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Dual EGFR/HER2 inhibitors and apoptosis inducers: New benzo[g]quinazoline derivatives bearing benzenesulfonamide as anticancer and radiosensitizers.

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0 Published in 2018 at "Bioorganic chemistry"

DOI: 10.1016/j.bioorg.2018.07.015

Abstract: Dual targeting of EGFR and HER2 is a proven anticancer strategy for the treatment of solid tumors. An array of new N-substituted-2-(4-oxo-3-(4-sulfamoylphenyl)-3,4-dihydrobenzo[g]quinazolin-2-ylthio) acetamides 5-18 were designed and synthesized from the starting compound 4-(2-mercapto-4-oxobenzo[g]quinazolin-3(4H)-yl) benzenesulfonamide 4.… read more here.

Keywords: dual egfr; her2 inhibitors; anticancer; egfr her2 ... See more keywords

Design, Synthesis, Antiproliferative Actions, and DFT Studies of New Bis–Pyrazoline Derivatives as Dual EGFR/BRAFV600E Inhibitors

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1 Published in 2023 at "International Journal of Molecular Sciences"

DOI: 10.3390/ijms24109104

Abstract: Some new Bis-pyrazoline hybrids 8–17 with dual EGFR and BRAFV600E inhibitors have been developed. The target compounds were synthesized and tested in vitro against four cancer cell lines. Compounds 12, 15, and 17 demonstrated strong… read more here.

Keywords: brafv600e inhibitors; brafv600e; egfr brafv600e; dual egfr ... See more keywords

One-Pot Synthesis of 1-Thia-4-azaspiro[4.4/5]alkan-3-ones via Schiff Base: Design, Synthesis, and Apoptotic Antiproliferative Properties of Dual EGFR/BRAFV600E Inhibitors

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2 Published in 2023 at "Pharmaceuticals"

DOI: 10.3390/ph16030467

Abstract: In this investigation, novel 4-((quinolin-4-yl)amino)-thia-azaspiro[4.4/5]alkan-3-ones were synthesized via interactions between 4-(2-cyclodenehydrazinyl)quinolin-2(1H)-one and thioglycolic acid catalyzed by thioglycolic acid. We prepared a new family of spiro-thiazolidinone derivatives in a one-step reaction with excellent yields (67–79%). The… read more here.

Keywords: thia azaspiro; azaspiro alkan; egfr brafv600e; synthesis ... See more keywords