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Synthesis and biological activity of novel platinum(II) complexes of glutamate tethered to hydrophilic hematoporphyrin derivatives by Yeong-Sang Kim; Rita Song; Chong Ock Lee; Youn Soo Sohn is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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A new series of hematoporphyrin-platinum(II) conjugates was prepared by platination of the glutamate ligand tethered to hydrophilic hematoporphyrin derivatives, in which different numbers of ethylene oxide unit were introduced to modulate the hydrophobic/hydrophilic balance of the conjugates. The antitumor activity of the hematoporphyrin-platinum(II) conjugates was assayed in vitro and in vivo against the leukemia L1210 cell line. Among the complexes, compound 11 exhibited not only higher in vivo activity (T/C% 1⁄4 192) than cisplatin (T/C% 1⁄4 184) and carboplatin (T/C% 1⁄4 168), but also elevated tumor-localizing effect (tumor/muscle ratio >3).

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Author

Yeong-Sang Kim; Rita Song; Chong Ock Lee; Youn Soo Sohn

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

2004

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)