Array synthesis of progesterone receptor antagonists: 3-Aryl-1,2-diazepines

被引：14

作者：

Wiethe, Robert W. ^{[1
]}

Stewart, Eugene L. ^{[1
]}

Drewry, David H. ^{[1
]}

Gray, David W. ^{[1
]}

Mehbob, Abdul ^{[1
]}

Hoekstra, William J. ^{[1
]}

机构：

[1] GlaxoSmithKline Inc, Discovery Res, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 14期

关键词：

progesterone receptor; diazepine;

D O I：

10.1016/j.bmcl.2006.04.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New non-steroidal chemotypes are required for the development of drugs targeting the steroid hormone receptors. The parallel array synthesis of 3-aryl-1,2-diazepines employing solid-supported reagents is described. The resulting compounds demonstrated high affinity binding to the progesterone receptor. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：3777 / 3779

页数：3

共 50 条

[21] SYNTHESIS OF 2-SUBSTITUTED 3,4-DIHYDRO-1,2-DIAZEPINES BY THE REACTIONS OF UNSATURATED-KETONES WITH HYDRAZIDES
ANDERSON, PN
ARGO, CB
SHARP, JT
JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1981, (11): : 2761 - 2763
[22] Novel 3-Aryl Indoles as Progesterone Receptor Antagonists for Uterine Fibroids
Richardson, Timothy I.
Clarke, Christian A.
Yu, Kuo-Long
Yee, Ying K.
Bleisch, Thomas J.
Lopez, Jose E.
Jones, Scott A.
Hughes, Norman E.
Muehl, Brian S.
Lugar, Charles W.
Moore, Terry L.
Shetler, Pamela K.
Zink, Richard W.
Osborne, John J.
Montrose-Rafizadeh, Chahrzad
Patel, Nita
Geiser, Andrew G.
Galvin, Rachelle J. Sells
Dodge, Jeffrey A.
ACS MEDICINAL CHEMISTRY LETTERS, 2011, 2 (02): : 148 - 153
[23] A GENERAL-ROUTE TO 3-(HYDROXYARYL)TETRAHYDRO PYRIDAZINES AND 1,2-DIAZEPINES AND DERIVATIVES
KALYANAM, N
DAVE, KG
LIKHATE, MA
SYNTHETIC COMMUNICATIONS, 1988, 18 (16-17) : 2183 - 2191
[24] PI-COMPLEXES OF 1H-1,2-DIAZEPINES - SYNTHESIS AND CHARACTERIZATION OF TRICARBONYLIRON AND -RUTHENIUM DERIVATIVES
CARTY, AJ
KAN, G
MADDEN, DP
SNIECKUS, V
STANTON, M
BIRCHALL, T
JOURNAL OF ORGANOMETALLIC CHEMISTRY, 1971, 32 (02) : 241 - &
[25] REACTIONS OF METHYL AROYLDITHIOACETATES WITH SALTS OF 3-ARYL-1,2-DITHIOLYLIUM
CLESSE, F
QUINIOU, H
COMPTES RENDUS HEBDOMADAIRES DES SEANCES DE L ACADEMIE DES SCIENCES SERIE C, 1969, 268 (07): : 637 - &
[26] Synthesis and characterization of 3-aryl-1,3,2-benzoxazaboroles
Gross, Dustin
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2018, 256
[27] SYNTHESIS OF 3-ARYL-1,2-DICARBA-CLOSO-DODECABORANES BY SUZUKI-MIYAURA COUPLING REACTION
Aizawa, Koei
Ohta, Kiminori
Endo, Yasuyuki
HETEROCYCLES, 2010, 80 (01) : 369 - 377
[28] STUDIES ON DIAZEPINES .17. SYNTHESIS OF MONOCYCLIC 1,3-DIAZEPINES .2. SUBSTITUENT EFFECTS ON THE THERMAL RING-CONVERSION OF 1,2-DIAZEPINES INTO 1,3-DIAZEPINES
KURITA, J
KOJIMA, H
ENKAKU, M
TSUCHIYA, T
CHEMICAL & PHARMACEUTICAL BULLETIN, 1981, 29 (12) : 3696 - 3705
[29] PHOTOCHEMICAL SYNTHESIS OF 1,2-DIAZEPINES .7. REGIOSPECIFICITY OF PHOTOINDUCED ELECTROCYCLIZATION OF N-AMINOPYRIDIUM YLIDES
NASTASI, M
STREITH, J
BULLETIN DE LA SOCIETE CHIMIQUE DE FRANCE, 1973, (02): : 630 - 634
[30] STUDIES ON DIAZEPINES .16. SYNTHESIS OF MONOCYCLIC 1,3-DIAZEPINES .1. THERMOLYSIS OF 1,2-DIAZEPINES FORMED FROM METHYLPYRIDINE N-IMIDES
KURITA, J
KOJIMA, H
TSUCHIYA, T
CHEMICAL & PHARMACEUTICAL BULLETIN, 1981, 29 (12) : 3688 - 3695

← 1 2 3 4 5 →