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Studies on Benzofuran-7-carboxamides as Poly(ADP-ribose) Polymerase-1 (PARP-1) Inhibitors
Lee, Sun-Kyung,Yi, Kyu-Yang,Lee, Byung-Ho,Oh, Kwang-Seok Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.4
Benzofuran-7-carboxamide was identified as a novel scaffold of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor. A series of compounds with various 2-substituents including (tertiary amino)methyl moieties substituted with aryl ring and aryl groups containing tertiary amines, were synthesized and biologically evaluated to elucidate the structure-activity relationships and optimize the potency. 2-[4-(Pyrrolidin-1-ylmethyl)phenyl]-benzofuran-7-carboxamide (42) was the most potent as an IC50 value of 40 nM among those.
Studies on Benzofuran-7-carboxamides as Poly(ADP-ribose) Polymerase-1 (PARP-1) Inhibitors
이선경,이규양,이병호,오광석 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.4
Benzofuran-7-carboxamide was identified as a novel scaffold of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor. A series of compounds with various 2-substituents including (tertiary amino)methyl moieties substituted with aryl ring and aryl groups containing tertiary amines, were synthesized and biologically evaluated to elucidate the structure-activity relationships and optimize the potency. 2-[4-(Pyrrolidin-1-ylmethyl)phenyl]- benzofuran-7-carboxamide (42) was the most potent as an IC50 value of 40 nM among those.
Chen Hao,Zhang Dong-Ming,Zhang Zhi-Ping,Li Ming-Zhang,Wu Hai-Feng 한국유전학회 2021 Genes & Genomics Vol.43 No.12
Background Mitochondrial unfolded protein response plays an important role in the occurrence and development of breast cancer. However, the role of mitochondrial unfolded protein response (UPRmt) in the sensitivity of breast cancer to cisplatin chemotherapy has not yet been cleared. Objectives The purpose of this study is to explore the role of mitochondrial unfolded protein response in breast cancer sensitivity to cisplatin. Methods In this study, qRT-PCR, Western blotting, Immunofuorescence, CCK-8, Colony formation, Transwell assay and TUNEL staining assay were used to confrm the role of UPRmt in breast cancer cells treated with cisplatin. Results Cisplatin increased the levels of UPRmt including CLPP, HSP60, LONP1 in MCF7 and MDA-MB-231 cells. UPRmt inducer Nicotinamide ribose (NR) could promote the proliferation and invasion of breast cancer cells treated with cisplatin. Importantly, SIRT3 was discovered to increase UPRmt in breast cancer cells and silencing of SIRT3 could inhibit the efect of NR in breast cancer. Conclusions UPRmt regulated by SIRT3 could protect breast cancer cell from cisplatin. Controlling SIRT3-induced UPR may be a potential therapeutic target to increase the sensitivity of breast cancer chemotherapy.