93344-48-0Relevant articles and documents
Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer
Long, Huan,Hu, Xiaolong,Wang, Baolin,Wang, Quan,Wang, Rong,Liu, Shumeng,Xiong, Fei,Jiang, Zhenzhou,Zhang, Xiao-Qi,Ye, Wen-Cai,Wang, Hao
, p. 12089 - 12108 (2021/09/06)
Poly (ADP-ribose) polymerase-1 (PARP-1) is a potential target for the discovery of chemosensitizers and anticancer drugs. Amentoflavone (AMF) is reported to be a selective PARP-1 inhibitor. Here, structural modifications and trimming of AMF have led to a series of AMF derivatives (9a-h) and apigenin-piperazine/piperidine hybrids (14a-p, 15a-p, 17a-h, and 19a-f), respectively. Among these compounds, 15l exhibited a potent PARP-1 inhibitory effect (IC50 = 14.7 nM) and possessed high selectivity to PARP-1 over PARP-2 (61.2-fold). Molecular dynamics simulation and the cellular thermal shift assay revealed that 15l directly bound to the PARP-1 structure. In in vitro and in vivo studies, 15l showed a potent chemotherapy sensitizing effect against A549 cells and a selective cytotoxic effect toward SK-OV-3 cells through PARP-1 inhibition. 15l·2HCl also displayed good ADME characteristics, pharmacokinetic parameters, and a desirable safety margin. These findings demonstrated that 15l·2HCl may serve as a lead compound for chemosensitizers and the (BRCA-1)-deficient cancer therapy.
BENZOTHIOPHENE DERIVATIVE HAVING ANTI-CANCER EFFECT
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Paragraph 0012, (2018/09/25)
PROBLEM TO BE SOLVED: To provide a novel compound that has an excellent anti-cancer effect. SOLUTION: Provided is a benzothiophene derivative represented by formula (1), or a pharmaceutically acceptable salt thereof. [R1 is H, OH, a halogeno group, a C1 to 12 alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylamino group or an alkylthio group, a substituted/unsubstituted aryl group, a substituted/unsubstituted benzyl group, or a substituted/unsubstituted carbon ring or heterocyclic ring condensed to 5-6 position; R2 is H, OH, a halogeno group, a C1 to 12 alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylamino group or an alkylthio group; a substituted/unsubstituted aryl group or a substituted/unsubstituted benzyl group.] SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2016,JPO&INPIT
Synthetic studies on flavone derivatives. XIV. Synthesis of 2',4'-5'-trioxygenated flavones
Iinuma,Iwashima,Matsuura
, p. 4935 - 4941 (2007/10/02)
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