Synthesis of amino acid ester phosphordiamidate derivatives of chrysin

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Title:	Synthesis of amino acid ester phosphordiamidate derivatives of chrysin
Authors:	Chen Xiao-Lan(陳曉嵐) Zang Shou-Ren(張守仁) Qu Ling-Bo(屈凌波) Zhao Yu-Fen(趙玉芬) Bai Yu-Zhu(白玉柱) Nig Juan(寧娟)
Contributors:	Key Laboratory of Chemical Biology and organic Chemistry,Department of Chemistry Henan University of Technology,Henan Province Key Laboratory of Bioorganic Phosphours Chemistry&Chemical Biology,Ministry of Education,Department of Chemistry
Date:	2008-07
Issue Date:	2017-12-04 15:52:14 (UTC+8)
Abstract:	Chrysin, a widely distributed flavone in plants, was reported to have many biological activities including anticancer activity [1,2].5,7-OH of chrysin can be glycosylated in intestine and therefore poor absorption was resulted in. However the non-equivalent phenolic hydroxy groups are potential sites for phosphorylation, a modification that could lead to improved pharmacological properties. In the work described in this paper, novel amino acid ester phosphordiamiamidate derivatives of chrysin (lll) were designed and synthesized as potential pro-drugs to changes the physical and chemical properties of the parent molecule and enhance its bio-availability. Amino Acid Esters first reacted with bis-ß-chloroethyl dichlorophosphamide (l) to yield phosphonamidic chlorides (ll), and then the resulting compounds (ll) coupled with chrysin smoothly to afford corresponding target products (III) in high yields. All structures of the newly synthesized compounds were confirmed by ESI-MS, 1HNMR,13C NMR. The initial biological activitie screening tests will be carried out.
Relation:	第五屆海峽化學、生物及材料研討會，起迄日：2008/07/21-2008/07/22，地點：嘉南藥理科技大學
Appears in Collections:	[Pharmacy and Science] The 5rh Conference of Channel-bridge Chemistry, Biology and materal Science

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