|
| Synthesis and Anticancer Activity of cis-[Pt(Ⅱ)(trans-1, 2-bis(methylamino)cyclobutane) (3-hydroxyl-1, 1-cyclobutanedicarboxylate)] |
| Author Name | Affiliation | E-mail | | GAO An-Li | Platinum-Based Drug Lab, Kunming Institute of Precious Metals, Kunming 650106, China | | | QIU Jie | Lincang Maternal and Child Health Care Hospital, Lincang, Yunnan 677000, China | | | HOU Shu-Qian | Platinum-Based Drug Lab, Kunming Institute of Precious Metals, Kunming 650106, China | | | JIANG Jing | Platinum-Based Drug Lab, Kunming Institute of Precious Metals, Kunming 650106, China | dianaair@126.com | | LOU Li-Guang | Tumor PharmacologyLab, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China | | | LIU Wei-Ping | Platinum-Based Drug Lab, Kunming Institute of Precious Metals, Kunming 650106, China | liuweiping1963@126.com |
|
| Abstract: A new water-soluble and more water-stable analogue of lobaplatin, cis-[Pt(Ⅱ)(trans-1,2-bis(methylamino) cyclobutane)(3-hydroxyl-1,1-cyclobutanedicarboxylate)], was designed, with an attempt to improve the water-stability of lobaplatin while retaining its excellent anticancer profile, via the structural recombination and optimization of lobaplatin and carboplatin. The analogue was synthesized by the direct reaction between cis-[Pt(Ⅱ)(trans-1,2-bis(methylamino))I2] as an intermediate and the silver salt of 3-hydroxyl-1,1-cyclobutanedicarboxylic acid, and characterized by elemental analysis, ESI-MS, IR and 1H, 13C NMR. The anticancer activity was evaluated by both in vitro cyotoxicity against four human cancer cell lines and in vivo antitumor efficiency in human lung carcinoma NCI-H460 xenografts in nude mice. The biological tests revealed that the analogue produced significant inhibition of the tumor growth, resulting in an inhibitory rate of 54% at the dose of 60 mg·kg-1 and more importantly, it had in vivo anticancer activity comparable to that of lobaplatin. |
| Keywords: platinum complexes synthesis characterization anticancer activity |
| Hits: 1691 |
| Download times: 966 |
| GAO An-Li,QIU Jie,HOU Shu-Qian,JIANG Jing,LOU Li-Guang,LIU Wei-Ping.Synthesis and Anticancer Activity of cis-[Pt(Ⅱ)(trans-1, 2-bis(methylamino)cyclobutane) (3-hydroxyl-1, 1-cyclobutanedicarboxylate)][J].Chinese Journal of Inorganic Chemistry,2017,33(5):837-842. |
| View Full Text View/Add Comment Download reader |
|
|
|
|
|
|
|
|
