Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors (Q27684210)

8

0 references

author name string

Victor S Gehling

1

0 references

Michael C Hewitt

2

0 references

Rishi G Vaswani

3

0 references

Yves Leblanc

4

0 references

Alexandre Côté

5

0 references

Christopher G Nasveschuk

6

0 references

Alexander M Taylor

7

0 references

James E Audia

9

0 references

Eneida Pardo

10

0 references

Shivangi Joshi

11

0 references

Peter Sandy

12

0 references

Jennifer A Mertz

13

0 references

Robert J Sims

14

0 references

Louise Bergeron

15

0 references

Barbara M Bryant

16

0 references

Steve Bellon

17

0 references

Florence Poy

18

0 references

Hariharan Jayaram

19

0 references

Ravichandran Sankaranarayanan

20

0 references

Sreegouri Yellapantula

21

0 references

Nandana Bangalore Srinivasamurthy

22

0 references

Swarnakumari Birudukota

23

0 references

Brian K Albrecht

ACS Medicinal Chemistry Letters

24

0 references

language of work or name

1 reference

12 September 2013

0 references

published in

1 reference

Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain

Crossref

volume

4

0 references

issue

9

0 references

page(s)

835-40

0 references

cites work

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A)

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Discovery and characterization of small molecule inhibitors of the BET family bromodomains

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Suppression of inflammation by a synthetic histone mimic

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Selective inhibition of BET bromodomains

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

BET bromodomain inhibition as a therapeutic strategy to target c-Myc

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

The double bromodomain-containing chromatin adaptor Brd4 and transcriptional regulation

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Targeting MYC dependence in cancer by inhibiting BET bromodomains

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Ligand efficiency indices for effective drug discovery

7 April 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

Ligand efficiency and fragment-based drug discovery

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

The Myc oncoprotein as a therapeutic target for human cancer

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

N-tert-Butanesulfinyl Imines: Versatile Intermediates for the Asymmetric Synthesis of Amines

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

An analysis of the binding efficiencies of drugs and their leads in successful drug discovery programs

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027525

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

27 November 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/24900758