Title of article :
The β-glucuronyl-based prodrug strategy allows for its application on β-glucuronyl-platinum conjugates
Author/Authors :
Reynier A Tromp، نويسنده , , Stella S.G.E van Boom، نويسنده , , C Marco Timmers، نويسنده , , Steven van Zutphen، نويسنده , , Gijsbert A. van der Marel، نويسنده , , Herman S. Overkleeft، نويسنده , , Jacques H. van Boom، نويسنده , , Jan Reedijk، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2004
Abstract :
The use of platinum drugs in antitumour therapy is well established. An important drawback of these chemotherapeutics is the lack of selectivity for tumour cells, usually resulting in severe toxic side effects. A glucuronyl-platinum conjugate was designed and synthesised to test the compatibility of platinum compounds with β-glucuronidase-based prodrug therapy. Instantaneous cleavage of the β-glucuronic bond in the glucuronyl-platinum conjugate was observed upon addition of β-glucuronidase resulting in PtII(dach)(4-hydroxybenzylmalonate) and glucuronic acid.
Keywords :
PMT. , Platinum , Anticancer drugs , Prodrug therapy , b-glucuronidase , ADEPT , Glucuronide prodrugs
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters