Shakya, Bhushan published the artcile2-Pyridineformamide N(4)-ring incorporated thiosemicarbazones inhibit MCF-7 cells by inhibiting JNK pathway, Computed Properties of 100-70-9, the main research area is neoplasm antitumor 2 pyridineformamide thiosemicarbazone JNK pathway; 2-Pyridineformamide thiosemicarbazone; A375; A431; Cell viability; HeLa; MCF-7.
In an effort to develop a more potent anticancer therapeutic agent, a series of 2-pyridineformamide thiosemicarbazones (I) (R = H, 4-CH3, 5-F, 6-CH3; heterocycle = pyrrolidine, piperidine, morpholine, thiomorpholine, azepane, 1-(2-pyridinyl)-piperazine) have been synthesized and evaluated for their anti-cancer activities against the cancer cells MCF-7 (breast cancer cell line), A-431 and A375 (epidermoid carcinoma cell line), and HeLa (cervical cancer cell line) using MTT assay. All these 2-pyridineformamide thiosemicarbazones exhibited anti-proliferative activities towards these cell lines. 5FAmPyrr(II) possess most profound effects against MCF-7 cells with IC50 of 0.9 μM. In flow cytometry using Propidium Iodide, II was found to induce cell death significantly in a dose dependent manner (100 nM-3 μM) and inhibited colony formation of MCF-7 cells. This compound induced pro-apoptotic protein Bax and inhibited anti apoptotic protein Bcl-2 as well as both c-Jun and Jun N-terminal kinase (abbreviated as JNK) in concentration dependent manner. Further pro-caspase 3 and PARP were inhibited by II at concentration of 3 μM. The results suggest that II exhibit anticancer potency and induced cell death by inhibiting MAPK signaling and inducing intrinsic apoptotic pathway. All these indicate that 2-pyridineformamide thiosemicarbazones could be developed as future therapeutics agents to treat cancer.
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 100-70-9 belongs to class nitriles-buliding-blocks, name is Picolinonitrile, and the molecular formula is C6H4N2, Computed Properties of 100-70-9.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts