The Korean Journal of Pharmacology (대한약리학회지)
- Volume 29 Issue 2
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- Pages.283-295
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- 1993
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- 0377-9459(pISSN)
A New Class of Platinum (II) Complexes [Pt (trans-1-daeh) (DPPP)] $2NO_3$ and [Pt (trans-1-daeh)(DPPE)] $2NO_3$ Exhibiting Antitumor Activity and Nephrotoxieity
새로운 Platinum (II) Complex ([Pt (II)(trans-1-dach)(DPPP)] $(NO_3)_2$ 와 [Pt (II)(trans-1-dach)(DPPE)] $(NO_3)_2$ 의 항암효과 및 신독성에 관한연구
- Jung, Jee-Chang (Department of Pharmacology, College of Medicine, Kyung Hee University) ;
- Yoon, Chin-Hee (Department of Pharmacology, College of Medicine, Kyung Hee University) ;
- Chang, Sung-Goo (Department of Urology, College of Medicine, Kyung Hee University) ;
- Lee, Kyung-Tae (Department of Medicinal Chemistry, College of Pharmacy, Kyung Hee University) ;
- Rho, Young-Soo (Department of Medicinal Chemistry, College of Pharmacy, Kyung Hee University)
- 정지창 (경희대학교 의과대학 약리학교실) ;
- 윤진희 (경희대학교 의과대학 약리학교실) ;
- 장성구 (경희대학교 의과대학 비뇨기과학교실) ;
- 이경태 (경희대학교 약학대학 약화학교실) ;
- 노영수 (경희대학교 약학대학 약화학교실)
- Published : 1993.12.30
Abstract
Pt-complexes is currently one of the most compounds used in the treatment of solid tumors. However, its used 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 analogues containing 1, 2-diaminocyclohexane (dach) as carrier ligand and 1, 3-bis (diphenylphosphino) propane (DPPP)/1,2-bis (diphenylphosphino) ethane (DPPE) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of (KHPC-001) [Pt (trans-1-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 연구에서는 합성한 Pt (II) complex는 carrier ligand로서 1, 2-diaminocyclohexane (dach)을 사용하였고, leaving group으로는 diphosphine류인 1, 3-bis (diphenylphosphine)의 propane (DPPP) 및 ethane (DPPE)을 도입하였으며, 물에 대한 용해도를 높이기 위해 dinitrate로 만들었다. 새로이 합성한 [Pt (II)-(trans-1-dach)(DPPP)]
Keywords
- Platinum complexes;
- Antitumor activity;
- Nephrotoxicity;
- Rabbit proximal tubule cells;
- Human kidney cortical cells