An innovative approach to development of new pyrazolylquinolin-2-one hybrids as dual EGFR and BRAFV600E inhibitors
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DOI: 10.1007/s11030-025-11127-4
Abstract: Novel quinoline-based derivatives 2a–e and 4a–j have been designed and synthesized as potential antiproliferative agents. The designed compounds were screened for their antiproliferative activity against sixty cell lines according to NCI protocol. The promising hybrids… read more here.
Keywords: approach development; brafv600e; egfr brafv600e; development new ... See more keywords
Design, synthesis, and antiproliferative activity of new 1,2,3-triazole/quinazoline-4-one hybrids as dual EGFR/BRAFV600E inhibitors
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DOI: 10.1039/d4ra06694d
Abstract: A novel series of 1,2,3-triazole/quinazoline-4-one hybrids (8a–t) were designed and synthesized as dual-targeted antiproliferative agents. Compounds 8a–t were evaluated for their antiproliferative efficacy against a panel of four cancer cell lines. The results indicated that… read more here.
Keywords: one hybrids; brafv600e inhibitors; triazole quinazoline; egfr brafv600e ... See more keywords
Design, Synthesis, Antiproliferative Actions, and DFT Studies of New Bis–Pyrazoline Derivatives as Dual EGFR/BRAFV600E Inhibitors
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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
Benzimidazole-Based Derivatives as Apoptotic Antiproliferative Agents: Design, Synthesis, Docking, and Mechanistic Studies
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DOI: 10.3390/molecules29020446
Abstract: A new class of benzimidazole-based derivatives (4a–j, 5, and 6) with potential dual inhibition of EGFR and BRAFV600E has been developed. The newly synthesized compounds were submitted for testing for antiproliferative activity against the NCI-60… read more here.
Keywords: benzimidazole based; cell; egfr brafv600e; antiproliferative activity ... 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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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
Design, Synthesis, and Anti-Proliferative Action of Purine/Pteridine-Based Derivatives as Dual Inhibitors of EGFR and BRAFV600E
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DOI: 10.3390/ph16050716
Abstract: The investigation of novel EGFR and BRAFV600E dual inhibitors is intended to serve as targeted cancer treatment. Two sets of purine/pteridine-based derivatives were designed and synthesized as EGFR/BRAFV600E dual inhibitors. The majority of the compounds… read more here.
Keywords: dual inhibitors; based derivatives; pteridine based; egfr brafv600e ... See more keywords