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Intercalator-linked cisplatin: synthesis and antitumor activity of cis-dichloroplatinum(II) complexes connected to acridine and phenylquinolines by one methylene chain by Yuji Mikata; Mika Yokoyama; Kaoru Mogami; Masako Kato; Ichiro Okura; Makoto Chikira; Shigenobu Yano is a Chemistry article available to read on EtoBox.

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Three novel intercalator-linked cisplatin-type platinum complexes, cis. [ PtCI, aminomethylacridine) ] ( I ), cis. [ PtCI,aminomethyl-2-phenylquinoline) ] (2), and cis- aminomethyl-2-phenylquinoline) ] { 3 ) were synthesized, q'hoe structure of I was determined by X-ray crystallography (triclinic, space group PI with a = 15.00716), b = 15.597{ 4). c~ !0,398{3) A, a=98.51(3) °, /.¢=96.79{3) °. 'F = 114.61(2) °, Z=4, R=0.053, R~,=0.063). The antitumor activity of the platinum complexes was investigated against the HeLa cell. Compound 3 was the most cytotoxic among the complexes synthesized here and was more eff~tive than cisplatin, It was suggested from mic|'oscopic analysis that the acridine complex 1, which had no cytotoxicity against the HeLa cell, was not incorporated in the nucleus of the cell. Against the P388 ceil, however, complex 1 gave a more therapeutic result than 3. The covalent binding ability of the cisplatin moiety was suppressed significantly in these compounds. The results of molecular mechanics showed that inter,:alation and covalent binding could be compatible. The cytotoxicity and DNA binding ability of phenylquinolineotype ligands wore also studied to evMuate th

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Author

Yuji Mikata; Mika Yokoyama; Kaoru Mogami; Masako Kato; Ichiro Okura; Makoto Chikira; Shigenobu Yano

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0020-1693)

Published

1998

Language

EN

Field

Chemistry (Physical Sciences)