PMID- 24370011
OWN - NLM
STAT- MEDLINE
DCOM- 20140826
LR  - 20140113
IS  - 1464-3405 (Electronic)
IS  - 0960-894X (Linking)
VI  - 24
IP  - 2
DP  - 2014 Jan 15
TI  - Synthesis, anticancer activity and DNA-binding properties of novel 
      4-pyrazolyl-1,8-naphthalimide derivatives.
PG  - 586-90
LID - S0960-894X(13)01386-3 [pii]
LID - 10.1016/j.bmcl.2013.12.014 [doi]
AB  - A novel series of 4-pyrazolyl-1,8-naphthalimide derivatives have been designed 
      and facilely synthesized. For anticancer activity in vitro, most of the compounds 
      were found to be more toxic against human mammary cancer cells (MCF-7) than human 
      cervical carcinoma cells (Hela) and human lung cancer cells (A549). Compounds 4i, 
      4h, 4b and 4a showed improved cytotoxic activity against MCF-7 cells over 
      amonafide, in particular compounds 4i and 4h, the IC50 values of which against 
      cell lines of MCF-7 were 0.51 muM and 0.79 muM, respectively. The DNA-binding 
      properties of 4i were investigated by UV-vis, fluorescence, and Circular 
      Dichroism (CD) spectroscopies and thermal denaturation. The results indicated 
      that compound 4i as the DNA-intercalating agent exhibited middle binding affinity 
      with CT-DNA.
CI  - Copyright (c) 2013 Elsevier Ltd. All rights reserved.
FAU - Li, Shenghui
AU  - Li S
AD  - Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and 
      Environmental Science, Hebei University, Baoding 071002, China; Key Laboratory of 
      Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, Hebei 
      University, Baoding 071002, China. Electronic address: lish@hbu.edu.cn.
FAU - Xu, Shengjie
AU  - Xu S
AD  - Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and 
      Environmental Science, Hebei University, Baoding 071002, China.
FAU - Tang, Yonghe
AU  - Tang Y
AD  - Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and 
      Environmental Science, Hebei University, Baoding 071002, China.
FAU - Ding, Shan
AU  - Ding S
AD  - Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and 
      Environmental Science, Hebei University, Baoding 071002, China.
FAU - Zhang, Jinchao
AU  - Zhang J
AD  - Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and 
      Environmental Science, Hebei University, Baoding 071002, China; Key Laboratory of 
      Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, Hebei 
      University, Baoding 071002, China. Electronic address: jczhang@126.com.
FAU - Wang, Shuxiang
AU  - Wang S
AD  - Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and 
      Environmental Science, Hebei University, Baoding 071002, China; Key Laboratory of 
      Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, Hebei 
      University, Baoding 071002, China.
FAU - Zhou, Guoqiang
AU  - Zhou G
AD  - Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and 
      Environmental Science, Hebei University, Baoding 071002, China.
FAU - Zhou, Chuanqi
AU  - Zhou C
AD  - Key Laboratory of Medicinal Chemistry and Molecular Diagnosis, Ministry of 
      Education, Hebei University, Baoding 071002, China.
FAU - Li, Xiaoliu
AU  - Li X
AD  - Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and 
      Environmental Science, Hebei University, Baoding 071002, China; Key Laboratory of 
      Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, Hebei 
      University, Baoding 071002, China.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20131214
PL  - England
TA  - Bioorg Med Chem Lett
JT  - Bioorganic & medicinal chemistry letters
JID - 9107377
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Intercalating Agents)
RN  - 0 (Naphthalimides)
RN  - 9007-49-2 (DNA)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents/*chemical synthesis/*metabolism
MH  - Cattle
MH  - DNA/*metabolism
MH  - Drug Screening Assays, Antitumor/methods
MH  - HeLa Cells
MH  - Humans
MH  - Intercalating Agents/chemical synthesis/metabolism
MH  - MCF-7 Cells
MH  - Naphthalimides/*chemical synthesis/*metabolism
MH  - Protein Binding/physiology
MH  - Structure-Activity Relationship
OTO - NOTNLM
OT  - Anticancer
OT  - DNA-binding
OT  - Naphthalimides
OT  - Pyrazole
EDAT- 2013/12/29 06:00
MHDA- 2014/08/27 06:00
CRDT- 2013/12/28 06:00
PHST- 2013/09/10 00:00 [received]
PHST- 2013/11/01 00:00 [revised]
PHST- 2013/12/03 00:00 [accepted]
PHST- 2013/12/28 06:00 [entrez]
PHST- 2013/12/29 06:00 [pubmed]
PHST- 2014/08/27 06:00 [medline]
AID - S0960-894X(13)01386-3 [pii]
AID - 10.1016/j.bmcl.2013.12.014 [doi]
PST - ppublish
SO  - Bioorg Med Chem Lett. 2014 Jan 15;24(2):586-90. doi: 10.1016/j.bmcl.2013.12.014. 
      Epub 2013 Dec 14.