• Journal of the Korean Chemical Society
• /
• v.39 no.10
• /
• pp.834-836
• /
• 1995

• Journal of the Korean Chemical Society
• /
• v.42 no.2
• /
• pp.245-247
• /
• 1998

• Bulletin of the Korean Chemical Society
• /
• v.29 no.2
• /
• pp.357-362
• /
• 2008

A method for synthesizing o-carborane substituted tetrahydroisoquinolines containing a polar functional group such as sulfamide, sulfonic, or phosphoric acid on the nitrogen atom of the piperidine ring, starting from arylethylamine, N-(2-arylethyl)sulfamide, N-(2-arylethyl)sulfamic acid or 2-arylethylamidophosphate, is described. In vitro studies showed the desired compounds 10, 15, 19, and 25 synthesized accumulate to high levels in B-16 melanoma cells with low cytotoxicity.

• Bulletin of the Korean Chemical Society
• /
• v.31 no.10
• /
• pp.2854-2860
• /
• 2010

Synthesis of a new series of pyrimidinyl-imidazo[2,1-b]thiazole derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the pyrimidinyl ring side chain was investigated. The biological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with Sorafenib. Among all of these derivatives, the cyclic sulfamide derivatives IIIa, IIIb, and IIIe showed the most potent antiproliferative activity against A375 human melanoma cell line. The IC50 values of compounds IIIa,b were in nanomolar scale. In addition, compound IIIe ($IC_{50}=1.9\;{\mu}M$) also demonstrated more potent antiproliferative activity compared with Sorafenib ($IC_{50}=5.6\;{\mu}M$).

• Bulletin of the Korean Chemical Society
• /
• v.23 no.1
• /
• pp.167-169
• /
• 2002

• Bulletin of the Korean Chemical Society
• /
• v.24 no.1
• /
• pp.129-132
• /
• 2003

• Bulletin of the Korean Chemical Society
• /
• v.24 no.9
• /
• pp.1399-1402
• /
• 2003

• Proceedings of the Membrane Society of Korea Conference
• /
• 2004.05a
• /
• pp.121-123
• /
• 2004

Sulfonamide moiety, RNSO$_2$, has been studied as biologically active compounds such as antibacterials.$^1$ Bissulfonylimide group,-SO$_2$NHSO$_2$-, has been introduced to the side chain of Nafion$^{(R)}$ to be the base moiety for an acid doping.$^2$However, to the best of our knowledge, there has been no report on SULFAMIDE ACID(Scheme 1), one of the sulfonic acid derivatives.(omitted)d)

• YAKHAK HOEJI
• /
• v.35 no.5
• /
• pp.368-371
• /
• 1991

For the development of new antiulcer agents 5, 6-dihydroimidazo[2, 1-b]- thiazoles substituted at the 3-position are sythesized. Thus, the reaction of 3-chloromethyl-5, 6-dihydroimidazo[2, 1-b]thiazole(2) with thiourea and subsequently with 3-chloro-propionitrile gives 3-[3-[5, 6-dihydroimidazo[2, 1-b]thiazolyl]methylthio]propionitrile(4), which by partial alcoholysis with methanol is converted into methyl-3-[3-[5, 6-dihydro-imidazo[2, 1-b]thiazoyl]methylthio]propionimidate(5) . This compound(5) is treated finally with sulfamide or sulfonamides. 3-[3-[5, 6-dihydroimidazo[2, 1-b]thiazoyl]methylthiol-N$^{2}$-sulfamoyl-propionamidine(6) inhibited gastric acid secretion (45%) when administered intraduodenally (100 mg/kg) to pylorus-ligated rats.

• Archives of Pharmacal Research
• /
• v.26 no.6
• /
• pp.441-445
• /
• 2003

New sulfonated amino ribofuranans were synthesized to elucidate the relationship between structure and specific biological activities such as anti-HIV and blood anticoagulant activities. The synthesis was performed by sulfonation of copolymers having various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranosidic unit. The sulfonation with piperidine N-sulfonic acid produced the sulfonated amino ribofuranans in high yield. The anti-HIV activity of sulfonated 3-amino-3-deoxy-(1$\rightarrow5)-\alpha$-D-ribofuranan showed more potent by increasing the degree of sulfonation and the average molecular weights. This activity was almost equal to the activities of sulfonated ribofuranans and ribopyranans reported before in spite of low molecular weight. The blood anticoagulant activities was observed at 36-48 mg/units, more potent than standard dextran sulfonate, 22.7 mg/units. In addition, the blood anticoagulant activities of sulfamide-copolysaccharide consisting various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranan units were potentiated by increasing sulfonated amino-ribofuranan units from 13 to 21 mg/units.