Structure-activity relationships of pyrazine-based CK2 inhibitors: Synthesis and evaluation of 2,6-disubstituted pyrazines and 4,6-disubstituted pyrimidines

被引：26

作者：

Suzuki, Yarnato ^{[1
]}

Cluzeau, Jerome ^{[1
]}

Hara, Takafumi ^{[1
]}

Hirasawa, Akira ^{[1
]}

Tsujimoto, Gozoh ^{[1
]}

Oishi, Shinya ^{[1
]}

Ohno, Hiroaki ^{[1
]}

Fujii, Nobutaka ^{[1
]}

机构：

[1] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan

来源：

ARCHIV DER PHARMAZIE | 2008年 / 341卷 / 09期

关键词：

CK2; glomerulonephritis; kinase inhibitor; pyrazine derivatives; SAR study;

D O I：

10.1002/ardp.200700269

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structually related to the known CK2 inhibitors, 2,6-disubstituted pyrazine and 4,6-disubstituted pyrimidine derivatives were synthesized and their inhibitory activities toward CK2 alpha and CK2 alpha' were evaluated. Structure-activity relationship study has revealed that several pyrazine derivatives bearing a (pyrrol-3-yl)acetic acid and a monosubstituted aniline possess potent inhibitory activities.

引用

页码：554 / 561

页数：8

共 50 条

[1] Discovery and structure-activity relationship of 2,6-disubstituted pyrazines, potent and selective inhibitors of protein kinase CK2
Fuchi, Nobuhiro
Iura, Yosuke
Kaneko, Hiroaki
Nitta, Aiko
Suyama, Kazuharu
Ueda, Hiroshi
Yamaguchi, Shinichi
Nishimura, Kazumi
Fujii, Shigeo
Sekiya, Yumiko
Yamada, Masateru
Takahashi, Toshiya
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2012, 22 (13) : 4358 - 4361
[2] Identification and structure-activity relationships of 2,6-disubstituted pyrazines as antituberculosis agents
Sun, Yongmao
Petukhova, Valentina
Giri, Rajan S.
Klein, Larry L.
Song, Yang
Zhang, Nan
Peng, Kuan Wei
Wan, Baojie
Wang, Yuehong
Franzblau, Scott G.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2010, 240
[3] Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases
Gingipalli, Lakshmaiah
Block, Michael H.
Bao, Larry
Cooke, Emma
Dakin, Les A.
Denz, Christopher R.
Ferguson, Andrew D.
Johannes, Jeffrey W.
Larsen, Nicholas A.
Lyne, Paul D.
Pontz, Timothy W.
Wang, Tao
Wu, Xiaoyun
Wu, Allan
Zhang, Hai-Jun
Zheng, Xiaolan
Dowling, James E.
Lamb, Michelle L.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2018, 28 (08) : 1336 - 1341
[4] SYNTHESIS OF 2,6-DISUBSTITUTED PYRAZINES AND RELATED DERIVATIVES
SHAREFKIN, DM
JOURNAL OF ORGANIC CHEMISTRY, 1959, 24 (03): : 345 - 348
[5] Structure-Activity Relationship of 4,6-Disubstituted Pyrimidines as EGFR and VEGFR-2 Tyrosine Kinase Inhibitors
Song, Jiho
Lee, Jung Wook
Chung, Shin Hyuck
Wenas, Michelle A.
Min, Kyung Hoon
BULLETIN OF THE KOREAN CHEMICAL SOCIETY, 2017, 38 (11): : 1255 - 1256
[6] Novel inhibitors of BRAF based on a 2,6-disubstituted pyrazine scaffold
Niculescu-Duvaz, I.
Roman, E.
Whittaker, S. R.
Friedlos, F.
Kirk, R.
Scanlon, I. J.
Davies, L. C.
Niculescu-Duvaz, D.
Marais, R.
Springer, C. J.
EJC SUPPLEMENTS, 2008, 6 (12): : 183 - 183
[7] Synthesis and Inhibitory Activity Evaluation of 2,6-Disubstituted Purine Derivatives
Liu, Hongxia
Li, Libo
Qurat-ul-ain, Shaikh
Jiang, Tao
JOURNAL OF HETEROCYCLIC CHEMISTRY, 2015, 52 (02) : 473 - 477
[8] 2,6-DISUBSTITUTED DECAHYDROPYRIDO[4,3-D] PYRIMIDINES
KRETZSCHMAR, E
DIETZ, G
PHARMAZIE, 1985, 40 (02): : 129 - 129
[9] Synthesis and structure-activity relationship of 2,6-disubstituted pyridine derivatives as inhibitors of β-amyloid-42 aggregation
Kroth, Heiko
Sreenivasachary, Nampally
Hamel, Anne
Benderitter, Pascal
Varisco, Yvan
Giriens, Valerie
Paganetti, Paolo
Froestl, Wolfgang
Pfeifer, Andrea
Muhs, Andreas
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 26 (14) : 3330 - 3335
[10] Synthesis, structure and reactivity of some 2,6-disubstituted dimethylsilylbenzenes
Beckmann, Jens
Hesse, Maxie
ZEITSCHRIFT FUR ANORGANISCHE UND ALLGEMEINE CHEMIE, 2007, 633 (08): : 1233 - 1238

← 1 2 3 4 5 →