Design, synthesis and biological evaluation of 7-(5-((substituted - amino)-methyl)-thiophen-2-yl)-spiro-[chroman-2,4'-piperidin]-4-one hydrochloride analogues as anticancer agents.

摘要: Abstract A series of thirty-one novel 7–(5–((amino)-methyl)-thiophen–2–yl)-spiro-[chroman–2,4′–piperidin]–4–one hydrochloride analogues (Cst 1 – 31) have been designed, synthesized and characterized by 1H NMR, 13C NMR MS spectral analysis. Here, we evaluated the anticancer potential biological results low-molecular-weight bridgehead oxygen nitrogen-containing spirochromanones on proliferation apoptosis human breast cancer cell line (MCF–7) Murine melanoma (B16F10). The activity ranged from 2.9 to 35.0 µM. most potent compounds Cst-22, Cst-24 Cst-31 were found be less toxic against embryonic kidney (HEK-293) lines. causing significant cytotoxicity through apoptotic death also G2 phase arrest cycle in B16F10 cells. In-silico ADME prediction stidies titled within rules outlined, these may not face any pharmacokinetic associated issues mere future upon developmental stage. These conjugates serve as a lead for discovery drug candidate with better therapeutic profile.