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Anti-proliferation evaluation of new derivatives of indole-6-carboxylate ester as receptor tyrosine kinase inhibitors.

Mustafa M AllawiAmmar Abdul Razzak MahmoodLubna H TahtamouniAbdulrahman M SalehSana I KanaanKhaled M M SalehMai F AlSakhenNisreen HimsawiSalem R Yasin
Published in: Future medicinal chemistry (2024)
Aim: The main goal was to create two new groups of indole derivatives, hydrazine-1-carbothioamide ( 4a and 4b ) and oxadiazole ( 5 , and 6a-e ) that target EGFR ( 4a , 4b , 5 ) or VEGFR-2 ( 6a-e ). Materials & methods: The new derivatives were characterized using various spectroscopic techniques. Docking studies were used to investigate the binding patterns to EGFR/VEGFR-2, and the anti-proliferative properties were tested in vitro . Results: Compounds 4a (targeting EGFR) and 6c (targeting VEGFR-2) were the most effective cytotoxic agents, arresting cancer cells in the G2/M phase and inducing the extrinsic apoptosis pathway. Conclusion: The results of this study show that compounds 4a and 6c are promising cytotoxic compounds that inhibit the tyrosine kinase activity of EGFR and VEGFR-2, respectively.
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