PMID- 26548744
OWN - NLM
STAT- MEDLINE
DCOM- 20170704
LR  - 20191027
IS  - 1875-6638 (Electronic)
IS  - 1573-4064 (Linking)
VI  - 12
IP  - 4
DP  - 2016
TI  - Design, Synthesis and Structure-Activity Relationship Studies of Novel 4 
      (1-adamantyl) Phenyl Analogues as HIF-1alpha Inhibitors.
PG  - 338-46
AB  - Hypoxia inducible factor-1 (HIF-1) is a key mediator during cancer cells to adapt 
      tumor hypoxic condition. In this study, a series of adamantane-based compounds 
      were synthesized and evaluated as potential inhibitors of HIF-1alpha. Examination of 
      their structure-activity relationship (SAR) identified the adamantane-containing 
      indole derivative 20a as a potent inhibitor of HIF-1alpha in Hep3B cell lines under 
      tumor hypoxia (IC50 = 0.02 microM). The study herein may provide valuable information 
      for the development of novel therapeutics against cancer and tumor angiogenesis.
FAU - Xia, Yan
AU  - Xia Y
FAU - Duan, Qiong
AU  - Duan Q
FAU - Zhao, Bao-Hua
AU  - Zhao BH
FAU - Li, Dong-Feng
AU  - Li DF
AD  - Laboratory of Photoelectric Material, Advanced Institute of Materials Science, 
      Changchun University of Technology, 130012, Changchun, P. R. China. 
      lidongfeng@ccut.edu.cn.
FAU - Hou, Rui-Bin
AU  - Hou RB
AD  - Department of Chemistry, College of Chemistry and Life Science, Changchun 
      University of Technology, 130012, Changchun, P. R. China. hrb1018@163.com.
LA  - eng
PT  - Journal Article
PL  - Netherlands
TA  - Med Chem
JT  - Medicinal chemistry (Shariqah (United Arab Emirates))
JID - 101240303
RN  - 0 (Acetanilides)
RN  - 0 (Antineoplastic Agents)
RN  - 0 (HIF1A protein, human)
RN  - 0 (Hypoxia-Inducible Factor 1, alpha Subunit)
RN  - 0 (methyl 
      3-(2-(2-(3-(1H-indol-3-yl)acrylamido)-4-(adamantan-1-yl)phenoxy)acetamido)benzoate)
RN  - PJY633525U (Adamantane)
SB  - IM
MH  - Acetanilides/chemical synthesis/*pharmacology/toxicity
MH  - Adamantane/*analogs & derivatives/chemical synthesis/*pharmacology/toxicity
MH  - Antineoplastic Agents/chemical synthesis/*pharmacology/toxicity
MH  - Cell Line, Tumor
MH  - Drug Screening Assays, Antitumor
MH  - Humans
MH  - Hypoxia-Inducible Factor 1, alpha Subunit/*antagonists & inhibitors
MH  - Structure-Activity Relationship
MH  - Tumor Hypoxia
EDAT- 2015/11/10 06:00
MHDA- 2017/07/05 06:00
CRDT- 2015/11/10 06:00
PHST- 2015/05/13 00:00 [received]
PHST- 2015/10/08 00:00 [revised]
PHST- 2015/10/26 00:00 [accepted]
PHST- 2015/11/10 06:00 [entrez]
PHST- 2015/11/10 06:00 [pubmed]
PHST- 2017/07/05 06:00 [medline]
AID - MC-EPUB-71664 [pii]
AID - 10.2174/1573406412666151109113007 [doi]
PST - ppublish
SO  - Med Chem. 2016;12(4):338-46. doi: 10.2174/1573406412666151109113007.