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3-카바모일옥시메틸-1-아자안트라퀴논 유도체들의 합성 및 세포독성
이희순(Hee Soon Lee),최재영(Jae Young Choi),홍승수(Seoung Soo Hong),조정숙(Jung Sook Cho),김영호(Young Ho Kim) 대한약학회 1997 약학회지 Vol.41 No.6
In the course of developing novel antitumor intercalating agents, we synthesized 3- carbamoyloxymethyl-azaanthraquinones 6-12, incorporating the latent alkylating functionality. These compounds were designed to explore the effect of heteroatom incorporation into anthraquinone chromophore and the effect of the incorporation of the latent alkylating functionality. The derivatives were prepared by hetero Diels-Alder reaction as a key step followed by functionality of allylic methyl to the desired substituents. Growth inhibitory studies of the azaanthraquinones were conducted in vitro against human cancer cell lines (SNU-354: liver and MCF7: breast) and human epidermoid carcinoma cells that are sensitive (KB-3-1) and multidrug-resistant (KB-V-1). The derivatives were 10 to lOO-fold less potent than doxorubicin against sensitive cell lines. However, they were marginally cross-resistant with doxorubicin against KB-V-1.
4-카바모일옥시메틸-1-아자얀트라퀴논 유도체들의 합성 및 세포독성
이희순(Hee Soon Lee),이승일(Seung Il Lee),홍승수(Seoung Soo Hong),조정숙(Jung Sook Cho),김영호(Young Hoon Jung) 대한약학회 1998 약학회지 Vol.42 No.5
In the course of developing novel antitumor intercalating agents. We synthesized 4-carbamoyloxymethyl-l-azaanthraquinones 7-12, incorporating the latent alkylating functionality. These compounds were designed to explore the effect of substituent on the nitrogen of carbamate. The target compounds were prepared by hetero Diels-Alder reaction as a key step followed by functionalization of benzylic methyl to the desired substituents. Growth inhibitory studies of the azaanthraquinones were conducted in vitro against human cancer cell lines (SNU-354; liver and MCF7; breast) and human epidermoid carcinoma cells that are sensitive (KB-3-1) and multidrug-resistant (KB-V-1). The compounds were less potent than doxorubicin against sensitive cell lines. However, the most active compound 12 was not cross-resistant with doxorubicin against KB-V-1.
4-카바모일옥시메틸-1-아자안트라퀴논 유도체들의 합성 및 세포독성
이희순,이승일,홍승수,조정숙,김영호 충남대학교 약학대학 의약품개발연구소 1998 藥學論文集 Vol.14 No.-
In the course of developing novel antitumor intercalating agents, we synthesized 4-carbamoyloxymethyl-1-azaanthraquinones 7-12. incorporating the latent alkylating functionality. These compounds were designed to explore the effect of substituent on the nitrogen of carbamate. The target compounds were prepared by hetero Diels-Alder reaction as a key step followed by functionalization of benzylic methyl to the desired substituents. Growth inhibitory studies of the azaanthraquinones were conducted in vitro against human cancer cell lne (SNU-354: liver and MCF7: breast) and human epidermoid carcinoma cells that are sensitive (KB-3-1) and multidrug-resistant (KB-V-1). the compounds were less potent than doxorubicin against sensitive cell lines. However, the most active compound 12 was not cross-resisitant with doxorubicin against KB-V-1.
Isolation and Structures of Guaianolides from Carpesium macrocephalum
Kim, Mi-Ran,Kim, Chang-Soo,Hwang, Kyung-Hwa,Park, Il-Yeong,Hong, Seoung-Soo,Son, Jong-Keun,Moon, Dong-Cheul 영남대학교 약품개발연구소 2002 영남대학교 약품개발연구소 연구업적집 Vol.11 No.-
Two new guaianolides, 4α,10α-dihydrory-1β(H),5β(H)-guai-11(13)-en-8α,12-olide (2) and 4β,10β-dihydroxy-5α(H)-1,11(13)-guaidien-8α,12-olide (3), from Carpesium macrocephalum were isolated, and their structures were elucidated on the basis of spectroscopic studies.