Development of a series of 4-hydroxycoumarin platinum(IV) hybrids as antitumor agents: Synthesis, biological evaluation and action mechanism investigation

Add time:08/06/2019    Source:sciencedirect.com

A series of new 4-hydroxycoumarin platinum(IV) complexes were designed, synthesized and evaluated as antitumor agents. All the title compounds display moderate to effective antitumor activities toward the tested cell lines and two prominent compounds were screened out with activities comparable to cisplatin and oxaliplatin. The mechanism investigation demonstrates that the platinum(IV) compounds could be reduced to bivalence and exert significant genotoxicity to tumor cells. Meanwhile the coumarin moiety endows the title compounds with cyclooxygenase inhibitory competence which might favour the reduction of tumor-related inflammation and further influence tumor proliferation. The coumarin platinum(IV) complex could effectively induce apoptosis of SKOV-3 cells through up-regulating the expression of caspase3 and caspase9. Furthermore, the conversion of platinum(II) drugs to platinum(IV) form via the conjunction with 4-hydroxycoumarin enhances the drug uptake in whole cells and DNA simultaneously. Moreover, the 4-hydroxycoumarin platinum(IV) complex could combine with human serum albumin via van der Waals force and hydrogen bond, which would influence their transport and bioactivities in vivo.

We also recommend Trading Suppliers and Manufacturers of PLATINUM (IV) BROMIDE (cas 13455-11-3). Pls Click Website Link as below: cas 13455-11-3 suppliers

Prev:The influence of the nonleaving group on the anticancer activity of tetrachlorido platinum(IV) complexes with pyridine/bipyridine derivatives
Next:Synthesis of new platinum(IV) complexes through breaking disulfide bond; crystal structure determination, electrochemical, photoluminescence and DNA interaction investigation)