2. Academic Validation
  3. Novel Meta-iodobenzylguanidine-Based Copper Thiosemicarbazide-1-guanidinomethylbenzyl Anticancer Compounds Targeting Norepinephrine Transporter in Neuroblastoma

Novel Meta-iodobenzylguanidine-Based Copper Thiosemicarbazide-1-guanidinomethylbenzyl Anticancer Compounds Targeting Norepinephrine Transporter in Neuroblastoma

  • J Med Chem. 2019 Aug 8;62(15):6985-6991. doi: 10.1021/acs.jmedchem.9b00386.
Haiyuan Zhang 1,  Fang Xie 2,  Muhua Cheng 3,  Fangyu Peng 1 2 4
Affiliations

Affiliations

  • 1 Carman & Ann Adams Department of Pediatrics, School of Medicine , Wayne State University , Detroit , Michigan 48201 , United States.
  • 2 Department of Radiology , University of Texas Southwestern Medical Center , Dallas , Texas 735390 , United States.
  • 3 Department of Nuclear Medicine , Third Affiliated Hospital of Sun Yat-sen University , Guangzhou , Guangdong 510630 , P. R. China.
  • 4 Harold C. Simmons Comprehensive Cancer Center , University of Texas Southwestern Medical Center , Dallas , Texas 75390 , United States.
PMID: 31283215 DOI: 10.1021/acs.jmedchem.9b00386
Abstract

Meta-iodobenzylguanidine (MIBG) is a ligand with high affinity against norepinephrine transporter (NET) that has been used for diagnostic imaging and radionuclide therapy of NET-expressing tumors, such as neuroblastoma. We hypothesize that MIBG can be used as a ligand for development of new Anticancer drugs targeting NET-expressing neuroblastoma (NB). To test our hypothesis, we synthesized two MIBG-based Anticancer copper complexes [Cu(m-TSBG)2 and Cu(p-TSBG)2] by conjugation of a thiosemicarbazone copper group onto MIBG ligand. Both Cu(m-TSBG)2 and Cu(p-TSBG)2 compounds showed potent Anticancer activity against NB cells (BE2C and SK-N-DZ cells). The NB-specific Anticancer activity of Cu(m-TSBG)2 and Cu(p-TSBG)2 was further demonstrated by the reduced Anticancer activities when nonconjugated MIBG ligand was used to competitively block binding of Cu(m-TSBG)2 or Cu(p-TSBG)2 onto NET-expressing NB cells. Both Cu(m-TSBG)2 or Cu(p-TSBG)2 compounds hold potential as promising new drugs for targeted therapy of neuroblastoma and Other NET-expressing tumors.

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