|
Type |
Poster Presentation |
Area |
Organic Chemistry |
Room No. |
Event Hall |
Time |
4월 19일 (목요일) 11:00~12:30 |
Code |
ORGN.P-568 |
Subject |
Synthesis and Anticancer Evaluation of Aminated 7-Azaindoles via Rh(III)-Catalyzed C−H Amination |
Authors |
Jihye Park, IN SU KIM1,* Department of Pharmacy, Sungkyunkwan University, Korea 1College of Pharmacy / Department of Pharmacy, Sungkyunkwan University, Korea |
Abstract |
The site-selective C–H amination reaction of 7-azaindoles with various benzisoxazoles as amination surrogates under cationic rhodium(III) catalysis is described. This transformation efficiently provides a range of ortho-aminated N-aryl-7-azaindoles with excellent siteselectivity and functional group compatibility. The formed ortho-aminated 7-azaindoles were readily transformed into biologically relevant heterocycles such as azaindoloacridine, azaindoloacridone, and bis-indole compounds. Moreover, the synthetic derivatives were tested for in vitro anticancer activity against human breast adenocarcinoma cells (MCF-7), human renal carcinoma cells (786-O), and human prostate adenocarcinoma cells (DU145). Notably, some synthetic compounds were found to display most potent anticancer activity, compared to that of anticancer doxorubicin as a positive control. we herein report the Rh(III)-catalyzed direct amination of 7-azaindoles with anthranils affording ortho-aminated azaindole derivatives as biologically interesting heterocycles. |
E-mail |
qkr3548@naver.com |
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