25908-92-3Relevant articles and documents
Design, synthesis and in-vitro biological evaluation of antofine and tylophorine prodrugs as hypoxia-targeted anticancer agents
Abdalla, Ashraf N.,Abdullah, Omeima,Chen, Linwei,Fischer, Peter M.,Guise, Chris P.,Liu, Yuxiu,Omran, Ziad,Patterson, Adam V.,Rauch, Cyril,Sindi, Ikhlas A.,Smaill, Jeff B.,Wang, Qingmin
, (2021/06/21)
Phenanthroindolizidines, such as antofine and tylophorine, are a family of natural alkaloids isolated from different species of Asclepiadaceas. They are characterized by interesting biological activities, such as pronounced cytotoxicity against different human cancerous cell lines, including multidrug-resistant examples. Nonetheless, these derivatives are associated with severe neurotoxicity and loss of in vivo activity due to the highly lipophilic nature of the alkaloids. Here, we describe the development of highly polar prodrugs of antofine and tylophorine as hypoxia-targeted prodrugs. The developed quaternary ammonium salts of phenanthroindolizidines showed high chemical and metabolic stability and are predicted to have no penetration through the blood–brain barrier. The designed prodrugs displayed decreased cytotoxicity when tested under normoxic conditions. However, their cytotoxic activity considerably increased when tested under hypoxic conditions.
Two optically pure isomers of NK007 and bactericidal applications
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, (2016/10/09)
The invention relates to two optically pure isomers of NK007 for short and applications in a bactericidal aspect. Compounds NK007-3 and NK007-4 have good bactericidal activity, can be used for treating plant bacteria diseases selected from fusarium wilt of cucumber, cercospora brown spot of peanut, apple ring spot, alternaria solani, puccinia polysora, rice bakanae disease, sclerotinia rot of colza, phytophthora capsici disease, wheat sharp eyespot, bipolaris maydis, watermelon anthracnose, potato late blight, rice sheath blight disease and cucumber gray mold.
Short asymmetric synthesis of phenanthroindolizidines through chiral homoallylic sulfinamines
Anton-Torrecillas, Cintia,Gonzalez-Gomez, Jose C.
, p. 7018 - 7025 (2014/10/15)
An efficient stereocontrolled preparation of chiral phenanthroindolizidines is detailed. The synthesis relies on the stereoselective indium-mediated allylation of 2-(phenanthren-9-yl)acetaldehyde derivatives with chiral tert-butylsulfinamide. Chemoselecti