Abstract：
:Three new platinum(II) complexes with pendent morpholine were synthesized, namely complex 1 ([Pt(L)Cl]CF3SO3), complex 2 ([Pt(L)(NH3)](CF3SO3)2) and complex 3 ([Pt(L)(PPh3)](CF3SO3)2), where L = 4'-[4-(4-morpholinobutyloxy)phenyl]-2,2':6',2″-terpyridine and PPh3 = triphenylphosphine. The detailed molecular structures of complex 3, L and its precursor L' (1,4'-[4-(4-bromobutyloxy)phenyl]-2,2':6',2″-terpyridine) were determined by single crystal X-ray diffraction. An evaluation of in vitro cytotoxicity for both ligand and complexes was performed by methyl thiazolyl tetrazolium (MTT) assay in three cancer cell lines and normal cells as the control, respectively. IC50 values of complexes 1-3 were lower than those exhibited for the reference drug cisplatin, and selectivity of these complexes were greater than cisplatin. Among them, complex 3 with a leaving group PPh3 was found to be the most efficacious complex against certain cell lines, especially for cisplatin-resistant A549cisR cells. These complexes were found to bind DNA, induce efficient DNA unwinding. Meanwhile, topoisomerase (Topo) I inhibitory activities by three complexes were detected, and a minimum inhibitory concentration of 15 μM of complex 3 was found totally inhibit Topo I activity.
journal_name
J Inorg Biochemjournal_title
Journal of inorganic biochemistryauthors
Chai K,Kuang W,Lan Z,Zhang L,Jiang Y,Han T,Niu J,Wang J,Duan Xdoi
10.1016/j.jinorgbio.2018.12.003subject
Has Abstractpub_date
2019-03-01 00:00:00pages
17-24eissn
0162-0134issn
1873-3344pii
S0162-0134(18)30432-Xjournal_volume
192pub_type
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journal_title：Journal of inorganic biochemistry
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journal_title：Journal of inorganic biochemistry
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journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2009.01.020
更新日期：2009-05-01 00:00:00
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更新日期：2018-03-01 00:00:00
