Design, synthesis, and antiproliferative activity of new indole/1,2,4‐triazole/chalcone hybrids as EGFR and/or c‐MET inhibitors

Author:

Mahmoud Esraa1,Abdelhamid Dalia23ORCID,Youssif Bahaa G. M.4,Gomaa Hesham A. M.5ORCID,Hayallah Alaa M.46,Abdel‐Aziz Mohamad2ORCID

Affiliation:

1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy Deraya University Minia Egypt

2. Department of Medicinal Chemistry, Faculty of Pharmacy Minia University Minia Egypt

3. Raabe College of Pharmacy Ohio Northern University Ohio USA

4. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy Assiut University Assiut Egypt

5. Pharmacology Department, College of Pharmacy Jouf University Sakaka Saudi Arabia

6. Department of Pharmaceutical Chemistry, Faculty of Pharmacy Sphinx University New‐Assiut Egypt

Abstract

AbstractA novel group of indolyl‐1,2,4‐triazole‐chalcone hybrids was designed, synthesized, and assessed for their anticancer activity. The synthesized compounds exhibited significant antiproliferative activity. Compounds 9a and 9e exhibited significant cancer inhibition with GI50 ranging from 3.69 to 20.40 µM and from 0.29 to >100 µM, respectively. Both compounds displayed a broad spectrum of anticancer activity with selectivity ratios ranging between 0.50–2.78 and 0.25–2.81 at the GI50 level, respectively. The synthesized compounds were also screened for their cytotoxicity by 3‐(4,5‐dimethylthiazole‐2‐yl)‐2,5‐diphenyltetrazol (MTT) assay and for inhibition of epidermal growth factor receptor (EGFR) and c‐MET (mesenchymal‐epithelial transition factor). Some of the tested compounds exhibited significant inhibition against EGFR and/or c‐MET. Compound 9b showed the highest c‐MET inhibition (IC50 = 4.70 nM) compared to foretinib (IC50 = 2.5 nM). Compound 9d showed equipotent activity compared with erlotinib against EGFR (IC50 = 0.052 µM) and displayed significant c‐MET inhibition with an IC50 value of 4.90 nM.

Publisher

Wiley

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