Cytotoxic Peptides: Naphthoquinonyl Derivatives of Luteinizing Hormone-Releasing Hormone

Letters in Peptide Science - Tập 5 - Trang 421-427 - 1998
Shai Rahimipour1, Lev Weiner1, Prativa Bade Shrestha-Dawadi2, Shmuel Bittner3, Yitzhak Koch4, Mati Fridkin1
1Department of Organic Chemistry, The Weizmann Institute of Science, Rehovot, Israel
2Department of Chemistry, Ben-Gurion University of the Negev, Beer-Sheva, Israel
3Department of Chemistry, Ben Gurion University of the Negev, Beer Sheva, Israel
4Department of Neurobiology, The Weizmann Institute of Science, c[Rehovot, Israel

Tóm tắt

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.

Tài liệu tham khảo

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