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Synthesis of Benzo[c]phenanthridine Derivatives and their in Vitro Antitumor Activities
Cho, Won-Jea,Yoo, Su-Jeong,Chung, Byung-Ho,Choi, Bo-Gil,Cheon, Seung-Hoon,Whang, Soon-Ho,Kim, Sin-Kyu,Kang, Boo-Hyon,Lee, Chong-Ock The Pharmaceutical Society of Korea 1996 Archives of Pharmacal Research Vol.19 No.4
Aiming at the development of anticancer agents by modification of phenolic benzo[c]phenanthridine alkaloid, additional hydroxyl group was put on C10 position of fagaridine (1) by a biomimetic synthetic procedure to afford 10-hydroxyfagaridine (12). All of the synthetic intermediates were also screened in vitro antitumor activities against five different cell lines as well as 12. Among them the representative cytotoxic results are shown as follows; P-quinone (11) $[ED_50;(A549=0.22; {\mu}g/ml)$, $(HCT;15=0.21 {\mu}g/ml)$, fagaridine (1) $(HCT;15=0.41 {\mu}g/ml)$, olefin (6) $(HCT; 15=0.06 {\mu}g/ml)$, acetal (7) $(SKMEL-2=0.07 {\mu}g/ml)$, dihydrofagaridne (10) $(A549=0.38 {\mu}g/ml)$, 10-hydroxyfagaridine (12) $(A 549=0.45{\mu}g/mi)$. From these observation three main remarks can be drawn; (i) the iminium part of benzo[c]phenanthridine is not essential for showing acitvities, (ii) the additional hydroxyl group did not contribute to enhance the cytotoxicity, (iii) the 3-arylisoquinolin-1(2H)-one derivatives were found to display significant in vitro antitumor activity.
Cho, Won Jea,Kim, Eui Ki,Park, Myun Ji,Choi, Sang Un,Lee, Chong Ock,Cheon, Seung Hoon,Choi, Bo Gil,Chung, Byung Ho 전남대학교 약품개발연구소 1998 약품개발연구지 Vol.7 No.1
In this study a series of 3-arylisoquinoline derivatives were synthesized and cytotoxicity against human melanoma tumor cell evaluated, and a three dimensional quantitative structure-activity relationship was investigated using the comparative molecular field analysis (CoMFA). The results suggested that the electrostatic, steric and hydrophobic factors of 3-arylisoquinolines were strongly correlated with the antitumor activity. Considerable predictive ability (cross-validated r² as high as 0.721) was obtained through CoMFA.
Synthesis of Antineoplaston A10 Analogs as Potential Antitumor Agents
Choi, Bo-Gil,Kim, Ok-Young,Chung, Byung-Ho,Cho, Won-Jea,Cheon, Seung-Hoon,Choi, Sang-Un,Lee, Chong-Ock The Pharmaceutical Society of Korea 1998 Archives of Pharmacal Research Vol.21 No.2
Several aniline mustard analogues were obtained by introducing N,N-bis(2-chloroethyl)amino moiety to phenyl ring of A10 analogues in order to increase reactivity of A10 analogs and selectivity into DNA. The in vitro antitumor activity of synthesized compounds was evaluated using five different solid tumor cell lines by SRB method. Aniline mustard analogues exhibited more potent antitumor activity than A10 analogs. Especially, m-aniline mustard of benzoyl analogue displayed remarkable antitumor activity.
항암제 안티네오플라스톤 A10의 동족체합성 및 항암 활성
최보길(Bo Gil Choi),서희경(Hee Kyoung Seo),김옥영(Ok Young Kim),정병호(Bung Ho Chung),오인준(In Jun Oh),조원제(Won Jea Cho),천승훈(Seung Hoon Cheon),박민수(Min Soo Park),최상운(Sang Un Choi),이정옥(Chong Ock Lee) 대한약학회 1997 약학회지 Vol.41 No.3
Some analogs and their Mannich bases of Antineoplaston A10 (A10) were synthesized. Chemical yield for the 2-(or 3-)thienyl, benzol, and phenylpropionyl analogs were high but 1-naphthyl analog was synthesized in low yield. the Mannich bases formation of these analogs with morpholine went verywell compared to other bases. 1-Naphthyl, 4-nitrobenzoyl, and phenylpropionyl analogs of A10 showed weak in vitro activity but the other A10 analogs showed weaker or no activity at 10-1000mcg/ml. But their Mannich bases containing A10analogs showed good in vitro activity compared to simple A10 analogs.
Synthesis of Antineoplaston A10 Analogs as Potential Antitumor Agents
Choi, Bo Gil,Kim, Ok Young,Chung, Byung Ho,Cho, Won Jea,Cheon, Seung Hoon,Choi, Sang Un,Lee, Chong Ock 전남대학교 약품개발연구소 1998 약품개발연구지 Vol.7 No.1
Several aniline mustard analogues were obtained by introducing N,N-bis(2-chloroethyl)amino moiety to phenyl ring of A10 analogues in order to increase reactivity of A10 analogs and selectivity into DNA. The in vitro antitumor activity of synthesized compounds was evaluated using five different solid tumor cell lines by SRB method. Aniline mustard analogues exhibited more potent antitumor activity than A10 analogs. Especially, m-aniline mustard of benzoyl analogue displayed remarkable antitumor activity.
항암제 안티네오플라스톤 A10 의 동족체합성 및 항암 활성
최보길,서희경,김옥영,정병호,오인준,조원제,천승훈,박민수,최상운,이정옥 전남대학교 약품개발연구소 1997 약품개발연구지 Vol.6 No.1
Some analogs and their Mannish bases of Antineoplaston A10 (A10) were synthesized Chemical yield for the 2-(or 3-)thienyl, benzoyl, and phenylproptonyl analogs were hight but 1-naphthyl analog was synthesized in low yield. The Mannish bases formation of these analogs with morpholine went very well compared to other bases. 1-Naphthyl, 4-nitrobenzoyl. and phenylpropiortyl analogs of A10 showed weak in vitro activity but the other A10 analogs shaved weaker or no activity at 10-1000 ㎍/㎖. But their Mannish bases containing A10 analogs showed good in vitro activity compared to simple A10 analogs.
이민욱(Minuk Lee),박성재(Soung-Jea Park),여태경(Tae-Kyeong Yeu),김형우(Hyong-Woo Kim),홍섭(Sup Hong),조수길(Su-gil Cho),장준용(Jun-yong Jang),이태희(Tae Hee Lee),최종수(Jong-Su Choi) 대한기계학회 2012 大韓機械學會論文集A Vol.36 No.12
심해저 장비에 사용되는 압력용기는 내장된 전자장비를 대기압 상태로 보호할 수 있도록 설계되어야 한다. 따라서 해수에 노출되지 않도록 수밀성과 심해의 높은 압력을 견딜 수 있는 구조적 안전성을 확보해야 한다. 본 연구의 압력용기는 원통형이며, 중앙부의 원통형 용기와 양 끝단의 평판형 덮개부로 이루어져있다. 일반적으로 압력용기 내부 전자장비와의 통신 및 전력전송을 위해 압력용기 덮개판에 다양한 수중 커넥터를 배치 한다. 그러나 한정된 덮개판 공간에 다수의 홀이 배치되면 응력집중을 유발하여 압력용기 덮개판의 구조적 안전성에 영향을 줄 수 있다. 본 논문에서는 구조적 안전성을 고려한 압력용기 덮개판의 홀 배치 최적화 기법에 대한 연구를 수행하였다. A deep-sea pressure vessel needs to protect the internal electrical equipment from the high external pressure. Thus, the pressure vessel should be designed to be watertight and structurally safe. In this study, a cylindrical-type pressure vessel comprising a hollow cylinder and cover plates at both ends is investigated. For communication between the internal electronic equipment and the external device, holes are bored on the cover plate to install underwater connectors. Considering the type of internal equipment and underwater connector specifications, multiple holes may be required. These holes can affect the structural safety of the pressure vessel cover plate. In this study, the optimum design of the hole arrangement in consideration of the structural safety of the cover plate was performed.
Development of grid-based hydraulc model for ecohydraulic connectivity assessment
Kim Chang Wan,Chegal Sun Dong,Cho Gil Jea 한국수자원학회 2018 한국수자원학회논문집 Vol.51 No.5
지금까지 추진해 오던 제외지 중심의 하천복원에서 벗어나 최근에는 제내지까지 복원하고자 하는 노력이 시도되고 있다. 이의 일환으로 구하도의 복원이 추진되고 있으나 이로 인한 수리적 연결성 및 생태적 연결성 향상을 정량적으로 평가할 적합한 모형의 개발은 미진한 상태이다. 본 연구에서는 구하도 복원을 통한 생태적 연결성 회복을 평가할 수 있는 격자기반의 수리해석 모형을 개발하였다. 본 모형의 적용성을 검토하기 위하여 노탑리 일원의 청미천 하천복원 사업지를 대상으로 수리생태적 연결성을 평가하였다. 본 모형으로 수리 및 생태적 특성의 시 ․ 공간적 분포를 신속하고 간단하게 해석할 수 있었으며 향후 수리적 생태적 연결성을 평가하는 적절한 도구로 활용될 수 있을 것으로 판단된다. Beyond river restoration focused on the inside region of main streams up to now, the river restoration including the outside region of streams has been started recently. As a part of this attempt, the restoration of abandoned rivers has been tried, but the development of a suitable model to quantitatively assess the improvement of hydraulic and ecological connectivity is not still satisfying. In this study, a grid - based hydraulic analysis model to evaluate the recovery of ecological connectivity through the restoration of abandoned rivers has been developed. In order to examine the applicability of this model, the ecohydaulic connectivity of the Cheongmi River Project area in Notap region was evaluated. This model can promptly and simply analyze the temporal and spatial distribution of the hydraulic and ecological characteristics, and it can be used as a appropriate tool to assess the hydraulic and ecological connectivity in the future.