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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.
Numerical Simulation on Disproportionate Collapse of the Tall Glulam Building under Fire Conditions
Zhao, Xuan,Zhang, Binsheng,Kilpatrick, Tony,Sanderson, Iain Council on Tall Building and Urban Habitat Korea 2021 International journal of high-rise buildings Vol.10 No.4
Perception of the public to structural fires is very important because there are only a number of tall timber buildings constructed in the world. People are hesitating to accept tall timber buildings, so it is essential to ensure the first generation of tall timber buildings to a very high standard, especially fire safety. Right now, there are no specific design standards or regulations for fire design of tall timber buildings in Europe. Even though heavy timber members have better fire resistance than steel components, many conditions still need to be verified before considering the use of timber materials, e.g. fire spread, post-fire collapse, etc. This research numerically explores the structural behaviours of a tall Glulam building when one of its internal Glulam (Glued laminated timber) columns fails after sustaining a full 120-min standard fire and is removed from the established finite element building model created in SAP2000. The numerical results demonstrate that the failure and removal of the selected internal Glulam column may lead to the local failure of the adjacent CLT (Cross laminated timber) floor slabs, but will not lead to large disproportionate damage and collapse of the whole building. Here, the building is assumed to be located in Glasgow, Scotland, UK.
Xuan, Zhu,Zhong, Zhao-Hui,Zhang, Xuan-Zhi,Zhang, Lei,Zhao, Xiao-Kun,Lv, Chen,Xu, Ran,Ren, Wei-Gang,Li, Song-Chao Asian Pacific Journal of Cancer Prevention 2012 Asian Pacific journal of cancer prevention Vol.13 No.3
To determine the relationship between comorbidity and outcome after radical cystectomy in Chinese patients by using the Adult Comorbidity Evaluation (ACE)-27 index. Two-hundred-and-forty-six patients treated with radical cystectomy at the Second Xiangya Hospital of Central South University, Hunan Province, China between 2000 and 2010 were retrospectively analyzed. Medical records were reviewed for age, gender, delayed time of radical cystectomy, urinary diversion type, pelvic lymphadenectomy status, TNM stage, and pathological grade. Comorbidity information was assessed by the ACE-27 index. The outcome measurement was overall survival. Univariate and multivariate Cox proportional hazards regression analyses were used to determine the association between comorbidity and outcome. The study population consisted of 215 (87.40%) males and 31 (12.60%) females with a mean age of $62{\pm}11$ years. Median duration of follow-up was $47{\pm}31$ months. A total of 151 (61.38%) patents died during follow-up. Of those, 118 (47.97%) had at least one comorbidity. According to the ACE-27 scores, 128 (52.03%) patients had no comorbidity, 79 (32.11%) had mild, 33 (13.41%) had moderate, and 6 (2.45%) had severe comorbidities. Multivariate analysis indicated that moderate (p=0.002) and severe (p<0.001) comorbidity was significantly associated with decreased overall survival. In addition, age ${\geq}70$ years (p=0.002), delayed time of radical cystectomy >12 weeks (p=0.044), pelvic lymphadenectomy status (p=0.014), and TNM stage >T3 (p<0.001) were determined to be independent risk factors of overall survival. Increasing severity of comorbidity statistically correlated with decreased overall survival after radical cystectomy.
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.
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).
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, 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.
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.