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ABSTRACT: For the development of safer anti-inflammatory agents, simple aromatic compounds containing propenone moiety were prepared and evaluated for their dual COX/5-LOX inhibitory activities. Among the 17 prepared compounds, most of the compounds exhibited considerable COX/5-LOX inhibitory activities. Especially compound C(15) showed the most significant dual COX/5-LOX inhibitory activity.
Bioorganic & Medicinal Chemistry Letters 06/2004; 14(10):2559-62. · 2.55 Impact Factor
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ABSTRACT: For the development of new anticonvulsive agents, analogs of gamma-vinyl GABA (vigabatrin) containing GABA, gamma-vinyl GABA, valproic acid, nipecotic acid or isonipecotic acid moieties were prepared and evaluated for their anticonvulsive activities. Most of the prepared compounds showed moderate anticonvulsive activities. Among them compounds 10 and 16 displayed the most potent anticonvulsive activity and a broader spectrum compared to vigabatrin.
Il Farmaco 06/2004; 59(5):381-8.
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Long-Xuan Zhao, Yoon-Soo Moon,
Arjun Basnet,
Eun-kyung Kim,
Yurngdong Jahng,
Jae Gyu Park,
Tae Cheon Jeong,
Won-Jea Cho,
Sang-Un Choi,
Chong Ock Lee,
Sun-Young Lee,
Chong-Soon Lee,
Eung-Seok Lee
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ABSTRACT: For the development of new anticancer agents, phenyl, 2-pyridyl, 2-furyl, 2-thienyl, 2-furylvinyl and 2-thienylvinyl substituted derivatives on 2,4,6-position in pyridine moiety were prepared and evaluated for their topoisomerase I inhibitory activity. Among the thirteen prepared compounds, four compounds exhibited strong topoisomerase I inhibitory activity. A structure-activity relationship study indicated that the 2-thienyl-4-furylpyridine skeleton was important for topoisomerase I inhibitory activity.
Bioorganic & Medicinal Chemistry Letters 04/2004; 14(5):1333-7. · 2.55 Impact Factor
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ABSTRACT: For the development of new anticonvulsive agents, GABAmimetics such as nipecotic acid, isonipecotic acid, gamma-aminobutyric acid (GABA), gamma-vinyl GABA (vigabatrin) and valproic acid were covalently coupled through an ester bond by a two-carbon linker chain as potential pro-drugs and evaluated for their anticonvulsive activities.
Archives of Pharmacal Research 11/2003; 26(10):785-95. · 1.59 Impact Factor
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ABSTRACT: Recently, we have reported that 2-bromopropane might have an immunotoxic potential in rats when exposed for 28 days. In the present studies, the possibility of 2i-deoxyguanosine adduct formation by 2-bromopropane was investigated in vitro to elucidate molecular mechanism of 2-bromopropane-induced immunosuppression. N7-Guanine adduct of 2'-bromopropane (i.e., N7-isopropyl guanine) was chemically synthesized and structurally characterized by analysis of UV, 1H-NMR, '3C-NMR, COSY and fast atom bombardment mass spectrometry to use as a reference material. Incubation of 2'-deoxyguanosine with an excess amount of 2-bromopropane in PBS buffer solution, pH 7.4, at 37 degrees C for 16 h, followed by a thermal hydrolysis, produced a detectable amount of N7-isopropyl guanine by an HPLC and UV analysis. The present results suggest that 2-bromopropane might form a DNA adduct in N7 position of 2'-deoxyguanosine at a physiological condition.
Archives of Pharmacal Research 03/2002; 25(1):39-44. · 1.59 Impact Factor
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ABSTRACT: Recently, we have reported that 2-bromopropane might have an immunotoxic potential in rats when exposed for 28 days. In the
present studies, the possibility of 2í-deoxyguanosine adduct formation by 2-bromopropane was investigatedin vitro to elucidate molecular mechanism of 2-bromopropane-induced immunosuppression.N7-Guanine adduct of 2′-bromopropane (i.e.,N7-isopropyl guanine) was chemically synthesized and structurally characterized by analysis of UV,1H-NMR,13C-NMR, COSY and fast atom bombardment mass spectrometry to use as a reference material. Incubation of 2′-deoxyguanosine with
an excess amount of 2-bromopropane in PBS buffer solution, pH 7.4, at 37°C for 16 h, followed by a thermal hydrolysis, produced
a detectable amount ofN7-isopropyl guanine by an HPLC and UV analysis. The present results suggest that 2-bromopropane might form a DNA adduct inN7 position of 2′-deoxyguanosine at a physiological condition.
Archives of Pharmacal Research 01/2002; 25(1):39-44. · 1.59 Impact Factor
