structural necessity of indole c5-o-substitution of seco-duocarmycin analogs for their cytotoxic activity结构的必要性吲哚c5-o-substitution seco-duocarmycin类似物的细胞毒性的活动.pdfVIP

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structural necessity of indole c5-o-substitution of seco-duocarmycin analogs for their cytotoxic activity结构的必要性吲哚c5-o-substitution seco-duocarmycin类似物的细胞毒性的活动.pdf

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structural necessity of indole c5-o-substitution of seco-duocarmycin analogs for their cytotoxic activity结构的必要性吲哚c5-o-substitution seco-duocarmycin类似物的细胞毒性的活动

Molecules 2010, 15, 7971-7984; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Structural Necessity of Indole C5-O-Substitution of seco- Duocarmycin Analogs for Their Cytotoxic Activity Taeyoung Choi and Eunsook Ma * College of Pharmacy, Catholic University of Daegu, Hayang, 712-702, Korea * Author to whom correspondence should be addressed; E-Mail: masook@cu.ac.kr; Tel. +82-53-850-3621; Fax: +82-53-850-3602. Received: 28 September 2010; in revised form: 24 October 2010 / Accepted: 28 October 2010 / Published: 8 November 2010 Abstract: A series of racemic indole C5-O-substituted seco-cyclopropylindole (seco-CI) compounds 1-5 were prepared by coupling in the presence of EDCI of 1-(tert- butyloxycarbonyl)-3-(chloromethyl)indoline (seg-A) with 5-hydroxy-, 5-O-methylsulfonyl, 5-O-aminosulfonyl, 5-O-(N,N-dimethylaminosulfonyl)- and 5-O-benzyl-1H-indole-2- carboxylic acid as seg-B. Compounds 1-5 were tested for cytotoxic activity against four human cancer cell lines (COLO 205, SK-MEL-2, A549, and JEG-3) using a MTT assay. Compounds 2 and 3 with small sized sulfonyl substituents like 5-O-methylsulfonyl and 5- O-aminosulfonyl exhibit a similar level of activity as doxorubicin against all cell lines tested. Keywords: duocarmycin; Indole C5-O-substituted seco-CI; cytotoxicity; DNA minor groove alkylation 1. Introduction Duocarmycins (DUMs) A, B1, B2, C1, C2, D 1