13754-38-6Relevant articles and documents
Design, synthesis and antitumor evaluation of new 1,8-naphthalimide derivatives targeting nuclear DNA
Liang, Gui-Bin,Wei, Jian-Hua,Jiang, Hong,Huang, Ri-Zhen,Qin, Jing-Ting,Wang, Hui-Ling,Wang, Heng-Shan,Zhang, Ye
, (2021)
Four series of new 3-nitro naphthalimides derivatives, 4(4a?4f), 5(5a?5i), 6(6a?6e) and 7 (7a?7j), were designed and synthesized as antitumor agents. Methyl thiazolyl tetrazolium (MTT) screening assay results revealed that some compounds displayed effecti
Design, synthesis, and biological evaluation of matrine derivatives possessing piperazine moiety as antitumor agents
Xu, Yiming,Liang, Pengyun,Rashid, Haroon ur,Wu, Lichuan,Xie, Peng,Wang, Haodong,Zhang, Shuyan,Wang, Lisheng,Jiang, Jun
, p. 1618 - 1627 (2019)
Using matrine (1) as the lead compound, a series of new piperazinyl matrine derivatives were designed, synthesized and evaluated for their antitumor activities in vitro and in vivo. Structure activity relationship (SAR) analysis indicated that introductio
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.
Anti-tumor compound, pharmaceutically acceptable salt, preparation method and application thereof
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, (2021/03/13)
The invention provides an anti-tumor compound and the pharmaceutically acceptable salt thereof, which have good anti-breast cancer activity, are excellent anti-breast cancer lead compounds, and have broad prospects in preparation of drugs for preventing or treating breast cancer. The preparation method is simple and convenient for industrial production.