Delving into the Latest Updates on DMU2139 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CYP1B1

Mechanism

CYP1B1 inhibitors(cytochrome P450 family 1 subfamily B member 1 inhibitors)

Therapeutic Areas

NeoplasmsCardiovascular DiseasesEndocrinology and Metabolic Disease+ [1]

Active Indication-

Inactive Indication

GlaucomaIschemiaNeoplasms+ [1]

Originator Organization

De Montfort University

Active Organization-

Inactive Organization

Indian Institute of Integrative Medicine

CYP Design Ltd.

De Montfort University

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC19H15NO2

InChIKeyMPDPEUALCUWORP-RUDMXATFSA-N

CAS Registry1821143-80-9

The structure of alpha-napthoflavone (ANF), a potent inhibitor of CYP1A1 and CYP1B1, mimics the structure of chalcones. Two potent CYP1B1 inhibitors 7k (DMU2105) and 6j (DMU2139) have been identified from two series of synthetic pyridylchalcones. They inhibit human CYP1B1 enzyme bound to yeast-derived microsomes (Sacchrosomes™) with IC₅₀ values of 10 and 9 nM, respectively, and show a very high level of selectivity towards CYP1B1 with respect to the IC₅₀ values obtained with CYP1A1, CYP1A2, CYP3A4, CYP2D6, CYP2C9 and CYP2C19 Sacchrosomes™. Both compounds also potently inhibit CYP1B1 expressed within 'live' recombinant yeast and human HEK293 kidney cells with IC₅₀ values of 63, 65, and 4, 4 nM, respectively. Furthermore, the synthesized pyridylchalcones possess better solubility and lipophilicity values than ANF. Both compounds overcome cisplatin-resistance in HEK293 and A2780 cells which results from CYP1B1 overexpression. These potent cell-permeable and water-soluble CYP1B1 inhibitors are likely to have useful roles in the treatment of cancer, glaucoma, ischemia and obesity.

100 Deals associated with DMU2139

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Glaucoma	Preclinical	GB	Indian Institute of Integrative Medicine	31 May 2017
Ischemia	Preclinical	GB	De Montfort University	31 May 2017
Ischemia	Preclinical	GB	Indian Institute of Integrative Medicine	31 May 2017
Ischemia	Preclinical	GB	CYP Design Ltd.	31 May 2017
Neoplasms	Preclinical	GB	CYP Design Ltd.	31 May 2017
Neoplasms	Preclinical	GB	De Montfort University	31 May 2017
Neoplasms	Preclinical	GB	Indian Institute of Integrative Medicine	31 May 2017
Obesity	Preclinical	GB	Indian Institute of Integrative Medicine	31 May 2017
Obesity	Preclinical	GB	De Montfort University	31 May 2017
Obesity	Preclinical	GB	CYP Design Ltd.	31 May 2017