2. Academic Validation
  3. Design, synthesis and biological evaluation of novel (E)-N-phenyl-4-(pyridine-acylhydrazone) benzamide derivatives as potential antitumor agents for the treatment of multiple myeloma (MM)

Design, synthesis and biological evaluation of novel (E)-N-phenyl-4-(pyridine-acylhydrazone) benzamide derivatives as potential antitumor agents for the treatment of multiple myeloma (MM)

  • Bioorg Chem. 2020 Oct;103:104189. doi: 10.1016/j.bioorg.2020.104189.
Xin-Yang Li 1,  Shuai Li 2,  Guo-Qing Lu 2,  De-Pu Wang 2,  Kai-Li Liu 2,  Xin-Hua Qian 2,  Wen-Han Xue 2,  Fan-Hao Meng 3
Affiliations

Affiliations

  • 1 School of Pharmacy, China Medical University, 77 Puhe Road, North New Area, Shenyang 110122, China; Department of Pharmacy, Shengjing Hospital of China Medical University, Shenyang 110122, China.
  • 2 School of Pharmacy, China Medical University, 77 Puhe Road, North New Area, Shenyang 110122, China.
  • 3 School of Pharmacy, China Medical University, 77 Puhe Road, North New Area, Shenyang 110122, China. Electronic address: fhmeng@cmu.edu.cn.
PMID: 32890996 DOI: 10.1016/j.bioorg.2020.104189
Abstract

A series of novel (E)-N-phenyl-4-(pyridine-acylhydrazone) benzamide derivatives were designed, synthesized, and evaluated for their anti-proliferative activity against two different human Cancer cell lines and one human normal cell line. Compound 8b had the best anti-proliferative activity (IC50 = 0.12 ± 0.09 μM, RPMI8226 cells) than the Other compounds. And compound 8b had lower toxicity than imatinib. Flow cytometry analysis showed that compound 8b could arrest the cell cycle at the G0/G1 phase, and induce Apoptosis of RPMI8226 cells by promoting mitochondrial ROS release, thereby effectively inhibiting cell proliferation. Our findings provided a promising lead compound 8b for further structural optimization and will be instructive for the discovery of more potent antitumor drugs with high selectivity and low toxicity.

Keywords

Antitumor; Apoptosis; Multiple myeloma (MM).

Figures
Products
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