Cytotoxic Peptides: Naphthoquinonyl Derivatives of Luteinizing Hormone-Releasing Hormone |
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| Authors: | Shai Rahimipour Lev Weiner Prativa Bade Shrestha-Dawadi Shmuel Bittner Yitzhak Koch and Mati Fridkin |
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| Institution: | (1) Department of Organic Chemistry, The Weizmann Institute of Science, Rehovot, 76100, Israel;(2) Department of Chemistry, Ben Gurion University of the Negev, Beer Sheva, 84105, Israel;(3) Department of Neurobiology, The Weizmann Institute of Science, c[Rehovot, 76100, Israel |
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| Abstract: | In an attempt to produce efficient cytotoxic derivatives of luteinizing hormone-releasing hormone (LH-RH), two novel 1,4-naphthoquinone derivatives of D-Lys6]-LH-RH were synthesized primarily by solid-phase peptide synthesis, in good yield and high purity. The ability of each analog to produce reactive oxygen species using enzymatic reduction, i.e. NADPH-cytochrome P-450 reductase, was evaluated employing electron spin resonance (ESR) spectroscopy and spin-trapping techniques. The ESR results suggest that the novel cytotoxic analogs are extremely effective in generating oxygen radicals. |
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| Keywords: | ESR LH-RH quinones solid phase synthesis targeted chemotherapy |
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