• Bulletin of the Korean Chemical Society
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• v.33 no.1
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• pp.111-114
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• 2012

Androgen receptor (AR) is ligand-inducible nuclear hormone receptor which has been focused on key molecular target in growth and progression of prostate cancer. We synthesized a series of 4-aryl 2-substituted aniline-thiazole analogs and evaluated their anti-cancer activity in AR-dependent human prostate cancer LNCap cells. Among them, the compound 6 inhibited the tumor growth in LNCap-inoculated xenograft model.

• Archives of Pharmacal Research
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• v.17 no.6
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• pp.411-414
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• 1994

Phenylazocyanothioacetamide 1 reacts with malononitrile to afford the pyridinethione 4 which reacts with phenacylbromide to yield the pyridine-S-phenacyl derivative 6, 1 reacts with ethyl cyanoacetate to yield the pyridazine derivative, 8, and with phenacyl bromide to afford the N-phenacyl derivative 11, instead of the thiazole 10. Compound 11 afforded the pyrazolopyridine 13 on reaction with malononitrile while 10 was obtained on coupling of the thiazole 14 with diazotised aniline. Compound 10 reacts with malononitrile to afford the thizaolyl pyridazine 15. Compound 1 reacts with malononitrile dimer to afford the pyriodopyridazine derivative 17a. 1 reacts also with active methylene heterocycies to afford the pyrazolo and thiazolo-fused phridazines 20 and 23 respectively.

• Journal of the Korean Chemical Society
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• v.57 no.1
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• pp.94-98
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• 2013

A new family of thiazole heterocycles, namely [4-(1H-benzoimidazol-2-yl)-thiazol-2-yl]-benzylidene-amines has been synthesized by the condensation of 4-(1H-Benzoimidazol-2-yl)-thiazol-2-ylamine with various aromatic aldehydes and N-[4-(1H-benzoimidazol-2-yl)-thiazol-2-yl]-N'-benzylidene-hydrazines through the cyclization of 1-(1H-benzoimidazol-2-yl)-2-bromo-ethanone with arylthiosemicarbazones. The target compounds are achieved by using 1-(1H-Benzoimidazol-2-yl)-ethanone as starting material. The chemical structures of all newly synthesized compounds were confirmed by their IR, $^1H$ NMR and Mass spectral data. Further the compounds were used to evaluate their antimicrobial activity and found that the appreciable antimicrobial activity by some of the title compounds.

• Journal of the Korean Chemical Society
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• v.34 no.1
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• pp.102-107
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• 1990

The reaction of thiazoline-azetidinone (7) with $I_2$ in $CH_2Cl_2-H_2O$ gave directly 3-iodo-3-methylcepham (4). A phase transfer catalyst considerably increased the reaction rate. Similar to the hydrolysis of thiazoline-azetidinone (7) under a weak acidic condition, thiazole (10) was given as major product in the treatment with 0.1 eq. of iodine. The difference between cyclization reaction and hydrolysis could be explained in terms of solvents, the amount of iodine and the nature of thiazoline-azetidinones (7).

• Archives of Pharmacal Research
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• v.13 no.3
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• pp.261-264
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• 1990

4-Arylazo-3-phenyl-5-aminopyrazoles (5a, b) and substituted hydroxythiazoles 8a, b were synthesized from the reaction of 4a, b with hydrazine hydrate and mercaptoacetic acid respectively. Compounds 5a, b and 8a, b were also obtained from coupling of 2a, b with 6 and 7, respectively. 4H-1, 4-Benzothiazine 11 was prepared from 1 and 10. The resaction of the diazonium salts 2a-c with diethyl 3-amino-2-cyanopenet-2-en-1, 5-dicarboxylate 12 was also reported.

• Polymer(Korea)
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• v.36 no.2
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• pp.235-244
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• 2012

A thiazole type accelerator MBT (2-mercapto benzothiazole) was added into silica filled natural rubber (NR) compound with various concentrations (0, 1, 2, 3, 4 phr). The effects of MBT on the cure rate, mechanical property, degree of rubber-filler interaction (${\alpha}_F$), crosslinking density, and viscoelastic property ($tan{\delta}$) were investigated. As accelerator concentration increased, the $t_{s2}$ and $t_{90}$ decreased and the crosslinking density and modulus at 300% elongation increased. The tensile strength and elongation increased up to 3 phr and no further increased at 4 phr. The $tan{\delta}$ value measured at room temperature was higher than that of the $70^{\circ}C$. The ${\alpha}_F$ value was not affected by the addition of MBT. The mechanisms for the vulcanization rate were reviewed.

• Applied Chemistry for Engineering
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• v.22 no.4
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• pp.411-415
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• 2011

Various types of accelerators, thiuram (TMTD, DPTT), thiazole (MBT, MBTS), and sulfenamide (CBS, NOBS) are added into a silica filled natural rubber compound. Their effects on vulcanization and mechanical properties are investigated. TMTD showed the fastest vulcanization rate, the higer maximum torque ($T_{max}$), and the excellent mechanical properties (300% modulus, tensile strength, elongation). MBT and MBTS showed an intermediate vulcanization rate between thiuram and sulfenamide type and added ones, and also showed the lower $T_{max}$ and mechanical properties compared to that of other compounds. Finally, NOBS showed the slowest vulcanization rate and the lower mechanical property but the moderate $T_{max}$.

• The Korean Journal of Food And Nutrition
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• v.17 no.3
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• pp.313-321
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• 2004

Separation-concentration of sulfur containing heterocyclic compounds(SCHC) from many reaction meat flavors manufactured with Maillard reaction was carried out. Profile of SCHC was identified and analyzed by GC and GC-MSD. The results were as follows. 1. Profile of SCHC could be identified 7 kinds thiazole and 11 kinds thiophene, the major produced compounds were thiophene, thiazolidine, 4-methyl-5-thiazole ethanol. 2. In the case of SCHC, relationship between changes of reaction conditions and the kind of produced components were as same, but produced amounts appeared the difference. Producing amount of complexed SCHC and caramellike note as well as oxygen containing heterocyclic compounds were high level more than high reaction temperature and long time reaction period. 3. Producing ratio of comparative simple structural SCHC were the highest level at reaction conditions of moisture content 50%, reaction temperature 100$^{\circ}C$ and reaction time 2 hours. Reaction conditions for the revelation of reaction meat flavor were below 110$^{\circ}C$ and less than 2 hours. 4. Relationship between moisture content and reaction temperature as well as reaction time had very relative relation. From the change of moisture content and reaction conditions could be obtained the simultaneously profile. Signal presentation for production of reaction meat flavor could be from extraction-separation-concentration of SCHC through simplification of raw-materials in the flavor and seasoning food industry.

• Bulletin of the Korean Chemical Society
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• v.28 no.12
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• pp.2511-2513
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• 2007

• Journal of Integrative Natural Science
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• v.8 no.4
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• pp.258-266
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• 2015

Xanthine Oxidase is an enzyme, which oxidizes hypoxanthine to xanthine, and xanthine to uric acid. It is widely distributed throughout various organs including the liver, gut, lung, kidney, heart, brain and plasma. It is involved in gout pathogenesis. In this study, we have performed Comparative Molecular Field Analysis (CoMFA) on a series of 2-(indol-5-yl) thiazole derivatives as xanthine oxidase (XO) inhibitors to identify the structural variations with their inhibitory activities. Ligand based CoMFA models were generated based on atom-by-atom matching alignment. In atom-by-atom matching, the bioactive conformation of highly active molecule 11 was generated using systematic search. Compounds were aligned using the bioactive conformation and it is used for model generation. Different CoMFA models were generated using different alignments and the best model yielded a cross-validated $q^2$ of 0.698 with five components and non-cross-validated correlation coefficient ($r^2$) of 0.992 with Fisher value as 236.431, and an estimated standard error of 0.068. The predictive ability of the best CoMFA models was found to be $r^2_{pred}$0.653. The CoMFA study revealed that the $R_3$ position of the structure is important in influencing the biological activity of the inhibitors. Electro positive groups and bulkier substituents in this position enhance the biological activity.