PMID- 28442256
OWN - NLM
STAT- MEDLINE
DCOM- 20170919
LR  - 20190430
IS  - 1464-3405 (Electronic)
IS  - 0960-894X (Print)
IS  - 0960-894X (Linking)
VI  - 27
IP  - 11
DP  - 2017 Jun 1
TI  - Functional evaluation of synthetic flavonoids and chalcones for potential 
      antiviral and anticancer properties.
PG  - 2350-2356
LID - S0960-894X(17)30410-9 [pii]
LID - 10.1016/j.bmcl.2017.04.034 [doi]
AB  - Flavonoids, stilbenes, and chalcones are plant secondary metabolites that often 
      possess diverse biological activities including anti-inflammatory, anti-cancer, 
      and anti-viral activities. The wide range of bioactivities poses a challenge to 
      identify their targets. Here, we studied a set of synthetically generated 
      flavonoids and chalcones to evaluate for their biological activity, and compared 
      similarly substituted flavonoids and chalcones. Substituted chalcones, but not 
      flavonoids, showed inhibition of viral translation without significantly 
      affecting viral replication in cells infected with hepatitis C virus (HCV). We 
      suggest that the chalcones used in this study inhibit mammalian target of 
      rapamycin (mTOR) pathway by ablating phosphorylation of ribosomal protein 6 
      (rps6), and also the kinase necessary for phosphorylating rps6 in Huh7.5 cells 
      (pS6K1). In addition, selected chalcones showed inhibition of growth in Ishikawa, 
      MCF7, and MDA-MB-231 cells resulting an IC(50) of 1-6microg/mL. When similarly 
      substituted flavonoids were used against the same set of cancer cells, we did not 
      observe any inhibitory effect. Together, we report that chalcones show potential 
      for anti-viral and anti-cancer activities compared to similarly substituted 
      flavonoids.
CI  - Copyright (c) 2017 Elsevier Ltd. All rights reserved.
FAU - Mateeva, Nelly
AU  - Mateeva N
AD  - Department of Chemistry, Florida A&M University, 1530 S MLK Blvd, Tallahassee, FL 
      32307, United States.
FAU - Eyunni, Suresh V K
AU  - Eyunni SVK
AD  - Department of Pharmacy and Pharmaceutical Sciences, Florida A&M University, 
      Tallahassee, FL 32307, United States.
FAU - Redda, Kinfe K
AU  - Redda KK
AD  - Department of Pharmacy and Pharmaceutical Sciences, Florida A&M University, 
      Tallahassee, FL 32307, United States.
FAU - Ononuju, Ucheze
AU  - Ononuju U
AD  - Department of Chemistry, Florida A&M University, 1530 S MLK Blvd, Tallahassee, FL 
      32307, United States.
FAU - Hansberry, Tony D 2nd
AU  - Hansberry TD 2nd
AD  - Department of Chemistry, Florida A&M University, 1530 S MLK Blvd, Tallahassee, FL 
      32307, United States.
FAU - Aikens, Cecilia
AU  - Aikens C
AD  - Department of Chemistry, Florida A&M University, 1530 S MLK Blvd, Tallahassee, FL 
      32307, United States.
FAU - Nag, Anita
AU  - Nag A
AD  - Department of Chemistry, Furman University, 3300 Poinsett Highway, Greenville, SC 
      29613, United States. Electronic address: anita.nag@furman.edu.
LA  - eng
GR  - G12 MD007582/MD/NIMHD NIH HHS/United States
GR  - P20 MD006738/MD/NIMHD NIH HHS/United States
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
PT  - Research Support, Non-U.S. Gov't
DEP - 20170413
PL  - England
TA  - Bioorg Med Chem Lett
JT  - Bioorganic & medicinal chemistry letters
JID - 9107377
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Antiviral Agents)
RN  - 0 (Chalcones)
RN  - 0 (Flavonoids)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents/chemistry/*pharmacology
MH  - Antiviral Agents/chemistry/*pharmacology
MH  - Cell Line, Tumor
MH  - Chalcones/chemistry/*pharmacology
MH  - Flavonoids/chemistry/*pharmacology
MH  - Humans
MH  - Structure-Activity Relationship
PMC - PMC5641219
MID - NIHMS871336
OTO - NOTNLM
OT  - Cancer
OT  - Chalcone
OT  - HCV
OT  - mTOR
OT  - rsp6
EDAT- 2017/04/27 06:00
MHDA- 2017/09/20 06:00
PMCR- 2018/06/01
CRDT- 2017/04/27 06:00
PHST- 2017/02/03 00:00 [received]
PHST- 2017/04/08 00:00 [revised]
PHST- 2017/04/10 00:00 [accepted]
PHST- 2017/04/27 06:00 [pubmed]
PHST- 2017/09/20 06:00 [medline]
PHST- 2017/04/27 06:00 [entrez]
PHST- 2018/06/01 00:00 [pmc-release]
AID - S0960-894X(17)30410-9 [pii]
AID - 10.1016/j.bmcl.2017.04.034 [doi]
PST - ppublish
SO  - Bioorg Med Chem Lett. 2017 Jun 1;27(11):2350-2356. doi: 
      10.1016/j.bmcl.2017.04.034. Epub 2017 Apr 13.