Synthesis, Cytotoxicity and Pro-apoptosis of Novel Benzoisoindolin Hydrazones as Anticancer Agents

Zhao, Yu; Jie, Hui; Wang, Dan; Zhu, Li; Fang, Jinghuai; Zhao, Xiaodong

doi:10.1248/cpb.58.1324

Cited by 21 publications

(9 citation statements)

References 18 publications

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“…3 More importantly, polycyclic γ-lactam derivative 1 exhibited efficient inhibitory effects on proliferation of cancer cells. 4 This biological activity has made the synthesis of polycyclic γ-lactams quite attractive, and several straightforward and robust methods for the construction of polycyclic γ-lactams have been elegantly established. 5 …”

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confidence: 99%

Construction of Polycyclic γ-Lactams and Related Heterocycles via Electron Catalysis

2016

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Cascade radical cyclization of 1,6-enynes for the construction of biologically important polycyclic γ-lactams and related heterocycles is reported. In these radical cascade processes, three new C–C bonds are formed and transition metals are not required to run these sequences. The mild reaction conditions, broad substrate scope, and the importance of the heterocyclic products render the approach valuable.

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confidence: 99%

Construction of Polycyclic γ-Lactams and Related Heterocycles via Electron Catalysis

2016

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“…For this study, 75, 100, and 150 μM concentrations of compounds 1 and 4g were used. Annexin V, which is a protein existing on the surface of the cells that undergo apoptosis, was also used to determine early apoptosis in the cells .…”

Section: Resultsmentioning

confidence: 99%

Synthesis of Tolmetin Hydrazide–Hydrazones and Discovery of a Potent Apoptosis Inducer in Colon Cancer Cells

Küçükgüzel

Koç

Çıkla-Süzgün

et al. 2015

Archiv der Pharmazie

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Tolmetin hydrazide and a novel series of tolmetin hydrazide-hydrazones 4a-l were synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR, (1)H NMR) methods. N'-[(2,6-Dichlorophenyl)methylidene]-2-[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetohydrazide (4g) was evaluated in vitro using the MTT colorimetric method against the colon cancer cell lines HCT-116 (ATCC, CCL-247) and HT-29 (ATCC, HTB-38) to determine growth inhibition and cell viability at different doses. Compound 4g exhibited anti-cancer activity with an IC50 value of 76 μM against colon cancer line HT-29 (ATCC, HTB-38) and did not display cytotoxicity toward control NIH3T3 mouse embryonic fibroblast cells compared to tolmetin. In addition, this compound was evaluated for caspase-3, caspase-8, caspase-9, and annexin-V activation in the apoptotic pathway, which plays a key role in the treatment of cancer. We demonstrated that the anti-cancer activity of this compound was due to the activation of caspase-8 and caspase-9 involved in the apoptotic pathway. In addition, in this study, we investigated the catalytical effect of COX on the HT-29 cancer line, the apoptotic mechanism, and the moleculer binding of tolmetin and compound 4g on the COX enzyme active site.

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“…and experimental conditions. For example, (2-hydroxyaryl)ydene hydrazones derived from quinoxalin-2-hydrazine were active in the range from 1.8 to 14.2 µM (HCT116) [26]; from benzoisoindoline-based hydrazides in the range from 5.8 to > 50 µM (HCT116) and >50 µM (A549) [27]; benzoisothiazol-based hydrazides from 0.5 to > 100 µM (CCRF-CEM); (2-N-heteroaryl)ydene hydrazones derived from bezoxazole-2-hydrazine showed IC 50 values in the range from 0.01 to > 50 µM (CCRF-CEM) [28,29]. These examples indicate that anticancer effect is strongly dependent on the structure of both aldehyde/ketone and hydrazine part of hydrazone molecule.…”

Section: Cytostatic Activitymentioning

confidence: 99%

Caffeine–hydrazones as anticancer agents with pronounced selectivity toward T-lymphoblastic leukaemia cells

Kaplánek

Jakubek

Rak

et al. 2015

Bioorganic Chemistry

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Synthesis, Cytotoxicity and Pro-apoptosis of Novel Benzoisoindolin Hydrazones as Anticancer Agents

Cited by 21 publications

References 18 publications

Construction of Polycyclic γ-Lactams and Related Heterocycles via Electron Catalysis

Construction of Polycyclic γ-Lactams and Related Heterocycles via Electron Catalysis

Synthesis of Tolmetin Hydrazide–Hydrazones and Discovery of a Potent Apoptosis Inducer in Colon Cancer Cells

Caffeine–hydrazones as anticancer agents with pronounced selectivity toward T-lymphoblastic leukaemia cells

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