- 4 β-nitrogen substituted [...] amine podophyllotoxin derivative and its preparation method and application
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The invention provides a 4beta-nitrogen-substituted furan tertiary amine podophyllotoxin derivative. The structural general formula of the derivative is as shown in the specification. The compound is good in solubility and strong in anti-tumor activity and has an obvious suppression effect on the tumor cells such as lung cancer, malignant lymphoma, acute leukemia and the like. The invention also provides a preparation method of the compound.
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- Synthesis and evaluation of novel podophyllotoxin derivatives as potential antitumor agents
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Cancer multidrug resistance (MDR) is a common cause of treatment failure in cancer patients. Increased expression of permeability glycoprotein (P-gp), which is also known as MDR-1, is the main cause of multidrug resistance. Podophyllotoxin derivatives hold great promise in the battle to overcome multidrug resistance, as they can induce cytotoxicity through multiple mechanisms. Here, we synthesized sixteen novel podophyllotoxin derivatives and evaluated their cytotoxicities in human cancer cell lines, HeLa, K562 and K562/A02. Some of these compounds were more potent than etoposide, a clinically relevant inhibitor of DNA repair enzymes. In particular, compound 5p exhibited the most potent activity toward drug-resistant K562/A02 cells, as it robustly inhibited tumor cell proliferation and induced apoptosis. Furthermore, preliminary investigation suggested that 5p inhibited the expression of MDR-1 in K562/A02 cells more effectively than etoposide.
- Cheng, Wei-Hua,Cao, Bo,Shang, Hai,Niu, Cong,Zhang, Li-Ming,Zhang, Zhong-Heng,Tian, Dan-Li,Zhang, Shi,Chen, Hong,Zou, Zhong-Mei
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p. 498 - 507
(2014/09/16)
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- THIOTRIAZOLYL DERIVATIVES
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The invention relates to KvI.5 ion channel antagonists. Novel thiotriazolyl derivative compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by KvI.5 ion channels, are disclosed. Such cond
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Page/Page column 43
(2008/06/13)
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- PIPERIDINE DERIVATIVES USEFUL AS HISTAMINE H3 ANTAGONISTS
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Disclosed are novel compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is -C(=O)-, -C(=S)-, -(CH2)q-, -C(=NOR7)
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Page/Page column 38-39
(2010/11/25)
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- Cholinergic Agents Structurally Related to Furtrethonium. 2. Synthesis and Antimuscarinic Activity of a Series of N--2-furfuryl>dialkylamines
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In the first part of this study, devoted to the discovery of selective antimuscarinic agents, (+/-)-N--2-furfuryl>dimethylamine (5a) proved to be at least 20 times more potent in the rat ileum and bladder than in
- Feriani, Aldo,Gaviraghi, Giovanni,Toson, Giancarlo,Mor, Marco,Barbieri, Annalisa,et al.
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p. 4278 - 4287
(2007/10/02)
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