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Epi-xanthatin의 Side Chain 변환을 통한 새로운 반합성 유도체들의 합성 및 세포독성
백두종(Du-Jong Bae),안종웅(Jong-Woong Ahn),이정옥(Chongock Lee) 大韓藥學會 2005 약학회지 Vol.49 No.1
Epi-xanthatin analogs containing hydrophilic substituents such as carboxylic acid, alcohol, morpholine, amino acid, and glucose derivatives were synthesized and their in vitro cytotoxicity and in vitro antitumor activity were evaluated. The target compounds were generally cytotoxic against tumor cell lines of human origin with ED so values of 0.1-30㎍/ml, except the highly hydrophilic analog 6 containing aspartic acid. Contrary to the potent cytotoxicity, weakly hydrophilic analogs 2 and 8 were not active in vivo, or even toxic to the test animals. As a result, hydrophilic analog of epi-xanthatin did not show in vitro cytotoxicity and hydrophobic analogs did not show in vivo antitumor activity thus it is presumed that amphiphilic analogs or those with medium hydrophilicity would exhibit the antitumor potency in vivo.