Discovery of novel amino-pyrimidine inhibitors of the insulin-like growth factor 1 (IGF1R) and insulin receptor (INSR) kinases; parallel optimization of cell potency and hERG inhibition-Reference-Cited by-同舟云学术

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Discovery of novel amino-pyrimidine inhibitors of the insulin-like growth factor 1 (IGF1R) and insulin receptor (INSR) kinases; parallel optimization of cell potency and hERG inhibition

Published:2015 Issue:7 Volume:6 Page:1244-1251
ISSN:2040-2503
Container-title:MedChemComm
language:en
Short-container-title:Med. Chem. Commun.

Author:

Tye Heather¹²³,Guertler Ulrich⁴⁵,Hofmann Marco H.⁶⁷,Mayer Moriz⁶⁷,Pal Sandeep¹²³,Rast Georg⁴⁵,Sanderson Michael P.⁶⁷,Schaaf Otmar⁶⁷,Treu Matthias⁶⁷,Zahn Stephan K.⁶⁷

Affiliation:

1. Evotec (UK) Ltd

2. Abingdon

3. UK

4. Boehringer Ingelheim Pharma GmbH & Co. KG

5. Germany

6. Boehringer Ingelheim RCV GmbH & Co KG

7. Austria

Abstract

Modulating hERG activity of IGF1R/INSR inhibitors by tuning log D and use of homology modelling.

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2015/MD/C5MD00097A

Reference16 articles.

1. The insulin-like growth factor-I receptor as a target for cancer therapy

2. The IGF-1 receptor in cancer biology

3. AMG 479, a fully human anti–insulin-like growth factor receptor type I monoclonal antibody, inhibits the growth and survival of pancreatic carcinoma cells

4. Pharmacodynamic and Antineoplastic Activity of BI 836845, a Fully Human IGF Ligand-Neutralizing Antibody, and Mechanistic Rationale for Combination with Rapamycin

5. BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR

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1. Matched Molecular Pair Analysis;Comprehensive Medicinal Chemistry III;2017

2. A comprehensive pharmacokinetic/pharmacodynamics analysis of the novel IGF1R/INSR inhibitor BI 893923 applying in vitro, in vivo and in silico modeling techniques;Cancer Chemotherapy and Pharmacology;2016-05-09

3. BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis;Molecular Cancer Therapeutics;2015-10-05

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