Design and Synthesis of a PSMA Inhibitor–Doxorubicin Conjugate for Targeted Prostate Cancer Therapy | Zendy

Jayaprakash Sarva | Zendy; Wang Xinning | Zendy; Heston Warren D. | Zendy; Kozikowski Alan P. | Zendy

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

Author(s) -

Jayaprakash Sarva,

Wang Xinning,

Heston Warren D.,

Kozikowski Alan P.

Publication year - 2006

Publication title -

chemmedchem

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.817

H-Index - 100

eISSN - 1860-7187

pISSN - 1860-7179

DOI - 10.1002/cmdc.200500044

Subject(s) - conjugate , prostate cancer , doxorubicin , cancer research , bioconjugation , cytotoxic t cell , chemistry , prostate , cancer , pharmacology , medicine , combinatorial chemistry , biochemistry , chemotherapy , in vitro , mathematical analysis , mathematics

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 μ M .

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