Delving into the Latest Updates on ER-34617 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

RARα

Action

agonists

Mechanism

RARα agonists(Retinoic acid receptor alpha agonists)

Therapeutic Areas

NeoplasmsHemic and Lymphatic Diseases

Active Indication-

Inactive Indication

Leukemia

Originator Organization

Eisai Co., Ltd.

Active Organization-

Inactive Organization

Eisai Co., Ltd.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC23H25N3O2

InChIKeyRREMNJZTZUKGKQ-UHFFFAOYSA-N

CAS Registry187400-18-6

The effect of retinoic acid receptor agonists on allograft skin survival was investigated in mice.ER-34617 prolonged graft survival in a dose-dependent manner at 0.1 mg/kg per day.In mice immunized with spleen cells from other mice, ER-38925 inhibited the induction of alloantigen-specific cytotoxic T lymphocytes at 0.3 and 3 mg/kg.The effect at the lower dose was comparable to that of CsA at 10 mg/kg, i.p.

01 Feb 2000·Journal of medicinal chemistryQ1 · MEDICINE

Syntheses and Structure−Activity Relationships of 5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline Derivatives with Retinoic Acid Receptor α Agonistic Activity

Q1 · MEDICINE

Article

Author: Tokuhara, Naoki ; Kikuchi, Kouichi ; Nagai, Mitsuo ; Hibi, Shigeki ; Hida, Takayuki ; Tai, Kenji ; Yamauchi, Toshihiko ; Yoshimura, Hiroyuki

In the course of our studies on retinoic acid receptor (RAR) agonists, we have designed and synthesized a series of quinoxaline derivatives. One of them, 4-[5-(5,6,7,8-tetrahydro-5,5,8, 8-tetramethyl-2-quinoxalinyl)-1H-2-pyrrolyl]benzoic acid (3a), which possesses a 2,5-disubstituted pyrrole moiety, showed selectivity for the RARalpha receptor and exerted highly potent cell-differentiating activity on HL-60 cells.

100 Deals associated with ER-34617

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