The Korean Journal of Pharmacology (대한약리학회지)
- Volume 31 Issue 1 Serial No. 57
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- Pages.103-114
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- 1995
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- 0377-9459(pISSN)
Antitumor Activity and Nephrotoxicity of the Novel Platinum(II) Coordination Complex
새로운 Platinum (II) Complex [Pt (II)(trans-d-dach)(DPPE)] $(NO_3)_2$ 의 항암효과 및 신독성에 관한 연구
- Jung Jee-Chang (Department of Pharmacology, College of Medicine, Kyung Hee University) ;
- Lee Moon-Ho (Department of Pharmacology, College of Medicine, Kyung Hee University) ;
- Chang Sung-Goo (Department of Urology, College of Medicine, Kyung Hee University) ;
- Rho Young-Soo (Department of Medicinal Chemistry, College of Pharmacy, Kyung Hee University)
- Published : 1995.06.01
Abstract
Platinum coordination complexes are currently one of the most compounds used in the treatment of solid tumors. However, its use is limited by severe side effects such as renal toxicity. Our platinum-based drug discovery program is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (Ⅱ) complex analogue containing 1,2-diaminocyclohexane (dach) as carrier ligand and 1,2-bis(diphenylphosphino) ethane (DPPE) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of [Pt(trans-ddach)(DPPE).
일부 malignant tumor에 Pt-complex의 일상 응용 과정에서 신장독성등의 심한 부작용이 문제점으로 지적되고 있다. 이 연구에서는 기존의 cisplatin보다 항암효과는 우수하면서, 부작용을 감소시킨 새로운 Pt-complex의 개발에 역점을 두었다. 본 연구에서 합성한 Pt(Ⅱ) complex는 carrier ligand로서 1,2-diaminocyclohexane(dach)을 사용하였고, leaving group으로는 diophosphine류인 1,2-bisdiphenylphosphinoethane(DPPE)을 도입하였으며, 물에 대한 용해도를 높이기 위해 dinitrate로 만들었다. 새로이 합성한 [Pt(Ⅱ)(trans-d-dach)(DPPE)]
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