A facile and efficient synthesis of d 6 ‐labeled PU‐H71, a purine‐scaffold Hsp90 inhibitor | Zendy

Taldone Tony | Zendy; Zatorska Danuta | Zendy; Kang Yanlong | Zendy; Chiosis Gabriela | Zendy

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A facile and efficient synthesis of d 6 ‐labeled PU‐H71, a purine‐scaffold Hsp90 inhibitor

Author(s) -

Taldone Tony,

Zatorska Danuta,

Kang Yanlong,

Chiosis Gabriela

Publication year - 2010

Publication title -

journal of labelled compounds and radiopharmaceuticals

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.432

H-Index - 47

eISSN - 1099-1344

pISSN - 0362-4803

DOI - 10.1002/jlcr.1689

Subject(s) - chemistry , hsp90 inhibitor , purine , combinatorial chemistry , scaffold , pharmacology , stereochemistry , biochemistry , enzyme , hsp90 , biomedical engineering , medicine , heat shock protein , gene

PU‐H71 is a purine‐scaffold Hsp90 inhibitor currently undergoing late stage preclinical evaluation for the treatment of cancer. In this investigation, we present a simple method for the synthesis of d 6 ‐labeled PU‐H71 for use as an internal standard to accurately quantitate the drug in biological matrices based on an LC‐MS‐MS method. PU‐H71‐d 6 was synthesized in five steps using readily available 1,3‐dibromopropane‐d 6 and is an important compound for the advancement of our clinical program. Copyright © 2009 John Wiley & Sons, Ltd.

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