2. Academic Validation
  3. Synthesis, biological evaluation and SAR analysis of O-alkylated analogs of quercetin for anticancer

Synthesis, biological evaluation and SAR analysis of O-alkylated analogs of quercetin for anticancer

  • Bioorg Med Chem Lett. 2014 Sep 15;24(18):4424-4427. doi: 10.1016/j.bmcl.2014.08.006.
Zhi-Hao Shi 1,  Nian-Guang Li 2,  Yu-Ping Tang 3,  Qian-Ping Shi 4,  Wei Zhang 4,  Peng-Xuan Zhang 4,  Ze-Xi Dong 4,  Wei Li 4,  Xu Zhang 4,  Hai-An Fu 5,  Jin-Ao Duan 6
Affiliations

Affiliations

  • 1 National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China; Department of Organic Chemistry, China Pharmaceutical University, Nanjing, Jiangsu 211198, China.
  • 2 National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China. Electronic address: linianguang@njutcm.edu.cn.
  • 3 National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China. Electronic address: yupingtang@njutcm.edu.cn.
  • 4 National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China.
  • 5 Department of Pharmacology, Emory University School of Medicine, Atlanta, GA 30322, United States.
  • 6 National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China. Electronic address: dja@njutcm.edu.cn.
PMID: 25139569 DOI: 10.1016/j.bmcl.2014.08.006
Abstract

O-Alkylated quercetin analogs were synthesized and their Anticancer activities were assessed by a high-throughout screening (HTS) method. The structure-activity relationships (SAR) showed that introduction of long alkyl chain such as propyl group at the C-3 OH position or short alkyl chain such as ethyl group at the C-4' OH position were very important for keeping inhibitory activities against the 16 Cancer cell lines. Furthermore, when the two n-butyl groups were introduced into the C-3, C-7 or C-4', C-7 positions, the Anticancer activity was enhanced.

Keywords

Alkylation; Anticancer; Quercetin; Structure–activity relationship.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z