Design and Synthesis of a PSMA Inhibitor-Doxorubicin Conjugate for Targeted Prostate Cancer Therapy

Design and Synthesis of a PSMA Inhibitor-Doxorubicin Conjugate for Targeted Prostate Cancer Therapy

Prostate‐specific membrane antigen (PSMA) provides an attractive target for the development of targeted chemotherapeutics for prostate cancer. We have designed and synthesized a bioconjugate 1 that comprises the cytotoxic drug doxorubicin and one of our previously described urea‐based PSMA inhibitor...

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Veröffentlicht in:ChemMedChem 2006-03, Vol.1 (3), p.299-302
Hauptverfasser: Jayaprakash, Sarva, Wang, Xinning, Heston, Warren D., Kozikowski, Alan P.
Format: Artikel
Sprache:eng
Schlagworte:
Antineoplastic Agents - therapeutic use
Cell Line, Tumor
doxorubicin
Doxorubicin - chemistry
Doxorubicin - therapeutic use
Drug Design
Humans
inhibitors
Male
neurotransmitters
prostate cancer
Prostate-Specific Antigen - chemistry
Prostatic Neoplasms - drug therapy
PSMA
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Zusammenfassung:Prostate‐specific membrane antigen (PSMA) provides an attractive target for the development of targeted chemotherapeutics for prostate cancer. We have designed and synthesized a bioconjugate 1 that comprises the cytotoxic drug doxorubicin and one of our previously described urea‐based PSMA inhibitors. While this bioconjugate retained high binding affinity for PSMA, it inhibited only 30 % of C4‐2 cell growth at a concentration of 5.0 μM.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.200500044