2. Academic Validation
  3. 2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent

2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent

  • Bioorg Med Chem Lett. 2017 Aug 1;27(15):3279-3283. doi: 10.1016/j.bmcl.2017.06.025.
Til Bahadur Thapa Magar 1,  Tara Man Kadayat 1,  Hwa-Jong Lee 2,  Seojeong Park 2,  Ganesh Bist 1,  Aarajana Shrestha 1,  Youngjoo Kwon 3,  Eung-Seok Lee 4
Affiliations

Affiliations

  • 1 College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
  • 2 College of Pharmacy, Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea.
  • 3 College of Pharmacy, Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea. Electronic address: ykwon@ewha.ac.kr.
  • 4 College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea. Electronic address: eslee@ynu.ac.kr.
PMID: 28633898 DOI: 10.1016/j.bmcl.2017.06.025
Abstract

A new series of 2-chloropheny-substituted benzofuro[3,2-b]pyridines were designed, synthesized, and evaluated for Topoisomerase I and II inhibition and antiproliferative activity. Compounds 17-19, 23, 24, 26, and 27 exhibited excellent Topo II inhibitory activity. A systematic structure-activity relationship study revealed the important role of chlorine substitution in the strong Topoisomerase inhibitory activity.

Keywords

Antiproliferative activity; Benzofuro[3,2-b]pyridines; Chlorine-substituent; Heterocycles; Topoisomerase I and II inhibition.

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