Rajesh Shashikala Mariswamy, Doddakunche Shivaramu Prasanna, Bhol Chandra Sekhar, Swaroop Toreshettahally R, Preetham Habbanakuppe D, Suresh Rajaghatta N, Chinnathambi Arunachalam, Govindasamy Chandramohan, Alharbi Sulaiman Ali, Shalini Veeresha Gowda, Ahn Kwang Seok, Rangappa Shobith, Rangappa Kanchugarakoppal S
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysuru, India.
Department of Applied Sciences, Visvesvaraya Technological University, Muddenahalli Campus, Chikkaballapur, India.
Chem Biol Drug Des. 2025 Apr;105(4):e70091. doi: 10.1111/cbdd.70091.
Epoxides are well-known compounds as anticancer agents. In this article, we present the synthesis of novel 3'-phenyl-1-((1-aryl-1H-1,2,3-triazol-5-yl)methyl)spiro[indoline-3,2'-oxiran]-2-one derivatives by the regioselective reaction of sulfur ylides with 1,2,3-triazole-tethered isatins and their anticancer effects on hepatocellular carcinoma (HCC) cells HepG2 and HCCLM3. The cell viability assays indicated that RR-01 and RR-07 had emerged as the most potent cytotoxic agents on the tested cell lines. Colony formation and migration assay results confirmed the anticancer effects of these compounds by inhibiting the formation of colonies and migration. Further, nuclear fragmentation staining assay showed that the compounds induce apoptosis. Acridine orange staining assays showed that our lead candidates (RR-01 and RR-07) induced autophagy in liver cancer cells.
环氧化合物是众所周知的抗癌剂。在本文中，我们报道了通过硫叶立德与1,2,3 - 三唑连接的异吲哚酮的区域选择性反应合成新型3'-苯基-1-((1-芳基-1H-1,2,3-三唑-5-基)甲基)螺[吲哚啉-3,2'-环氧乙烷]-2-酮衍生物及其对肝癌细胞HepG2和HCCLM3的抗癌作用。细胞活力测定表明，RR-01和RR-07已成为对测试细胞系最有效的细胞毒剂。集落形成和迁移试验结果通过抑制集落形成和迁移证实了这些化合物的抗癌作用。此外，核碎裂染色试验表明这些化合物诱导细胞凋亡。吖啶橙染色试验表明，我们的主要候选物（RR-01和RR-07）诱导肝癌细胞自噬。
