, Xuzhou 221116, Jiangsu, Peoples R China

[2] Guangxi Normal Univ, State Key Lab Chem & Mol Engn Med Resources, Guilin 541004, Guangxi, Peoples R China

[3] Xavier Univ Louisiana, RCMI Canc Res Ctr, New Orleans, LA 70125 USA

[4] Xavier Univ Louisiana, Dept Chem, New Orleans, LA 70125 USA

来源：

FUTURE MEDICINAL CHEMISTRY | 2019年 / 11卷 / 21期

关键词：

anticancer activities; drug design; molecular docking; structure-activity relationship; synthesis; HYDROXAMIC ACID; BIOLOGICAL EVALUATION; DERIVATIVES;

D O I：

10.4155/fmc-2018-0587

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aim: Histone deacetylase (HDAC) is an attractive target for antitumor therapy. Therefore, the development of novel HDAC inhibitors is warranted. Materials & methods: A series of HDAC inhibitors based on N-hydroxycinnamamide fragment was designed as the clinically used belinostat analog using amide as the connecting unit. All target compounds were evaluated for their in vitro HDAC inhibitory activities and some selected compounds were tested for their antiproliferative activities. Conclusion: Among them, compound 7e showed an IC50 value of 11.5 nM in inhibiting the HDAC in a pan-HDAC assay, being the most active compound of the series.

引用

页码：2765 / 2778

页数：14

共 50 条

[31] Novel amide derivatives as inhibitors of histone deacetylase: Design, synthesis and SAR
Andrianov, Victor
Gailite, Vija
Lola, Daina
Loza, Einars
Semenikhina, Valentina
Kalvinsh, Ivars
Finn, Paul
Petersen, Kamille Dumong
Ritchie, James W. A.
Khan, Nagma
Tumber, Anthony
Collins, Laura S.
Vadlamudi, Sree M.
Bjorkling, Fredrik
Sehested, Maxwell
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (03) : 1067 - 1085
[32] Design and Synthesis of Orally Bioavailable Aminopyrrolidinone Histone Deacetylase 6 Inhibitors
Lin, Xianfeng
Chen, Wenming
Qiu, Zongxing
Guo, Lei
Zhu, Wei
Li, Wentao
Wang, Zhanguo
Zhang, Weixing
Zhang, Zhenshan
Rong, Yiping
Zhang, Meifang
Yu, Lingjie
Zhong, Sheng
Zhao, Rong
Wu, Xihan
Wong, Jason C.
Tang, Guozhi
JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (06) : 2809 - 2820
[33] MEDI 148-Synthesis and evaluation of cyclopeptide inhibitors of histone deacetylase
Marson, Charles M.
Sengmany, Stephane
Middleton, Brian
Dines, Jonathan
Thomas, N. Shaun B.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2006, 232
[34] Synthesis and biological evaluation of cyclic tetrapeptides serving as histone deacetylase inhibitors
Singh, Erinprit K.
Lapera, Stephanie
Nazarova, Lidia
Vasko, Robert C.
McAlpine, Shelli R.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2009, 238
[35] Synthesis and pharmacological evaluation of histone deacetylase inhibitors as fetal hemoglobin inducers
Dos Santos, Jean
Melchior, Aylime
Bosquesi, Priscila
Pavan, Aline
Lanaro, Carolina
Chung, ManChin
Rusinova, Radda
Chelucci, Rafael
Andersen, Olaf
Costa, Fernando
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2018, 255
[36] SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors
Desai, Dhimant
Salli, Ugur
Vrana, Kent E.
Amin, Shantu
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (06) : 2044 - 2047
[37] Design, Synthesis, and Biological Evaluation of New Urushiol Derivatives as Potent Class I Histone Deacetylase Inhibitors
Zhou, Hao
Qi, Zhiwen
Liu, Danyang
Xue, Xingyin
Wang, Chengzhang
CHEMBIOCHEM, 2023,
[38] Design, synthesis, docking studies and biological evaluation of novel chalcone derivatives as potential histone deacetylase inhibitors
Mohamed, Mamdouh F. A.
Shaykoon, Montaser Sh. A.
Abdelrahman, Mostafa H.
Elsadek, Bakheet E. M.
Aboraia, Ahmed S.
Abuo-Rahma, Gamal El-Din A. A.
BIOORGANIC CHEMISTRY, 2017, 72 : 32 - 41
[39] Design, synthesis, and biological evaluation of N-hydroxycinnamamide/salicylic acid hybrids as histone deacetylase inhibitors
You, Tao
Chen, Ke
Wang, Fei-Hai
Li, Pi-Hong
Li, Li-Yi
Wu, Zhi-Hao
Ni, Kong-Hai
Zheng, Zhi-Qiang
CHINESE CHEMICAL LETTERS, 2014, 25 (03) : 474 - 478
[40] Total synthesis of azumamide A and azumamide E, evaluation as histone deacetylase inhibitors, and design of a more potent analogue
Wen, Shijun
Carey, Krystle L.
Nakao, Yoichi
Fusetani, Nobuhiro
Packham, Graham
Ganesan, A.
ORGANIC LETTERS, 2007, 9 (06) : 1105 - 1108

← 1 2 3 4 5 →