• The Korean Journal of Physiology and Pharmacology
• /
• 제4권2호
• /
• pp.159-167
• /
• 2000

We have synthesized a novel platinum(II) coordination complex containing cis-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,2-dichloroethane (DCE) as a leaving group. In addition, nitrate was added to improve the water-solubility. A new series of [Pt(cis-DACH)(DCE)] $2NO_3(PC)$ was evaluated for its cytotoxic activity on T-24 and J-82 human bladder carcinoma cells and normal primary cultured kidney cells. PC has demonstrated high levels of cytotoxicity against T-24 and J-82 cells. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues, determined using the MTT assaying technique, the $[^3H]-thymidine$ uptake and glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum(II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new clinically available anticancer chemotherapeutic agents.

• 약학회지
• /
• 제44권5호
• /
• pp.399-405
• /
• 2000

We have synthesized a novel platinum (II) coordination complex containing trans-ι-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,2-bis (diphenylphosphino)ethane (DPPE) as a leaving group. In addition, nitrate was added to improve the water-solubility. A new series of [Pt (trans-ι-DACH) (DPPE)].2NO$_3$(PC) was evaluated for its cytotoxic activity on MKN-45 human gastric adenocarcinoma cells and normal primary cultured kidney cells. PC has demonstrated high levels of cytotoxicity against MKN-45/S, MKN-45/ADR and MKN-45/CDDP cells. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells, and human renal cortical tissues, determined using the MTT assaying technique, the ($^3$H)-thymidine uptake and the glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum (II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new clinically available anticancer chemotherapeutic agents.

• 대한화학회지
• /
• 제31권3호
• /
• pp.258-270
• /
• 1987

여러 용매(methanol, ethanol, butanol, ethylether, methylacetate, acetone, THF 및 acetylacetone)중에서 아직 보고된 바 없는 공동을 달리한 crown ether들을 리간드로 한 토륨(IV) 고체 착물을 합성하였다. 이 고체 착물에 대한 배위 화학적인 정보를 얻기 위하여 원소분석(C.H.N) 및 ICPAS법에 의한 토륨분상, 열분석과 Karl-Fischer적정법에 의한 착물중의 결정수 분석에 의해서 고체 착물들의 조성을 결정하였다. 그리고 적외선, 자외선 분광분석, $^1H$-핵자기 공명 분석 및 X-선 회절분석법에 의하여 각 합성 착물들의 결합구조에 대한 정보들을 얻었고 각 합성 착물들에 대한 용매화 현상을 논의하였다. 그 결과 아세틸아세톤 용매하에서 합성된 착물들은 아세틸아세톤을 제외한 모든 실험 용매중에서 합성된 crown ether를 가지는 토륨(IV) 착물들은 용매화 반응이 일어나지 않았다. $Th^{4+}$금속이온에 대한 리간드 결합비는 고리의 크기에 주로 영향을 받으며 12-crown-4의 경우는 1:1([$Th^{4+}$]:[lig.]) 착물, 15-crown-5의 경우는 2:3 착물 및 18-crown-6와 dicyclohexano-18-crown-6의 경우는 1:1 착물이었다. 용매화가 일어나는 15-crown-5 와 18-crown-6 착물의 경우는 1:1:1([$Th^{4+}$]:[lig.]:$[CH_3COCH_2COCH_3]$)이었다. 용매화하지 않는 모든 착물들은 crown-ether의 n-${\sigma}^{\ast}$전자전이를, 그리고 용매화된 착물은 crown-ether n-${\sigma}^{\ast}$와 acac의 $n-{\pi}^{\ast}$전자전이를 동시에 나타냈다. 반양성자성 용매에서 모든 착물들은 1:1전해질로, 물에서는 1:4전해질로 각각 행동하는 9배위자 착물임을 알 수 있다.

• 대한화학회지
• /
• 제55권4호
• /
• pp.594-602
• /
• 2011

4[N-(furfural)amino]antipyrine semicarbazone(FFAAPS)와 질산 란탄(III)이 형성하는 배위화합물의 입체화학에 미치는 ${\alpha}$-, ${\beta}$- 및 ${\gamma}$-picolines의 영향을 연구하였다. 이들 배위화합물의 일반적 조성은 [Ln(FFAAPS)$(NO_3)_3$Pic] (Ln=La, Pr, Nd, Sm, Gd, Tb, Dy 또는 Ho 및 Pic=${\alpha}$-, ${\beta}$- or ${\gamma}$-picolines)이다. 모든 배위화합물은 원소분석, 분자량, 몰전기전도도, 자기수자율, 적외선 및 자외선 스펙트럼으로 특성을 조사하였다. 적외선 연구결과 FFAAPS는 N, N, O 주개를 갖는 중성 삼배위 리간드로 행동하는 반면, ${\alpha}$-, ${\beta}$- 또는 ${\gamma}$-picoline는 헤테로 N-원자를 통하여 란탄(III) 이온에 배위된다. 질산 음이온은 이들 화합물에서 이배위로 결합한다. 자외선 스펙트럼 결과로부터 전자구름 퍼짐 효과(${\beta}$), covalence factor($b^{1/2}$), Sinha parameter (${\delta}%$) 및 covalence angular overlap parameter(${\eta}$)를 계산하였다. 이들 착물의 열적성질을 열무게 분석법에 의해 연구하였다. 본 화합물에 있어서 란탄(III)의 배위수는 10으로 조사되었다. 기본 리간드인 FFAAPS와 착물의 항박테리아 선별조사 결과, 이들 착물은 중간 정도의 항박테리아 활성을 보였다.

• 대한화학회지
• /
• 제43권6호
• /
• pp.628-635
• /
• 1999

활성화된 $Mn(IV)O_2$를 이용하여 2,6-bis(hydroxymethyl)-4-methylphenol로부터 2,6-diformyl-p-cresol과 2-hydroxy-3-hydroxymethyl-5-methylbenzaldehyde를 제조하였다. 2-hydroxy-3-hydroxymethyl-5-methylbenzaldehyde와 ethylenediamine 및 1,3-diaminopropane의 축합반응에 의해 6-배위 칸막이 리간드, $H_4L[A]와\; H_4L[B]$를 각각 얻었다. methanol에서 2,6-diformyl-p-cresol과 1,2-diaminobenzene으로부터 부분적으로 환원된 거대고리, $H_4[20]DOTA$를 얻을 수 있었다. 이 $H_4[20]DOTA$와 lanthanide(IlI) nitrate 간의 반응 또는 methanol에서 주형과정(template procedure)에 의해 일핵 착물, $[Ln(IIl)(H_2[20]DOTA)(ClO_4)(H_2O)]\;{\cdot}\;3H_2O과\; [Ln([20]DOTA)(NO_3)(H_2O)](NO_3)_2\;{\cdot}\;xH_2O$를 각각 합성하였다. $[Ln([20]DOTA)(NO_3)(H_2O)](NO_3)_2\;{\cdot}\;xH_2O$를 2일 정도 methanol에 정치함으로써 얻은 $[Ln([20]DOTA)(NO_3)(CH_3OH)]^{2+}$에서 배위된 $CH_3OH$이 주게원자가 O인 보조리간드, $L_a$(=salicylic acid, p-chlorobenzoic acid, benzoic acid, acetic acid, 4-bromophenol)에 의해 치환될 때 평형상수 (K)를 25$^{\circ}C$, ${\mu}$=0.1M $NaClO_4$에서 분광학적 방법으로 결정하였다. 이 때 평형상수(K) 값들은 보조리간드 pKa 크기의 반대 경향인 salicylic acid>p-chlorobenzoic acid>benzoic acid>acetic acid>4-bromophenol 순서로 나타났다.

• Biomolecules & Therapeutics
• /
• 제5권2호
• /
• pp.125-132
• /
• 1997

Cisplatin, a platinum-complex, is currently one of the most effective compounds used in the treat-ment 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 selective cytotoxicity. 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(cia-DACH)(DPPE)] . $2NO_3$ (PC) was synthes-ized and characterized by their elemental analysis and by various spectroscopic techniques [infrared (IR), $_{13}$carbon nuclear magnetic resonance (NMR)] .PC demonstrated acceptable and significant antitumor activity against SKOV-3 and OVCAR-3 human ovarian carcinoma cell lines as compared with that of cisplatin. The cytotoxicity of PC in normal cells was found quite less than that of cisplatin using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), ($^3$H)thymidine uptake and glucose consumption tests in rabbit renal proximal tubular cells, human renal cortical cells and tissues. In conclusion, PC is considered to be more selective cytotoxicity toward human ovarian cancer cells than normal human/rabbit kidney cells.

• The Korean Journal of Physiology and Pharmacology
• /
• 제3권3호
• /
• pp.283-291
• /
• 1999

We have synthesized novel platinum (II) coordination complex containing cis-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,2-bis(diphenylphosphino)ethane (DPPE) as leaving group. Furthermore, nitrate was added to improve the water-solubility. A new series of [Pt(cis-DACH)(DPPE)] $2NO_3(PC)$ was evaluated its antitumor activity on various MKN-45 human gastric adenocarcinoma cell-lines and normal primary cultured kidney cells. The new platinum complex demonstrated high efficacy in the cytotoxicity on MKN-45 cell-lines as well as adriamycin-resistant (MKN-45/ADR) and cisplatin-resistant (MKN-45/CDDP) cells. The cytotoxicities of PC were found quite less than those of cisplatin in rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues using MTT assay, $[^3H]-thymidine$ uptake and glucose consumption tests. Based on these results, this novel platinum (II) coordination complex, was considered as better a valuable lead for improving antitumor activities with low nephrotoxicities in the development of a new clinically available anticancer chemotherapeutic agents.

• 대한화학회지
• /
• 제63권6호
• /
• pp.453-458
• /
• 2019

Synthesis of ZnCo₂O₃ oxide is performed by sol-gel method via nitrate-citrate route. Powder X-ray diffraction (XRD) study shows monoclinic unit cell having lattice parameters: a = 5.721(1) Å, b = 8.073(2) Å, c = 5.670(1) Å, β = 93.221(8)°, space group P_2/m and Z = 4. Average crystallite sizes determined by Scherrer equation are the range ~14-32 nm, whereas SEM micrographs show nano-micro meter size particles formed in ZnCo₂O₃. Endothermic peak at ~798 K in the Differential scanning calorimetric (DSC) trace without weight loss could be due to structural transformation and the endothermic peak ~1143 K with weight loss is due to reversible loss of O₂ in air atmosphere. Energy Dispersive X-ray (EDX) analysis profile shows the presence of elements Zn, Co and O which indicates the purity of the sample. Magnetic measurements in the range of +12 kOe to -12 kOe at 10 K, 77 K, 120 K and at 300 K by PPMS-II Physical Property Measurement System (PPMS) shows hysteresis loops having very low values of the coercivity and retentivity which indicates the weakly ferromagnetic nature of the oxide. Observed X-band EPR isotropic lineshapes at 300 K and 77 K show positive g-shift at g_iso ~2.230 and g_iso ~2.217, respectively which is in agreement with the presence of paramagnetic site Co²⁺(3d⁷) in the oxide. DC conductivity value of 2.875 ×10^-8 S/cm indicates very weakly semiconducting nature of ZnCo₂O₃ at 300 K. DRS absorption bands ~357 nm, ~572 nm, ~619 nm and ~654 nm are due to the d-d transitions ⁴T_1g(⁴F)→²E_g(²G), ⁴T_1g(⁴F)→⁴T_1g(⁴P), ⁴T_1g(⁴F)→⁴A_2g(⁴F), ⁴T_1g(⁴F)→⁴T_2g(⁴F), respectively in octahedral ligand field around Co²⁺ ions. Direct band gap energy, E_g~ 1.5 eV in the oxide is obtained by extrapolating the linear part of the Tauc plot to the energy axis indicates fairly strong semiconducting nature of ZnCo₂O₃.