Abstract
A trans-DDP based monofunctional phenanthridine Pt(ii) complex was synthesized and characterized. Its anticancer activity was studied in vitro on a panel of human cancer cell lines and mouse intestinal cancer organoids. This complex displays significant antitumor properties, with a different spectrum of activity than that of classic bifunctional cross-linking agents like cisplatin.
Highlights
A trans-DDP based monofunctional phenanthridine Pt(II) complex was synthesized and characterized
The development of platinum-based anticancer agents was focused on the synthesis and evaluation of complexes that obeyed structure–activity relationships (SARs)[1] set forth in the 1970’s
We report the synthesis and anticancer activity of a trans-DDP based monofunctional phenanthridine Pt(II) complex, in further pursuit of novel platinum cancer drug candidates
Summary
A trans-DDP based monofunctional phenanthridine Pt(II) complex was synthesized and characterized. The effect of geometric isomerism on the anticancer activity of the monofunctional platinum complex trans-[Pt(NH3)2(phenanthridine)Cl]NO3† Pyriplatin, cis-diammine(pyridine)chloroplatinum(II), a monofunctional, cationic platinum(II) compound, displayed a spectrum of activity that differed from that of any of the clinically approved platinum drugs.[6] the overall potency of pyriplatin was much less than that of cisplatin in all cancer cell lines tested.
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