Premium
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 .