Conjugation of vitamin E analog α-TOS to Pt(IV) complexes for dual-targeting anticancer therapy.
We report two platinum(IV) complexes conjugated with a vitamin E analog, α-tocopherol succinate (α-TOS). One of the conjugates displays the activity of both cisplatin and α-TOS in cancer cells, causing damage to DNA and mitochondria simultaneously. Accordingly, it serves as a promising dual-targeting anticancer agent.
Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA. lippard@mit.edu.
Kogularamanan
K
Suntharalingam
Ying
Y
Song
Stephen J
SJ
Lippard
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004249:DNA Damage; D006801:Humans; D008928:Mitochondria / Q000187:drug effects; D010984:Platinum / Q000737:chemistry* / Q000494:pharmacology*; D014810:Vitamin E / Q000737:chemistry*; D024502:alpha-Tocopherol / Q000737:chemistry*; D051028:bcl-2-Associated X Protein / Q000378:metabolism; D051020:bcl-X Protein / Q000378:metabolism
D000970:Antineoplastic Agents; C494826:BAX protein, human; C494811:BCL2L1 protein, human; D051028:bcl-2-Associated X Protein; D051020:bcl-X Protein; D014810:Vitamin E; D010984:Platinum; D024502:alpha-Tocopherol