Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors

被引：31

作者：

Chen, Fei ^{[1
]}

Chai, Hui ^{[1
]}

Su, Ming-Bo ^{[1
]}

Zhang, Yang-Ming ^{[1
]}

Li, Jia ^{[1
]}

Xie, Xin ^{[1
]}

Nan, Fa-Jun ^{[1
]}

机构：

[1] Shanghai Inst Mat Med, Chinese Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2014年 / 5卷 / 06期

基金：

中国国家自然科学基金;

关键词：

Histone deacetylase inhibitors; largazole; bisthiazole; CONCISE TOTAL-SYNTHESIS; HDAC INHIBITORS; BIOLOGICAL EVALUATION; LARGAZOLE ANALOGS; TRICHOSTATIN-A; DERIVATIVES; SAHA; INDUCTION; MECHANISM; APOPTOSIS;

D O I：

10.1021/ml400470s

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inspired by the thiazole thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be orally efficacious in ameliorating clinical symptoms of EAE mice.

引用

页码：628 / 633

页数：6

共 50 条

[21] Pyrimidine-Based Tricyclic Molecules as Potent and Orally Efficacious Inhibitors of Wee1 Kinase
Tong, Yunsong
Torrent, Maricel
Florjancic, Alan S.
Bromberg, Kenneth D.
Buchanan, Fritz G.
Ferguson, Debra C.
Johnson, Eric F.
Lasko, Loren M.
Maag, David
Merta, Philip J.
Olson, Amanda M.
Osterling, Donald J.
Soni, Nirupama
Shoemaker, Alexander R.
Penning, Thomas D.
ACS MEDICINAL CHEMISTRY LETTERS, 2015, 6 (01): : 58 - 62
[22] Potent and Selective Non-hydroxamate Histone Deacetylase 8 Inhibitors
Kleinschek, Alexander
Meyners, Christian
Digiorgio, Eros
Brancolini, Claudio
Meyer-Almes, Franz-Josef
CHEMMEDCHEM, 2016, 11 (23) : 2598 - 2606
[23] Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors
Wang, Fang
Lu, Wen
Zhang, Tao
Dong, Jinyun
Gao, Hongping
Li, Pengfei
Wang, Sicen
Zhang, Jie
BIOORGANIC & MEDICINAL CHEMISTRY, 2013, 21 (22) : 6973 - 6980
[24] Potent histone deacetylase inhibitors:: N-hydroxybenzamides with antitumor activities
Maeda, T
Nagaoka, Y
Kuwajima, H
Seno, C
Maruyama, S
Kurotaki, M
Uesato, S
BIOORGANIC & MEDICINAL CHEMISTRY, 2004, 12 (16) : 4351 - 4360
[25] Discovery of a series of hydroximic acid derivatives as potent histone deacetylase inhibitors
Zhang, Lei
Wang, Xuejian
Li, Xiaoguang
Zhang, Lihui
Xu, Wenfang
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2014, 29 (04) : 582 - 589
[26] Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors
Baud, Matthias G. J.
Leiser, Thomas
Petrucci, Vanessa
Gunaratnam, Mekala
Neidle, Stephen
Meyer-Almes, Franz-Josef
Fuchter, Matthew J.
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY, 2013, 9 : 81 - 88
[27] Histone deacetylase inhibitors
Miller, TA
Witter, DJ
Belvedere, S
JOURNAL OF MEDICINAL CHEMISTRY, 2003, 46 (24) : 5097 - 5116
[28] Histone deacetylase inhibitors
Sharma, S.
LUNG CANCER, 2006, 54 : S51 - S51
[29] Histone Deacetylase Inhibitors
Ramalingam, Suresh S.
JOURNAL OF THORACIC ONCOLOGY, 2011, 6 (11) : S1808 - S1809
[30] Histone deacetylase inhibitors
Grant, S
ANNALS OF ONCOLOGY, 2005, 16 : 29 - 29

← 1 2 3 4 5 →