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Scientific Reports

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Design, in silico studies and biological evaluation of novel chalcones tethered triazolo[3,4-a]isoquinoline as EGFR inhibitors targeting resistance in non-small cell lung cancer

Published:4 November 2024 DOI: 10.1038/s41598-024-76459-x PMID: 39496648
Nesma Abdelaal,?Mohamed A Ragheb,?Hamdi M Hassaneen,?Emad M Elzayat,?Ismail A Abdelhamid

Abstract

A novel series of six [1,2,4]triazolo[3,4-a]isoquinolin-3-yl)-3-(1,3-diphenyl-1H-pyrazol-4-yl)prop-2-en-1-ones (3a-3f) was designed and synthesized. They were characterized based on spectral and elemental analyses. In silico studies were also committed to provide insights and a better understanding of their structural features. The six compounds were screened for their antiproliferative activity using the MTT assay against five human cancer cell lines, namely, A549, HCT116, PC3, HT29, and MCF-7 in parallel with the non-cancerous human lung cell line WI-38. The results showed that 3e and 3f have potential cytotoxic activities, especially on A549 cells with IC50?=?2.3 μM and 1.15 μM, respectively. Meanwhile, they recorded a minimal cytotoxic effect on WI-38 cells. Concerning the molecular mechanism of action, the present study showed the inhibitory effect of the six compounds against total EGFR. The most potent EGFR inhibitors were 3e and 3f with IC50?=?0.031 μM and 0.023 μM, respectively. The selectivity index of 3f for EGFRT790M was 1.81 times more selective than that of lapatinib. In addition, 3e and 3f initiated cell cycle arrest at the G2/M and pre-G1 phases along with the downregulation of anti-apoptotic protein Bcl2 and the upregulation of pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. Further studies are recommended to evaluate animal models' promising anticancer activity and molecular mechanism of triazolo[3,4-a]isoquinoline derivatives 3e and 3f.

Substances (20)

Materials
Procduct Name CAS Molecular Formula Supplier Price
Gefitinib 184475-35-2 C22H24ClFN4O3 810 suppliers $5.00-$1191.00
Gefitinib 184475-35-2 C22H24ClFN4O3 810 suppliers $5.00-$1191.00
Gefitinib 184475-35-2 C22H24ClFN4O3 810 suppliers $5.00-$1191.00
Gefitinib 184475-35-2 C22H24ClFN4O3 810 suppliers $5.00-$1191.00
Lapatinib 231277-92-2 C29H26ClFN4O4S 572 suppliers $10.00-$1900.00
Lapatinib 231277-92-2 C29H26ClFN4O4S 572 suppliers $10.00-$1900.00
Lapatinib 231277-92-2 C29H26ClFN4O4S 572 suppliers $10.00-$1900.00
Lapatinib 231277-92-2 C29H26ClFN4O4S 572 suppliers $10.00-$1900.00
Erlotinib 183321-74-6 C22H23N3O4 468 suppliers $5.00-$2776.00
Erlotinib 183321-74-6 C22H23N3O4 468 suppliers $5.00-$2776.00

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