• Archives of Pharmacal Research
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• v.27 no.9
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• pp.893-900
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• 2004

2- or 6-Substituted BZT-N derivatives were synthesized, and their cytotoxic activity against can-cer L1210 and SNU-1 cells was examined. The antitumor action was also assessed in mice bearing S-180 cells in peritoneal cavity. In a comparison, it was found that 6-substituted BZT-N derivatives exhibited higher potencies in both bioactivities than 2-substituted BZT-N derivatives against L1210 cells in in vitro and S-180 in vitro tests exception of compound 36. Interestingly, it was observed that 2-substituted compound 36, which has methyl group at RI position, exhib-ited a better antitumor activity than 6-substituted compounds against L1210 and SNU-1 in vitro. The EDso value of 2-substituted compound 36 against L1210 was found to be comparable to the EDso value of adriamycin and was even better against the solid cancer cell line SNU-1. It was also observed that 2-substituted compound 36 showed better antitumor activity in mice bearing S-180 cells in the peritoneal cavity. The T/C (％) value of 2-substituted compound 36 was simi-lar to that of adriamycin. Quantitative structure-activity relationship (QSAR) tests reveal that the experimental E $D_{50}$ values against SNU-1 closely correlate with both the calculated HOMO ener-gies ( $E_{HOMO}$) and the measured H-NMR chemical shift of 3-H ($\delta$$_{H}$). The results suggests that a compound having higher $E_{HOMO}$ and $\delta$$_{H}$ values usually should have a lower E $D_{50}$ (SNU-1) value.lue.lue.lue.

• Bulletin of the Korean Chemical Society
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• v.34 no.8
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• pp.2455-2460
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• 2013

Second-order rate constants ($k_N$) have been measured spectrophotometrically for the nucleophilic displacement reactions of 4-nitrophenyl X-substituted-cinnamates (4a-4e) and Y-substituted-phenyl cinnamates (5a-5e) with Z-substituted-phenoxide anions in 80 mol % $H_2O$/20 mol % DMSO at $25.0{\pm}0.1^{\circ}C$. The Hammett plot for the reactions of 4a-4e with 4-chlorophenoxide (4-$ClPhO^-$) consists of two intersecting straight lines, which might be taken as a change in the rate-determining step (RDS). However, it has been concluded that the nonlinear Hammett plot is not due to a change in the RDS but is caused by stabilization of the ground state of substrates possessing an electron-withdrawing group in the cinnamoyl moiety through resonance interactions, since the Yukawa-Tsuno plot exhibits an excellent linear correlation with ${\rho}X=0.89$ and r = 0.58. The Br${\o}$nsted-type plot for the reactions of 4-nitrophenyl cinnamate (4c) with Z-substituted-phenoxides is linear with ${\beta}_{nuc}=0.76$. The Br${\o}$nsted-type plot for the reactions of Y-substituted-phenyl cinnamates (5a-5d) with 4-chlorophenoxides (4-$ClPhO^-$) is also linear with ${\beta}_{lg}=-0.72$. The Hammett plot correlated with ${\sigma}^-$ constants for the reactions of 5a-5d results in a much better linear correlation than that correlated with ${\sigma}^o$ constants, indicating that a partial negative charge develops on the O atom of the leaving aryloxide. Thus, the reactions have been concluded to proceed through a concerted mechanism.

• YAKHAK HOEJI
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• v.35 no.4
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• pp.258-263
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• 1991

Seven drivatives of 2, 3-alkyl substituted aziridinecarboximidates were prepared from alkyl substituted alkene and cyanamide. Their ED$_{50}$ values against L$_{1210}$ cell in vitro were evaluated as 1.5 to 4 $\mu\textrm{g}$/ml.

• Journal of the Korean Ceramic Society
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• v.34 no.12
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• pp.1261-1267
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• 1997

Four kids of powder admixtures(A, B, C, D) based on anhydrite were manufactured by mixing at a fixed rate of II-anhydrite, fly ash and active silica as an industrial by-product. Fluidity properties of cement paste such as mini-slump, apparent viscosity with elapsed time, as well as setting time of cement pastes of these admixtures substituted up to 11wt% of cement were compared to those of cement paste(SS) substisuted by marketed high-strength powder admixture(S). Among these powder admixtures, the fluidity of cement pastes(PA, PC) substituted by A and C powder admixtures manufactured from II-anhydrite and fly ash had an excellent property than that of cement paste substituted by marketed powder admixture and also a good fluidity-retention effect with elapsed time by adding of superplasticizer. The setting time of cement paste substituted by powder admixtures based on anhydrite slightly retarded than that of cement paste substituted by marketed powder admixture.

• Journal of the Korean Chemical Society
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• v.25 no.4
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• pp.263-269
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• 1981

The substituted pyridinium salts of oxochloromolybdates(V) have been prepared characterized by visible and infrared spectra, and magnetic moments. The electrical conductance of aqueous solutions of substituted pyridinium salts have been measured over a range of concentrations. The results indicate that the complex anions are monomeric in the solid. The magnetic moments of the complexes are similar to the spin-only values. Substituted pyridines are present as pyridinium cation in solid state.

• Journal of Environmental Health Sciences
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• v.18 no.2
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• pp.92-101
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• 1992

Halogen substituted-phenol and analog phenol degrading strains were identified as Aeromonas, Moraxella, and Flavobacterium genus. Optimal degrading condition was generally 50~100 $\mu$M substituted-phenol as carbon source, $NH_4NO_3$ as nitrogen source, 30$\circ$C , and initial pH 7.2. $\rho$-Chlorophenol degrading strain of Aeromonas sp. C4 had biodegradability to the various substituted-phenols. Flavobacterium sp. M9 had substrate specificity to methyl substituted-function. Catechol was cleavaged by catechol 1, 2-dioxygenase in Aeromonas sp. C4, Moraxella sp. N7, and Flavobacterium sp. M9.

• Journal of Environmental Health Sciences
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• v.7 no.2
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• pp.113-117
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• 1981

Twelve benzothiazolyl and 6-substituted benzothiazoly phenyl and chlorophenyl ureas have been newly synthesized by reacting 2-amino benzothiazole and 2-amino-6-substituted benzothazole with three or four phenyl and chlorophenyl isocyanate, respectively. The structures of these compounds were determined by measurement of the molecular weights and elementary analysis as well as IR spectrophotometry. The compounds generally exhibited antibacterial activity against Staphylococcus aureus and Escherichia coli in the concentration of $50\mu g/ml$. The compounds containing chloro group exhibited stronger antibacterial activity than those containing methyl group against Eschichia coli. The difference in the antibacterial activity according to the substituted group (phenyl, o-, m-, and p-chlorophenyl) was also noted. The compounds containing o-chlorophenyl group, on the whole, exhibited more potent growth-inhibitory activity againsts staphylococcus aureus.

• Journal of the Korean Applied Science and Technology
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• v.11 no.2
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• pp.105-111
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• 1994

Intermediates, 1-benzyl-2-substituted-3-carboxaldehyde[I]-[II], were prepared by the reaction of 2-substituted indole-3-carboxaldehyde with benzyl chloride. Indolylacrylophenone derivatives[III]-[X] were prepared from 1-benzyl-2-substituted-3-carboxaldehyde with acetophenone derivatives. They are as follows; 3-(1'-benzylindole-3'-yl)-1acrylophenone [III] 3-(1'-benzylindole-3-yl)-1(p-methoxy)acrylophenone [IV] 3-(1'-benzylindole-3-yl)-1(p-bromo)acrylophenone [V] 3-(1'-benzylindole-3-yl)-1(p-chloro)acrylophenone [VI] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-acrylophenone [VII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-methoxy)acrylophenone [VIII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-bromo)acrylophenone [VIII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-chloro)acrylophenone [X]

• Bulletin of the Korean Chemical Society
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• v.33 no.1
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• pp.128-136
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• 2012

We report the solid-phase library construction of 222 number of a novel N-[alkyl sulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 1A and amine 1B derivatives. The polymer-bound N-[alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 9 and amine 10 derivatives were obtained by first diversity generation with various acid chlorides and alkyl halides. Further reactions on the resins 9 and 10 with substituted sulfonyl chlorides produced the desired N-[alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 1A and amine 1B analogues.

• Journal of the Korean Chemical Society
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• v.11 no.4
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• pp.170-172
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• 1967

2-Phenyl-5-substituted phenyltetrazole and 2-substituted phenyl-5-phenyltetrazole were prepared from the corresponding hydrazone and phenyl azide with 2-methoxyethanol and metallic sodium as reaction medium at 110~115 $^{\circ}C$. At this reaction condition, however, the preparation of 2-substituted phenyl-5-phenyltetrazoles with substituents of relatively high Hammett substituent constant was unsuccessful. Surprisingly it was found that the solvent molecule was exchanged with substituent during the reaction when tried to obtain 2-m-fluorophenyl-5-phenyltetrazole using benzaldehyde m-fluorophenylhydrazone as starting material. Also disscussed the effect of electronic nature of substituents on the formation of 2,5-diphenyltetrazole derivatives.