PREPARATION OF A CISPLATIN PRODRUG FOR USE AGAINST NON-SMALL CELL LUNG CANCER

dc.creatorRedfearn, Warren
dc.creatorShi, Yi
dc.creatorKoneru, Bhuvaneswari
dc.creatorDi Pasqua, Anthony
dc.date.accessioned2019-08-22T19:45:46Z
dc.date.available2019-08-22T19:45:46Z
dc.date.issued2014-03
dc.date.submitted2014-02-04T14:44:56-08:00
dc.description.abstractBackground: Lung cancer is the leading cause of cancer-related death in the United States, and non-small cell lung cancer (NSCLC) the most common type. NSCLC is extremely difficult to treat, resulting in a poor prognosis for patients. Platinum (Pt) anti-cancer agents, such as cisplatin, remain a mainstay in the clinic; however, these Pt complexes act nonspecifically, and thus result in serious side-effects. Development and delivery of a Pt complex with an improved therapeutic index would be highly advantageous to the fight against NSCLC. We prepared trans, cis, cis-bis(heptanoato)amine(cyclohexylamine)dichloridoplatinum(IV), referred to here as PtC, and studied its DNA binding and toxicity toward normal lung and NSCLC cells. Methods: A lipophilic Pt(IV) complex, PtC, was synthesized and characterized, and its binding to DNA and toxicity toward various cancer and normal cell lines determined. Results: We confirmed that the synthesized Pt complex binds to DNA in a manner similar to that of cisplatin, which suggests that it is cisplatin prodrug; however, probably due to its lipophilic nature and improved stability, PtC is much more toxic toward NSCLC cell lines than is cisplatin, and has a much improved therapeutic index. Conclusions: PtC shows promise as a therapeutic agent against NSCLC, and, furthermore, its lipophilic nature allows for us to incorporate it into mesoporous silica nanoparticles for fine-controlled release and the targeting of tumors.
dc.identifier.urihttps://hdl.handle.net/20.500.12503/26932
dc.language.isoen
dc.subjectcisplatin
dc.subjectNSCLC
dc.subjectcancer
dc.titlePREPARATION OF A CISPLATIN PRODRUG FOR USE AGAINST NON-SMALL CELL LUNG CANCER
dc.typeposter
dc.type.materialtext

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