• Title/Summary/Keyword: Novel chemical structure

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Synthesis and Biological Evaluation of Novel GSK-3β Inhibitors as Anticancer Agents

  • Choi, Min-Jeong;Oh, Da-Won;Jang, Jae-Wan;Cho, Yong-Seo;Seo, Seon-Hee;Jeong, Kyu-Sung;Ko, Soo-Young;Pae, Ae-Nim
    • Bulletin of the Korean Chemical Society
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    • v.32 no.6
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    • pp.2015-2020
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    • 2011
  • A series of isoxazol-indolin-2-one was designed for GSK-3${\beta}$ inhibitors as novel anticancer agents based on their binding mode analysis in GSK-3${\beta}$ crystal structure. Total 21 compounds were synthesized and evaluated for their inhibitory activity against two tumor cell lines (DU145 and HT29). Most of the synthesized compounds were potent with above 80% inhibitory activity at 100 ${\mu}M$, and several compounds were examined for inhibitory activity against GSK-3${\beta}$. Among them, 15(Z) ($R_1$=H, $R_2$=3-Cl-phenyl) was most active with 78% inhibition of tumor cell line (HT29) at 20 ${\mu}M$ and 72% inhibition of GSK-3${\beta}$ at 20 ${\mu}M$.

Synthesis of Novel Polythiol for Plastic Optical Lens and its Ophthalmic Lens

  • Jang, Dong-Gyu;Roh, Soo-Gyun;Kim, Jong-Hyo;Jin, Wen-Yi;Seo, Jin-Moo;Kwon, Myeong-Ja;Lee, Soo-Min
    • Bulletin of the Korean Chemical Society
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    • v.30 no.10
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    • pp.2227-2232
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    • 2009
  • Novel polythiol materials of urethane lens series for plastic optical lens were synthesized from polyol materials via thioisouronium of thiourea with c-HCl in refluxing aqueous solution, in which polythiol material was carried out from hydrolysis of thioisouronium by ammonia water. Their structure properties were identified by EA, EI-MS, FT-IR, $^1H\;and\;^{13}C$ NMR spectroscopies and TGA. Their ophthalmic lenses as polythiourethane material were prepared by thermal curing to an injected glass mold using the evenly solutions of diisocyanates series (TDI, XDI, HDI or IPDI) with polythiols. Polythiourethane shows that the strong stretching mode for SH group of polythiol disappeared in FT-IR spectra after thermosetting polymerization. Thermal deformation starting temperature of ophthalmic lenses was determined by TMA. Ophthalmic lenses made from characteristic polythiol and diisocyanate series have transparency, colorless and good impact strength, in which thermal resistance and impact strength of ophthalmic lenses were influenced by diisocyanate series. Physical properties of ophthalmic lens have contrast thermal resistance with impact strength. The property of thermal resistance and impact strength for respective ophthalmic lenses was examined by TMA and drop ball test.

Novel 99mTc(CO)3 Complexes with WAY-100635 Moiety for the Development of 5-HT1A Receptor lmaging Agent

  • Choi, Kang-Hyuk;Pyun, Mi-Sun;Hong, Young-Don;Choi, Sun-ju
    • Bulletin of the Korean Chemical Society
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    • v.30 no.5
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    • pp.1107-1112
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    • 2009
  • The aim of this study is to develop and synthesize $5-HT_{1A}$ receptor imaging agents with WAY-100635 moiety and $^{99m}Tc(CO)_3$ core. WAY-100635 is commonly known as $5-HT_{1A}$ antagonist and its labeled compound ([$^{11}C$] WAY-100635) has been used as effective radioligand for imaging brain $5-HT_{1A}$ receptors with PET(Positron Emission Tomography). However, there are several restrictions in using a radioisotope of C-11 and requires for more effective radioisotopes and ligands. In order to produce a structure most similar to WAY-100635, WAY-100635 derivatives containing a cysteine chelator were designed and confirmed by using in silico (Hyperchem). The novel compounds (7a, 7b, 7c) were prepared in five or 7 steps with yields of 16%, 36% and 42%, respectively and radiolabeled with $[^{99m}Tc(CO)_3(H_2O)_3]^{+}$. The labeling yield was 99% for all the newly synthesized compounds. [$^{99m}Tc(CO)_3$]- WAY-100635 derivatives show a neutral charge which were confirmed by paper electrophoresis.

Synthesis and Properties of Novel Y-type Nonlinear Optical Polyester Containing Cyanovinylthiophene with Enhanced Thermal Stability of Second Harmonic Generation

  • Lee, Ga-Young;Kim, Jin-Hyang;Jang, Han-Na;Won, Dong-Seon;No, Hyo-Jin;Lee, Ju-Yeon;Rhee, Bum-Ku;Choi, Hee-Dok
    • Bulletin of the Korean Chemical Society
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    • v.30 no.3
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    • pp.661-666
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    • 2009
  • 1-{2,4-Di-(2-hydroxyethoxy)phenyl}-2-(2-thienyl)ethene (5) was prepared and condensed with terephthaloyl chloride to yield polyester (6). Polymer 6 was reacted with tetracyanoethylene to give novel Y-type polyester (7) containing 1-(2,4-dioxyethoxy)phenyl-2-{5-(2,2,3-tricyanovinyl)-2-thienyl)}ethenyl groups as NLO-chromophores, which are parts the polymer backbones. Polymer 7 is soluble in common organic solvents such as acetone and N,N-dimethylformamide. It showed thermal stability up to 300 ${^{\circ}C}$ in thermogravimetric analysis with glasstransition temperature obtained from differential scanning calorimetry near 134 ${^{\circ}C}$. The second harmonic generation (SHG) coefficient ($d_33$) of poled polymer film at the 1560 nm fundamental wavelength was around 6.74 x $10^{-9}$ esu. The dipole alignment exhibited high thermal stability up to the glass-transition temperature ($Tg$), and there was no SHG decay below 135 ${^{\circ}C}$ because of the partial main-chain character of polymer structure, which is acceptable for NLO device applications.

Synthesis of Novel Prepolymers Containing No Bisphenol A and Preparation of Organic Matrices for Dental Applications (비스페놀 A를 함유하지 않은 치과용 신규 프리폴리머의 합성 및 유기 매트릭스의 제조)

  • Son, Jun-Sik;Lee, Ki-Baek;Park, Kwi-Deok;Kim, Jae-Jin;Ahn, Kwang-Duk;Kim, Jung-Hyun;Han, Dong-Keun
    • Polymer(Korea)
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    • v.30 no.6
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    • pp.538-544
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    • 2006
  • Two kinds of novel bifunctional methacrylated prepolymers (170-2MA and 631-2MA) which have similar structure with 2,2-bis[4- (2'-hynroxy-3'-methacryloyloxypropoxy)phenyl] propane (Bis-GMA) was synthesized for dental applications as an alternative to Bis-GMA containing bisphenol A that is doubtful as an endocrine disrupter. The organic matrices were prepared by mixing a diluent and/or a monomer with the synthesized methacrylated prepolymers. The yield, viscosity, and chemical structures of the prepolymers and the physical and methanical properties of the organic matrices were evaluated. The yields of the prepolymers synthesized through a ring-opening reaction of epoxy compound and methacrylic acid were above 90% and the viscosities of the prepolymers were much lower than that of the Bis-GMA control. From the results of $^1H-NMR$ and FTIR analyses, the chemical structures of the prepolymers were similar to that of Bis-GMA. In addition, the curing time, poly-merization shrinkage, photoconversion, polymerization depth, and compressive strength of the organic matrices formulated with 170-2MA and 631-2MA prepolymers exhibited comparable to or better than those of the existing Bis-GMA-based one. These results suggest that the novel methacrylated prepolymers which have no endocrine disrupter can be an alternative to Bis-GMA and be applicable to dental polymer materials.

Synthesis of New Blue OLEDs with Biphenyl Structure and Relationship between EL Efficiency and Drift Mobility (Biphenyl 구조를 가진 새로운 청색 유기 발광 재료의 합성 및 EL효율과 이동도의 관계에 대한 연구)

  • Lee, Tae-Hoon;Ryu, Jung-Yi;Kim, Tae-Hoon;Nam, Jang-Hyun;Park, Seong-Soo;Son, Se-Mo
    • Journal of the Korean Graphic Arts Communication Society
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    • v.22 no.2
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    • pp.179-198
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    • 2004
  • Organic electroluminescent devices are light-emitting diodes in which the active materials consist entirely of organic materials. Recently, many fluorescent organic materials have been reported and the study on synthesis and application of new organic light-emitting materials has been demanded. This paper reports the optical and electrical characteristics of OLEDs using novel polymers containing biphenyl structure. First, Optical properties of novel light-emitting biphenyl derivatives doped with poly(9-vinyl carbazole)(PVK) and emitted blue, bluish green color, which is attributed to the overlap area between PL spectrum of host(PVK) and absorption spectra of guests(polymer). This is correspondent with F$\"{o}$rster energy transfer process in the blends. And, OLED devices were fabricated using poly (3,4-ethylenedioxy thiophene) (PEDOT) as a hole injection material and tris-(8-hydroxyquinoline) aluminum ($Alq_3$) as an electron transporting material. EL devices fabricated as ITO/PEDOT/PVK doped with biphenyl derivatives/$Alq_3$/Li:Al and I-V-L chatacteristics and emitting efficiency of EL devices were examined. Finally, the drift mobility of PVK doped with biphenyl derivatives and $Alq_3$ were measured by TOF technique varying applied electric field. EL efficiency was increased as the ratio of hole mobility of PVK doped with biphenyl derivatives and electron mobility of $Alq_3$ was close to one.

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Structures and Magnetic Properties of Monomeric Copper(II) Bromide Complexes with a Pyridine-Containing Tridentate Schiff Base

  • Kang, Sung Kwon;Yong, Soon Jung;Song, Young-Kwang;Kim, Young-Inn
    • Bulletin of the Korean Chemical Society
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    • v.34 no.12
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    • pp.3615-3620
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    • 2013
  • Two novel copper(II) bromide complexes with pyridine containing Schiff base ligands, $Cu(pmed)Br_2$ and $Cu(pmed)Br_2$ where pmed = N'-((pyridin-2-yl)methylene)ethane-1,2-diamine (pmed) and dpmed = N,N-diethyl-N'-((pyridin-2-yl)methylene)ethane-1,2-diamine (dpmed) were synthesized and characterized using X-ray single crystal structure analysis, optical and magnetic susceptibility measurements. Crystal structural analysis of $Cu(pmed)Br_2$ showed that the copper(II) ion has a distorted square-pyramidal geometry with the trigonality index of ${\tau}=0.35$ and two intermolecular hydrogen bonds, which result in the formation of two dimensional networks in the ab plane. On the other hand, $Cu(pmed)Br_2$ displayed a near square-pyramidal geometry with the value of ${\tau}=0.06$. In both compounds, the NNN Schiff base and one Br atom occupy the basal plane, whereas the fifth apical position is occupied by the other Br atom at a greater Cu-Br apical distance. The reported complexes show $g_{\mid}$ > $g_{\perp}$ > 2.0023 with a $d_{x2-y2}$ ground state and a penta-coordinated square pyramidal geometry. Variable temperature magnetic susceptibility measurements showed that the developed copper(II) complexes follow the Curie-Weiss law, that is there are no magnetic interactions between the copper(II) ions since the Cu--Cu distance is too far for magnetic contact.

Ni Nanoparticle Anchored on MWCNT as a Novel Electrochemical Sensor for Detection of Phenol

  • Wang, Yajing;Wang, Jiankang;Yao, Zhongping;Liu, Chenyu;Xie, Taiping;Deng, Qihuang;Jiang, Zhaohua
    • Nano
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    • v.13 no.11
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    • pp.1850134.1-1850134.10
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    • 2018
  • Increasing active sites and enhancing electric conductivity are critical factors to improve sensing performance toward phenol. Herein, Ni nanoparticle was successfully anchored on acidified multiwalled carbon nanotube (a-MWCNT) surface by electroless plating technique to avoid Ni nanoparticle agglomeration and guarantee high conductivity. The crystal structure, phase composition and surface morphology were characterized by XRD, SEM and TEM measurement. The as-prepared Ni/a-MWCNT nanohybrid was immobilized onto glassy carbon electrode (GCE) surface for constructing phenol sensor. The phenol sensing performance indicated that Ni/a-MWCNT/GCE exhibited an amazing detection performance with rapid response time of 4 s, a relatively wide detection range from 0.01 mM to 0.48 mM, a detection limit of $7.07{\mu}M$ and high sensitivity of $566.2{\mu}A\;mM^{-1}\;cm^{-2}$. The superior selectivity, reproducibility, stability and applicability in real sample of Ni/a-MWCNT/GCE endowed it with potential application in discharged wastewater.

Fabrication of Zirconium Titanate Thin film from Layer-by-Layer Structure of Primitive Oxides prepared by PRTMOCVD (PRTMOCVD 법을 통한 단성분계 산화막의 적층형 구조로부터 Zirconium Titanate 박막의 제조)

  • Song, Byung-yun;Kwon, Yong Jung;Lee, Won Gyu
    • Korean Chemical Engineering Research
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    • v.45 no.4
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    • pp.378-383
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    • 2007
  • A novel fabrication method for the multi-component metal oxides such as zirconium titanate($Zr_xTi_{1-x}O_2$) has been suggested, which would yield the uniform film characteristics and control the film composition at relatively low process temperature. The method has the basic concept that firstly layer-by-layer structure is constructed with the primitive oxide layers, which are components of the desired multi-component oxides, and secondly the film is annealed at appropriate thermal conditions for the transformation to a single-phase multi-component oxides. In this study, PRTMOCVD(pulsed rapid thermal metalorganic chemical vapor deposition) possessing the superior thickness controllability was introduced to prepare $ZrO_2$ and $TiO_2$ thin film for zirconium titanate. Single-phase zirconium titanate thin films have been prepared successfully by the interdiffusion of oxide multilayers having several alternating layers of $ZrO_2$ and $TiO_2$. The Zr/Ti ratio of zirconium titanate could be controlled easily by altering the thickness of $ZrO_2$ and $TiO_2$ thin film.

Effect of Substituents on Benzenesulfonyl Motif of 4-Phenyl-1-arylsulfonylimidazolidinones for Their Cytotoxicity

  • Lee, Hui-Soon;Park, Kyung-Lae;Choi, Sang-Un;Lee, Chong-Ock;Jung, Sang-Hun
    • Archives of Pharmacal Research
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    • v.23 no.6
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    • pp.579-584
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    • 2000
  • To explore the effect of substituents' on phenyl motif on sulfonyl function of novel anticancer 4-phenyl-1-benzenesulfonylimidazolidinones (1), electron donating or withdrawing sub-stituents were introduced at 3 or 4-position and the analogs were tested against human lung (A549) and colon (HCT-15) cancer cell lines. Quantitative structure activity relation-ship of the 4-substituted series shows that only STERIMOL L values are well correlated. The increment of substituent's volume enhances the activity against both cell lines. The small substituent at 3-position additionally increases the activity. However naphthyl group in place of phenyl reduces the activity, Therefore the phenyl motif with sterically large substituent at 4-position and small substituent at 3-position may be important for their activity. Integration of these substituents' effects into the structural design led to discover the more potent analog, 4-phenyl-1-(N-acetylindoline-5-sulfonyl) imidazolidinone (1n).

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