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Synthesis, Cytotoxicity and Structure-Activity Relationship Study of Terpyridines
Zhao, Long-Xuan,Sherchan, Jyoti,Park, Jung-Ki,Jahng, Yurng-Dong,Jeong, Byeong-Seon,Jeong, Tae-Cheon,Lee, Chong-Soon,Lee, Eung-Seok The Pharmaceutical Society of Korea 2006 Archives of Pharmacal Research Vol.29 No.12
For the development of novel antitumor agents, we designed and synthesized terpyridines, and their biological activities were evaluated. Although most of the newly prepared terpyridines showed strong cytotoxicity against several human cancer cell lines, [2,2';6',2"]-terpyridine displayed the most significant cytotoxicity.
Zhao, Long-Xuan,Park, Hyeung-Geun,Jew, Sang-Sup,Lee, Mi-Kyeong,Kim, Young-Choong,Thapa, Pritam,Karki, Radha,Jahng, Yurng-Dong,Jeong, Byeong-Seon,Lee, Eung-Seok Korean Chemical Society 2007 Bulletin of the Korean Chemical Society Vol.28 No.6
For the development of novel hepatoprotective agents, C11, C28, C2,3,23 or C2,23,28 functional groups on asiatic acid were modified, and their hepatoprotective effects were evaluated. Most of the prepared compounds displayed potent hepatoprotective activities against CCl4- and galactosamine (GaIN)-induced hepatotoxicity. Especially, compounds 16 and 20 showed the most significant hepatoprotective effects against GaIN-induced hepatotoxicity (54.2% and 46.4% protection at 50 mM, respectively).
Design, Synthesis and Anticonvulsive Activities of Potential Prodrugs Linked by Two-carbon Chain
Zhao, Long-Xuan,Moon, Yoon-Soo,Basnet, Ar-Jun,Park, Jae-Gyu,Kim, Eun-kyung,Kim, Dae-Ok,Jeong, Tae-Cheon,Jahng, Yurng-Dong,Choi, Jong-Won,Lee, Eung-Seok The Pharmaceutical Society of Korea 2003 Archives of Pharmacal Research Vol.26 No.10
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 prodrugs and evaluated for their anticonvulsive activities.
Long-Xuan Zhao,박형근,주상섭,Mi Kyeong Lee,Young Choong Kim,Pritam Thapa,Radha Karki,장영동,정병선,이응석 대한화학회 2007 Bulletin of the Korean Chemical Society Vol.28 No.6
For the development of novel hepatoprotective agents, C11, C28, C2,3,23 or C2,23,28 functional groups on asiatic acid were modified, and their hepatoprotective effects were evaluated. Most of the prepared compounds displayed potent hepatoprotective activities against CCl4- and galactosamine (GaIN)-induced hepatotoxicity. Especially, compounds 16 and 20 showed the most significant hepatoprotective effects against GaIN-induced hepatotoxicity (54.2% and 46.4% protection at 50 mM, respectively).
Synthesis, Characterization and in Vitro Identification of $N^7-Guanine$ Adduct of 2-Bromopropane
Zhao, Long-Xuan,Kim, Eun-Kyung,Lim, Hyun-Tae,Moon, Yoon-Soo,Kim, Nam-Hee,Kim, Tae-Hyung,Choi, Heesung,Chae, Whigun,Jeong, Tae-Cheon,Lee, Eung-Seok The Pharmaceutical Society of Korea 2002 Archives of Pharmacal Research Vol.25 No.1
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 abduct formation by 2- bromopropane was investigated in vitro to elucidate molecular mechanism of 2-bromopropane-induced immunosuppression. $N^7-Guanine adduct$ of 2'-bromopropane (i.e., $N^7-isopropyl$ guanine) was chemically synthesized and structurally characterized by analysis of UV,$^1H-NMR,{\;}^{13}C-NMR$, 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 $37^{\circ}C$ for 16 h, followed by a thermal hydrolysis, produced a detectable amount of $N^7-isopropyl$ guanine by an HPLC and UV analysis. The present results suggest that 2-bromopropane might form a DNA adduct in $N^7-position$ of 2'-deoxyguanosine at 3 Physiological condition.
Zhao, Long-Xuan,Kim, Tae Sung,Ahn, Soo-Hyun,Kim, Tae-Hyung,Kim, Eun-Kyung,Cho, Won-Jea,Choi, Heesung,Lee, Chong-Soon,Kim, Jung-Ae,Jeong, Tae Cheon,Chang, Ching-Jer,Lee, Eung-Seok 전남대학교 약품개발연구소 2001 약품개발연구지 Vol.10 No.-
For the development of new anticancer agents, 2,2':6',2"-,2,2':6',3"-and 2,2':6',4"-terpyridine derivatives were designed and evaluated for their topoisomerase I inhibitory activity and antitumor cytotoxicity. Structure-activity relationship studies indicated that 2,2':6',2"-terpyridine derivatives were highly cytotoxic toward several human tumor cell lines, whereas 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives were potent topoisomerase I inhibitors.
Zhao, Long-Xuan,Kim, Tae Sung,Ahn, Soo-Hyun,Kim, Tae-Hyung,Kim, Eun-Kyung,Cho, Won-Jea,Choi, Heesung,Lee, Chong-Soon,Kim, Jung-Ae,Jeong, Tae Cheon,Chang, Ching-jer,Lee, Eung-Seok 영남대학교 약품개발연구소 2002 영남대학교 약품개발연구소 연구업적집 Vol.11 No.-
For the development of new anticancer agents. 2.2':6'.2"-, 2.2':6'3"??and 2.2':6'4"-terpyridine derivatives were designed and evaluated for their topoisomerase I inhibitory activity and antitumor cytotoxicity-Structuer-activity relationship studies indicated that 2.2':6'.2"-terpyridine derivatives were highly cytotoxic toward several human tumor cell lines, whereas 2.2':6'.3"- and 2.2':6'.4"-terpyridine derivatives were potent topoisomerase I inhibitors.
Synthesis, Cytotoxicity and Structure-Activity Relationship Study of Terpyridines
Long-Xuan Zhao,Jyoti Sherchan,Jung Ki Park,장영동,정병선,정태천,이종순,이응석 대한약학회 2006 Archives of Pharmacal Research Vol.29 No.12
For the development of novel antitumor agents, we designed and synthesized terpyridines, and their biological activities were evaluated. Although most of the newly prepared terpyridines showed strong cytotoxicity against several human cancer cell lines, [2,2';6',2'']-terpyridine displayed the most significant cytotoxicity.
Synthesis, Characterization and in Vitro Identification of N^7-Guanine Adduct of 2-Bromopropane
Zhao, Long-Xuan,Kim, Eun-Kyung,Lim, Hyun-Tae,Moon, Yoon-Soo,Kim, Nam-Hee,Kim, Tae-Hyung,Choi, Heesung,Chae, Whigun,Jeong, Tae Cheon,Lee, Eung-Seok 영남대학교 약품개발연구소 2002 영남대학교 약품개발연구소 연구업적집 Vol.11 No.-
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. N^7-Guanine adduct of 2'-bromopropane (i.e., N^7-isopropyl guanine) was chemically synthesized and structurally characlerized by analysis of UV, ^H-NMR, ^12C-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℃ for 16 h, followed by a thermal hydrolysis, produced a detectable amount of N^7-isopropyl guanine by an HPLC and UV analysis. The present results suggest that 2-bromopropane might form a DNA adduct in N^7 position of 2'-deoxyguanosine at a physiological condition.
연구논문 : 의약화학 ; 2,4,6-치환 피리딘 유도체의 합성, topoisomerase 1 억제능 및 구조-활성 관계 연구
조룡현 ( Long Xuan Zhao ),문윤수 ( Yoon Soo Moon ),알준바스넷 ( Arjun Basnet ),김은경 ( Eun Kyung Kim ),장영동 ( Yurng Dong Jahng ),박재규 ( Jae Gyu Park ),정태천 ( Tae Cheon Jeong ),조원제 ( Won Jea Cho ),최상운 ( Sang Un Choi ) 영남대학교 약품개발연구소 2004 영남대학교 약품개발연구소 연구업적집 Vol.14 No.-