Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and IGF-1R

Cornelius HempelDepartment of Pharmaceutical Chemistry, Institute of Pharmacy, Martin Luther University, Halle, Germany;

Frank TotzkeProQinase GmbH, Freiburg, Germany;

Christoph SchächteleProQinase GmbH, Freiburg, Germany;

Abdulkarim NajjarDepartment of Pharmaceutical Chemistry, Institute of Pharmacy, Martin Luther University, Halle, Germany;

Wolfgang SipplDepartment of Pharmaceutical Chemistry, Institute of Pharmacy, Martin Luther University, Halle, Germany;

Christoph RitterDepartment of Clinical Pharmacy, Institute of Pharmacy, Ernst Moritz Arndt University Greifswald, Germany

Andreas HilgerothDepartment of Pharmaceutical Chemistry, Institute of Pharmacy, Martin Luther University, Halle, Germany; Correspondence[email protected]

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Figures & data

Figure 1. Structure of quinazolines A, thienopyrimidines B and benzopyrrolopyridines C as EGFR inhibitors.

Figure 2. Quinazoline compound erlotinib binding to the hinge region of EGFR with hydrogen bonds.

Scheme 1. Formation of 6-bromo-substituted compounds

Scheme 2. Formation of 6-cyano and 6-carboxy-substituted compounds

Table 1. Protein kinase inhibitory activity as determined K_i values of our target compounds 5a–h, 6a–c and 7 for the tyrosine receptor kinases EGFR and IGF-1R.

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Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and IGF-1R

Table 1. Protein kinase inhibitory activity as determined K_i values of our target compounds 5a–h, 6a–c and 7 for the tyrosine receptor kinases EGFR and IGF-1R.

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Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and IGF-1R

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Table 1. Protein kinase inhibitory activity as determined Ki values of our target compounds 5a–h, 6a–c and 7 for the tyrosine receptor kinases EGFR and IGF-1R.

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Table 1. Protein kinase inhibitory activity as determined K_i values of our target compounds 5a–h, 6a–c and 7 for the tyrosine receptor kinases EGFR and IGF-1R.