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In Vitro Cytotoxicity of Novel Platinum(II) Coordination Complexes Containing Diaminocyclohexane and Diphenylphosphines
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  • In Vitro Cytotoxicity of Novel Platinum(II) Coordination Complexes Containing Diaminocyclohexane and Diphenylphosphines
저자명
Jee-ChangJung,Young-KyuKim,Seung-JoonPark,Joo-HoChung,Sung-GooChang,Kyung-TaeLee,Min-SonBaek,Jong-JipPark,Young-SooRho
간행물명
The Korean Journal of Physiology & PharmacologyKCI,SCI,SCOPUS
권/호정보
1998년|2권 3호(통권9호)|pp.395-401 (7 pages)
발행정보
대한생리학회-대한약리학회|한국
파일정보
정기간행물|ENG|
PDF텍스트(0.39MB)
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영문초록

We have synthesized new platinum(II) analogs containing 1,2-diaminocyclohexane (dach) as a carrier ligand, 1,3-bis(diphenylphosphino) propane (DPPP) /1,2-bis(diphenylphosphino)ethane (DPPE) as a leaving group and nitrates to improve solubility. In the present study, the cytotoxicity of [Pt(trans-l-dach)(DPPP)]·2NO3 (KHPC-001) and [Pt(trans-l-dach)(DPPE)]·2NO3 (KHPC-002) was evaluated and compared on various P-388 cancer cell lines and porcine kidney cell line (LLC-PK1). The new platinum complexes demonstrated high efficacy on P-388 mouse leukemia cell line as well as cisplatin-resistant (P-388/CDDP) and adriamycin-resistant (P-388/ADR) P-388 cell lines. The intracellular platinum content was measured by a flame atomic absorption spectrophotometer (FAAS), and it was comparable to the results of IC50 of the three complexes on LLC-PK1 and P-388/S cells, while only DPPE compound was accumulated in high volume in P-388/ADR and P-388/CDDP cells. While the DNA-interstrand cross-links of KHPC-001, KHPC-002 and cisplatin were similar on P-388/S leukemia cells, these new platinum complexes were much less DNA cross-linking to a kidney derived cell line, LLC-PK1. These results indicate that KHPC-001 and KHPC-002 are a third-generation platinum complexes with potent antitumor activity and low nephrotoxicity.

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