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Organische Chemie I - Prof. Dr. Rainer Schobert

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Targeted Metallodrugs

Tumours are often intrinsically resistant to cisplatin (CDDP), a mainstay of cancer therapy. Acquired resistance of initially well-responding tumours and unwanted side effects are other problems that frequently thwart regimens based on CDDP. We evaluate analogues of CDDP that overcome these problems, e.g., conjugates of Pt(II) complexes with bioactive shuttle components such as hormones, (1) or with modulators that expedite the trans-membrane transport or the drug accumulation within the cell such as terpenes. (2)
A ferrocene dicarboxylate of illudin M, (3) a toxic metabolite of the fungus Omphalotus olearis ("Jack o Lantern") exhibited selective activity in CLL cells from leukaemia patients with poor prognosis factors by targeting the transcription-coupled NER machinery. Its combination with the standard leukaemia drug fludarabine led to synergy effects in CLL cells from patients with aberrations del.17p and del.11q (high-risk group patients). This conjugate also induced p53-independent apoptosis in isolated CLL cells. Unlike illudin M, it is well tolerated by mice. (4)

1 ChemMedChem, 2, 2007, 333 and Steroids, 76, 2011, 393
2 J Inorg Biochem, 105, 2011, 1630
3 J Med Chem, 54, 2011, 6177
4 Leukemia, 2017, DOI: 10.1038/leu.2016.294

Verantwortlich für die Redaktion: André Wetzel

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