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Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles
Department of Pharmaceutical Sciences, The Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, 34 Rainbow Drive, Hilo, HI 96720, USA
* Author to whom correspondence should be addressed.
Received: 3 April 2013; in revised form: 15 May 2013 / Accepted: 20 May 2013 / Published: 24 May 2013
Abstract: Macrocyclic scaffolds are commonly found in bioactive natural products and pharmaceutical molecules. So far, a large number of macrocyclic natural products have been isolated and synthesized. The construction of macrocycles is generally considered as a crucial and challenging step in the synthesis of macrocyclic natural products. Over the last several decades, numerous efforts have been undertaken toward the synthesis of complex naturally occurring macrocycles and great progresses have been made to advance the field of total synthesis. The commonly used synthetic methodologies toward macrocyclization include macrolactonization, macrolactamization, transition metal-catalyzed cross coupling, ring-closing metathesis, and click reaction, among others. Selected recent examples of macrocyclic synthesis of natural products and druglike macrocycles with significant biological relevance are highlighted in each class. The primary goal of this review is to summarize currently used macrocyclic drugs, highlight the therapeutic potential of this underexplored drug class and outline the general synthetic methodologies for the synthesis of macrocycles.
Keywords: macrocycles; macrocyclization; macrocyclic drugs; natural products; retrosynthesis; methodology; macrolactonization; macrolactamization; transition-metal catalyzed cross coupling; ring-closing metathesis; click chemistry
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Cite This Article
MDPI and ACS Style
Yu, X.; Sun, D. Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles. Molecules 2013, 18, 6230-6268.
Yu X, Sun D. Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles. Molecules. 2013; 18(6):6230-6268.
Yu, Xufen; Sun, Dianqing. 2013. "Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles." Molecules 18, no. 6: 6230-6268.