Photo-induced anticancer activity of polypyridyl platinum(II) complexes.
Polypyridyl platinum(II) complexes (1-5), viz., [Pt(pyphen)Cl]Cl (1), [Pt(pyphen)(C≡CFc)]Cl (2), [Pt(pydppz)Cl]Cl (3), [Pt(pydppz)(C≡CPh)]Cl (4) and [Pt(pydppz)(C≡CFc)]Cl (5), where pyphen is 6-(2-pyridyl)-1,10-phenanthroline, pydppz is 6-(2-pyridyl)-dipyrido-[3,2-a:2',3'-c]-phenazine, FcC≡CH is ferrocenyl acetylene and PhC≡CH is phenyl acetylene, were synthesized, characterized and their DNA binding and photocytotoxic properties studied. The complexes showed strong binding affinity to calf-thymus DNA giving K(app) of ∼10(6)-10(7) M(-1). Complexes 4 and 5 showed dual mode of binding to ct-DNA. The pydppz complexes 3-5 having a photoactive phenazine moiety showed photocytotoxicity in HeLa and MCF-7 cells in UV-A light of 365 nm with apoptotic cell death as evidenced from the acridine orange/ethidium bromide dual staining and the FACS data.
Department of Inorganic and Physical Chemistry, Indian Institute of Science, Sir C.V. Raman Avenue, Bangalore 560012, India.
Basudev
B
Maity
Sudarshan
S
Gadadhar
Tridib K
TK
Goswami
Anjali A
AA
Karande
Akhil R
AR
Chakravarty
D000165:Acridine Orange; D000480:Alkynes / Q000737:chemistry*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002417:Cattle; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000494:pharmacology; D003603:Cytotoxins / Q000138:chemical synthesis* / Q000494:pharmacology; D004247:DNA / Q000737:chemistry; D053837:DNA Cleavage / Q000187:drug effects / Q000528:radiation effects; D004996:Ethidium; D006801:Humans; D008958:Models, Molecular; D010618:Phenanthrolines / Q000737:chemistry*; D010619:Phenazines / Q000737:chemistry*; D055668:Photochemical Processes; D010984:Platinum / Q000737:chemistry*; D011725:Pyridines / Q000737:chemistry*; D014466:Ultraviolet Rays
D000480:Alkynes; D000970:Antineoplastic Agents; D056831:Coordination Complexes; D003603:Cytotoxins; D010618:Phenanthrolines; D010619:Phenazines; D011725:Pyridines; D010984:Platinum; D004247:DNA; C427203:calf thymus DNA; D004996:Ethidium; D000165:Acridine Orange