1204-22-4Relevant articles and documents
Collective enantioselective total synthesis of (+)-sinensilactam A, (+)-lingzhilactone B and (-)-lingzhiol: Divergent reactivity of styrene
Fan, Hui-Lan,Li, Cheng-Ji,Luo, Sanzhong,Qin, Hong-Bo,Zhang, Da-Wei,Zhang, Wenzhao
, p. 10066 - 10069 (2020)
The collective total synthesis of (+)-sinensilactam A, (+)-lingzhilactone B, (+)-lingzhilactone C and (-)-lingzhiol has been accomplished from a common epoxide intermediate 9. Chemoselective epoxy opening with either an aryl or alkene moiety of styrene le
Discovery of Novel Polycyclic Heterocyclic Derivatives from Evodiamine for the Potential Treatment of Triple-Negative Breast Cancer
Chen, Zhe-Sheng,Li, Dahong,Qiu, Yangyi,Wu, Liang,Xu, Jinyi,Xu, Shengtao,Yang, Dong-Hua,Yao, Hong,Zhou, Manzhen
supporting information, p. 17346 - 17365 (2021/12/09)
Evodiamine (Evo) is a quinazolinocarboline alkaloid found in Evodia rutaecarpa and exhibits moderate antiproliferative activity. Herein, we report using a scaffold-hopping approach to identify a series of novel polycyclic heterocyclic derivatives based on Evo as the topoisomerase I (Top1) inhibitor for the treatment of triple-negative breast cancer (TNBC), which is an aggressive subtype of breast cancer with limited treatment options. The most potent compound 7f inhibited cell growth in a human breast carcinoma cell line (MDA-MB-231) with an IC50 value of 0.36 μM. Further studies revealed that Top1 was the target of 7f, which directly induced irreversible Top1-DNA covalent complex formation or induced an oxidative DNA lesion through an indirect mechanism mediated by reactive oxygen species. More importantly, in vivo studies showed that 7f exhibited potent antitumor activity in a TNBC-patient-derived tumor xenograft model. These results suggest that compound 7f deserves further investigation as a promising candidate for the treatment of TNBC.
Novel evodiamine derivatives as well as preparation method and application of novel evodiamine derivatives
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Paragraph 0098; 0100, (2018/03/13)
The invention relates to the field of medicinal chemistry and particularly relates to novel evodiamine derivatives and also discloses a preparation method of the novel evodiamine derivatives and an application of the novel evodiamine derivatives to treatm
Synthesis of midodrine HCI from a novel intermediate 1-(2′,5′-dimethoxyphenyl)-2-azidoethanone
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, (2008/06/13)
Midodrine hydrochloride, ±1-(2′,5′-dimethoxyphenyl)-2-glycineamido-ethanol-(1)-HCl, is prepared from a novel intermediate, 1-(2′,5′-dimethoxyphenyl)-2-azidoethanone.
α-Chlorination of Aromatic Acetyl Derivatives with Benzyltrimethylammonium Dichloroiodate
Kajigaeshi, Shoji,Kakinami, Takaaki,Moriwaki, Masayuki,Fujisaki, Shizuo,Maeno, Kimihiro,Okamoto, Tsuyoshi
, p. 545 - 546 (2007/10/02)
Reaction of aromatic acetyl derivatives with benzyltrimethylammonium dichloroiodate in refluxing dichloroethane/methanol for several hours gave α-chloroacetyl derivatives in good yields.