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Synthesis and structure–activity relationships of novel benzoxaboroles as a new class of antimalarial agents

✍ Scribed by Yong-Kang Zhang; Jacob J. Plattner; Yvonne R. Freund; Eric E. Easom; Yasheen Zhou; Jiri Gut; Philip J. Rosenthal; David Waterson; Francisco-Javier Gamo; Inigo Angulo-Barturen; Min Ge; Zhiya Li; Lingchao Li; Yong Jian; Han Cui; Hailong Wang; Jian Yang


Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
801 KB
Volume
21
Category
Article
ISSN
0960-894X

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✦ Synopsis


A series of boron-containing benzoxaborole compounds was designed and synthesized for a structureactivity relationship investigation surrounding 7-(HOOCCH 2 CH 2 )-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (1) with the goal of discovering a new antimalarial treatment. Compound 1 demonstrates the best potency (IC 50 = 26 nM) against Plasmodium falciparum and has good drug-like properties, with low molecular weight (206.00), low ClogP (0.86) and high water solubility (750 lg/mL at pH 7).


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Synthesis and Structure-Activity Relatio
✍ Xueling Hou; Zemei Ge; Tingmin Wang; Wei Guo; Jun Wu; Jingrong Cui; Chingsan Lai 📂 Article 📅 2011 🏛 John Wiley and Sons 🌐 English ⚖ 490 KB 👁 2 views

## Abstract Based on a novel lead compound 4‐methylpiperazine‐1‐carbodithioic acid 3‐cyano‐3,3‐diphenylpropyl ester **1**, the systematic structural modification was carried out. All the synthesized compounds were evaluated for their __in‐vitro__ anticancer activities on four to six different cell