Effect of the diamine nonleaving group in platinum-acridinylthiourea conjugates on DNA damage and cytotoxicity |
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Authors: | Guddneppanavar Rajsekhar Choudhury Jayati Roy Kheradi Alexander R Steen Bartlett D Saluta Gilda Kucera Gregory L Day Cynthia S Bierbach Ulrich |
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Institution: | Department of Chemistry, Wake Forest University, Winston-Salem, North Carolina 27109, USA. |
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Abstract: | The following complexes of type PtCl(R)(ACRAMTU)](NO3)2 (ACRAMTU = 1-2-(acridin-9-ylamino)ethyl]-1,3-dimethylthiourea)), derived from prototype 1 (with R = ethane-1,2-diamine), were synthesized: 2 (with R = (1R,2R)-1,2-diaminocyclohexane), 3 (with R = propane-1,3-diamine), 4 (with R = N1,N1,N2,N2-tetramethylethane-1,2-diamine), and 5 (with R = 2,2'-bipyridine). The DNA sequence specificity of the conjugates and their antiproliferative potential in HL-60 and H460 cells were investigated. Conjugate 3 showed the strongest non-cisplatin-type DNA damage in polymerase stop assays and superior cell kill efficacy in H460 lung cancer (IC50 = 70 nM). |
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