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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.
Al-Wahaibi, Lamya H; El-Sheref, Essmat M; Hammouda, Mohamed M; Youssif, Bahaa G M.
Afiliação
  • Al-Wahaibi LH; Department of Chemistry, College of Sciences, Princess Nourah Bint Abdulrahman University, Riyadh 11564, Saudi Arabia.
  • El-Sheref EM; Chemistry Department, Faculty of Science, Minia University, El Minia 61519, Egypt.
  • Hammouda MM; Department of Chemistry, College of Science and Humanities in Al-Kharj, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
  • Youssif BGM; Chemistry Department, Faculty of Science, Mansoura University, Mansoura 35516, Egypt.
Pharmaceuticals (Basel) ; 16(3)2023 Mar 22.
Article em En | MEDLINE | ID: mdl-36986566
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 various NMR, mass spectra, and elemental analyses verified the structures of all the newly obtained compounds. The antiproliferative effects of 6a-e, 7a, and 7b against four cancer cells were investigated. The most effective antiproliferative compounds were 6b, 6e, and 7b. Compounds 6b and 7b inhibited EGFR with IC50 values of 84 and 78 nM, respectively. Additionally, 6b and 7b were the most effective inhibitors of BRAFV600E (IC50 = 108 and 96 nM, respectively) and cancer cell proliferation (GI50 = 35 and 32 nM against four cancer cell lines, respectively). Finally, the apoptosis assay results revealed that compounds 6b and 7b had dual EGFR/BRAFV600E inhibitory properties and showed promising antiproliferative and apoptotic activity.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: Pharmaceuticals (Basel) Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Arábia Saudita País de publicação: Suíça

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: Pharmaceuticals (Basel) Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Arábia Saudita País de publicação: Suíça