The Korean Journal of Pharmacology (대한약리학회지)
- Volume 32 Issue 1
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- Pages.93-102
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- 1996
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- 0377-9459(pISSN)
In Vitro Antitumor Activity and Nephrotoxicity of the Novel Platinum(II) Coordination Complex Containing Cis-dach/Diphosphine
새로운 Platinum(II)Complex ([Pt(II)(cis-dach)(DPPP)].$(NO_3)_2$ 의 항암효과 및 신독성
- Jung, Jee-Chang (Department of Pharmacology, School of Medicine, Kyung Hee University) ;
- Yim, Sung-Vin (Department of Pharmacology, School of Medicine, Kyung Hee University) ;
- Park, Seung-Joon (Department of Pharmacology, School of Medicine, Kyung Hee University) ;
- Chung, Joo-Ho (Department of Pharmacology, School of Medicine, Kyung Hee University) ;
- Ko, Kye-Chang (Department of Pharmacology, School of Medicine, Kyung Hee University) ;
- Chang, Sung-Goo (Department of Urology, School of Medicine, Kyung Hee University) ;
- Rho, Young-Soo (College of Pharmacy, Kyung Hee University)
- 정지창 (경희대학교 의과대학 약리학교실) ;
- 임성빈 (경희대학교 의과대학 약리학교실) ;
- 박승준 (경희대학교 의과대학 약리학교실) ;
- 정주호 (경희대학교 의과대학 약리학교실) ;
- 고계창 (경희대학교 의과대학 약리학교실) ;
- 장성구 (경희대학교 의과대학 비뇨기과학교실) ;
- 노영수 (경희대학교 약학대학)
- Published : 1996.06.30
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 nephrotoxicity. Our platinum-based drug discovery program is aimed at developing drugs capable of diminishing toxicity and broadening the clinical spectrum of activity of cisplatin. We synthesized new Pt(II) complex analogue containing 1,2-diaminocyclohexane (dach) as carrier ligand and 1,3-bis(diphenyl phosphino)propane (DPPP) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of PC-1 [Pt(cis-dach) (DPPP)].
일부 malignant tumor에 Pt-complex의 임상 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 diphosphine류인 1,3-bis (diphenylphosphine의 propane(DPPP) 을 도입하였으며, 물에 대한 용해도를 높이기 위해 dinitrate로 만들었다. 새로이 합성한 [Pt(II)(cia-dach)(DPPP)].
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