Design, synthesis, and biological activity of a novel non-cisplatin-type platinum-acridine pharmacophore
ET Martins, H Baruah, J Kramarczyk…
Index: Martins; Baruah; Kramarczyk; Saluta; Day; Kucera; Bierbach Journal of Medicinal Chemistry, 2001 , vol. 44, # 25 p. 4492 - 4496
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Citation Number: 126
Abstract
Platinum-acridine conjugates were prepared from [PtCl2 (ethane-1, 2-diamine)] and the novel acridinylthioureas MeHNC (S) NMeAcr (6) and MeHNC (S) NMe (CH2CH2) NHAcr (15) by replacing one chloro leaving group in the cisplatin analogue with thiourea sulfur. In HL-60 leukemia cells, IC50 values for 7 (Pt-tethered 6) and 16 (Pt-tethered 15) were 75 and 0.13 μM, respectively. In the ovarian cell lines 2008 and C13*, 16 was active at ...
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