Akademik Veri Yönetim Sistemi
12th International Drug Chemistry Congress, Antalya, Türkiye, 7 - 10 Mart 2024, ss.42-46
Compounds bearing 2-indolinone moiety have significant anticancer activities. Sunitinib malate is a 3-arylidene-2-indolinone derivative anticancer agent approved by FDA for the treatment of advanced renal carcinoma and gastrointestinal stromal tumors. In this study, new 1-benzyl-3-arylidene-2-indolinones were designed and their ADME profiles and compliance with Lipinski’s rules were examined and it is found that all of the compounds met the criteria. For the synthesis of 5-nonsubstituted/methyl-2-indolinones, 1H-indole-2,3-diones were benzylated from the position 1-, then reduced to 2-indolinones with hydrazine hydrate, followed by the reaction with 1H-indole-3-carbaldehyde. The newly synthesized 1-benzyl-3-[(1H-indol-3-yl)methylidene]-1,3-dihydro-2H-indol-2-ones were tested against human kidney (CAKI-1 and A498), pancreas (MIA PaCa-2), colon (HT-29 and HCT-116), breast (MCF-7 and MDA-MB-231) and lung (A549) cancer cells by using Sunitinib malate as reference standard. HUVEC (human umbilical vein endothelial cell), MCF-10F (human breast epithelial cell) and Beas2b (human lung bronchial epithelial cell) cell lines have been used as healthy control cells. Test results showed that most of the compounds were effective against A498, HT-29 and HCT-116 cancer cells at 1 μM and below, and were more effective and less toxic than Sunitinib malate.