154902-09-7Relevant articles and documents
Design, synthesis and anti-cancer activity evaluation of podophyllotoxin-norcantharidin hybrid drugs
Han, Hong-Wei,Qiu, Han-Yue,Hu, Cui,Sun, Wen-Xue,Yang, Rong-Wu,Qi, Jin-Liang,Wang, Xiao-Ming,Lu, Gui-Hua,Yang, Yong-Hua
, p. 3237 - 3242 (2016)
In this study, we designed and synthesized eighteen podophyllotoxin-norcantharidin hybrid drugs which could exhibit more potent anti-cancer activity than the parent drugs. Through the anti-proliferation assay, the most potent anti-cancer agent was screened out, namely Q9 (IC50?=?0.88?±?0.18?μM against MCF-7 cell line), and it showed lower cytotoxicity against non-cancer cells, human embryonic kidney cells (293T) (IC50?=?54.38?±?3.78?μM). Additionally, based on the flow cytometry analysis result, it can cause a remarkable cell cycle arrest at G2/M phase and induce apoptosis in MCF-7 cells more significantly than podophyllotoxin or norcantharidin per se. Moreover, the expression of cell cycle relative protein CDK1 was up regulated while a protein required for mitotic initiation, Cyclin B1 was down regulated. Furthermore, according to the confocal microscopy observation results, it was shown that Q9 was a potent tubulin polymerization inhibitor and the effect is comparable to that of colchicine. For further investigation on the aforementioned mechanisms, we performed western blot experiments, thus finding the increase of the cleavage of PARP. Consistent with these new findings, molecular docking observations suggested that compound Q9 could be developed as a potential anticancer agent.
Synthesis and biological evaluation of camptothecin substituted norcantharimide derivatives
Lan, Qing,Zhou, Yiqi,Wang, Xianheng,Wang, Yuhe,Zhao, Changkuo
, p. 5752 - 5756 (2020/10/23)
In this paper, a series of novel derivatives of camptothecin substituted norcantharimide was designed by mimic strategy. These compounds were synthesized in moderate yields by directly coupling CPT with N-amino acid norcantharimides. Their cytotoxicity to
Synthesis of l-ascorbic acid-amino acid-norcantharidin conjugates and their biological activity evaluation in vitro
Wang, Xianheng,Wu, Caoyuan,Zhang, Jidong,Zhao, Changkuo,Zhou, Yiqi
supporting information, (2022/01/06)
Three components of L-ascorbic acid, amino acid and functionalized norcantharidins were constructed together in several steps to form 42 norcantharidin derivatives in a high yield. The structure of these synthesized l-ascorbic acid-amino acid-norcantharidin conjugates are determined by 1HNMR, 13CNMR and MS spectrum. The results showed that compounds 6e, 6g, 6j, 6l, 6m, 6b, 6e, 6i, and 6n showed high cytotoxicity to HepG2 and compounds 6b, 6e-g, 6l, 6n, 7b, 7d, 7h, 7i, 7n, 8g, 8i exhibited high cytotoxicity to SW480; Meanwhile, besides 6b, 6e, 6g, and 6k, the other compounds showed less toxic to LO2 at a concentration of 50 μg/mg after 72 h. Compound 6g can induce Mφ-type macrophages derived from mouse bone marrow to polarize to M1-type macrophages.
Amide compounds for regulating WNT signal channel and application of compounds
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Paragraph 0297; 0299, (2019/07/11)
The invention belongs to the technical field of medicine, and particularly relates to amide compounds for regulating a WNT signal channel and an application of the compounds. The compounds have a structure represented by a general formula I shown in the description.
Conjugates of podophyllotoxin and norcantharidin as dual inhibitors of topoisomeraseⅡ and protein phosphatase 2A
Tang, Zhen-Bo,Chen, Yao-Zhang,Zhao, Jie,Guan, Xiao-Wen,Bo, Yong-Xin,Chen, Shi-Wu,Hui, Ling
, p. 568 - 576 (2016/08/12)
A series of novel conjugates of podophyllotoxin and norcantharidin was designed using association strategy, and synthesized by coupling 4′-demethylepipodophyllotoxin with N-amino acid norcantharimides, and their cytotoxicitiy was evaluated against four hu
Synthesis of phosphonodipeptide derivatives of exo-7-oxabicyclo [2.2.1] heptane-2, 3-dicarboxylic anhydride
Zhou, Zheng Hong,Zhang, Zhong Biao,Chen, Ru Yu
, p. 45 - 52 (2007/10/03)
A series of phosphonodipeptide derivatives of norcantharidin (exo-7-oxabicyclo[2.2.1] heptane-2,3-dicarboxylic anhydride) were synthesized and their structures were confirmed by 1H NMR, 31P NMR, IR, MS and elemental analysis.
Synthesis and Anticonvulsant Activity of 7-Oxabicycloheptane Derivatives: Part 1 - N-Alkyl, N-Aryl and N-Heteroaryl Derivatives of 3,6-Epoxyhexahydrophthalimide
Joshi, Balawant S.,David, Joy,Gawad, Dilip H.
, p. 131 - 135 (2007/10/02)
A series (sixty one) of N-substituted 3,6-epoxyhexahydrophthalimides have been prepared by the condensation of the appropriately substituted alkyl, aryl and heteroarylamines with exo-cis-3,6-epoxyhexahydrophthalic anhydride (2).Some of the compounds exhib
