http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-102432622-B

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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4245
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D493-04
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439
filingDate 2011-11-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2014-07-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c1e4710e433dc21888f084793ca26c45
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a089137294b3941738a3341dcf58077f
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f196634a8b0e7ac0a80ad17f40416aa4
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publicationDate 2014-07-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-102432622-B
titleOfInvention 4-amino oxadiazole epipodophyllotoxin derivative and preparation method and application thereof
abstract The invention discloses a 4-amino oxadiazole epipodophyllotoxin derivative and a preparation method and application thereof. The 4-amino oxadiazole epipodophyllotoxin derivative has a structure shown as a Formula (1), wherein R1 represents hydrogen or methyl, and R2 represents hydrogen, alkyl, aryl, heteroaryl or heteroaryl alkyl. The derivative is prepared according to the following steps of: firstly, subjecting podophyllotoxin serving as a raw material to azido reaction, reduction, addition and elimination to obtain isothiocyanate epipodophyllotoxin; secondly, reacting an isothiocyanate epipodophyllotoxin intermediate with a hydrazide compound to obtain a thiosemicarbazide derivative; and finally, subjecting to cyclization, and thus obtaining a corresponding 4-amino oxadiazole derivative. The preparation method is simple and is easy to operate. Initial in-vitro screening tests show that the toxicity of the derivative on normal cells is obviously reduced, meanwhile, certain compounds have better anti-tumor activity, and high-efficiency and low-toxicity anti-tumor drugs can be expected to be prepared.
priorityDate 2011-11-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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