synthetic approaches and biological activities of 4-hydroxycoumarin derivatives4-hydroxycoumarin衍生物的合成方法和生物活性.pdf

Molecules 2009, 14, 4790-4803; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Review Synthetic Approaches and Biological Activities of 4-Hydroxycoumarin Derivatives Jae-Chul Jung 1 and Oee-Sook Park 2,* 1 Ewha Global Challenge, BK21 and Medical Research Institute, School of Medicine, Ewha Womans University, Seoul 158–710, Korea; E-Mail: jcjung10@yahoo.co.kr (J.-C.J.) 2 Department of Chemistry, Institute for Basic Sciences, College of Natural Sciences, Chungbuk National University, Cheongju 361–763, Chungbuk, Korea * Author to whom correspondence should be addressed; E-Mail: ospark@cbnu.ac.kr. Received: 19 October 2009; in revised form: 16 November 2009 / Accepted: 18 November 2009 / Published: 23 November 2009 Abstract: The main purpose of this review is to summarize recent chemical syntheses and structural modifications of 4-hydroxycoumarin and its derivatives, of interest due to their characteristic conjugated molecular architecture and biological activities. Keywords: 4-hydroxycoumarin; anticoagulant; rodenticide; ring cyclization; tetralone; coupling reaction 1. Introduction 4-Hydroxycoumarins (2H-1-benzopyran-2-ones, Figure 1) have evoked a great deal of interest due to their biological properties and characteristic conjugated molecular architecture. Many of them display important pharmacological effects, including analgesic [1], anti-arthritis [2], anti-inflammatory [3], anti-pyretic [4], anti-bacterial [5], anti-viral [6], and anti-cancer [7] properties. 4-Hydroxy-