PMID- 32429433
OWN - NLM
STAT- MEDLINE
DCOM- 20210212
LR  - 20210212
IS  - 1420-3049 (Electronic)
IS  - 1420-3049 (Linking)
VI  - 25
IP  - 10
DP  - 2020 May 16
TI  - Exploiting the Indole Scaffold to Design Compounds Binding to Different 
      Pharmacological Targets.
LID - 10.3390/molecules25102331 [doi]
LID - 2331
AB  - Several indole derivatives have been disclosed by our research groups that have 
      been collaborating for nearly 25 years. The results of our investigations led to 
      a variety of molecules binding selectively to different pharmacological targets, 
      specifically the type A gamma-aminobutyric acid (GABA(A)) chloride channel, the 
      translocator protein (TSPO), the murine double minute 2 (MDM2) protein, the A(2B) 
      adenosine receptor (A(2B) AR) and the Kelch-like ECH-associated protein 1 
      (Keap1). Herein, we describe how these works were conceived and carried out 
      thanks to the versatility of indole nucleus to be exploited in the design and 
      synthesis of drug-like molecules.
FAU - Taliani, Sabrina
AU  - Taliani S
AUID- ORCID: 0000-0001-8675-939X
AD  - Department of Pharmacy, University of Pisa, Via Bonanno Pisano, 6, 56126 Pisa, 
      Italy.
FAU - Da Settimo, Federico
AU  - Da Settimo F
AD  - Department of Pharmacy, University of Pisa, Via Bonanno Pisano, 6, 56126 Pisa, 
      Italy.
FAU - Martini, Claudia
AU  - Martini C
AUID- ORCID: 0000-0001-9379-3027
AD  - Department of Pharmacy, University of Pisa, Via Bonanno Pisano, 6, 56126 Pisa, 
      Italy.
FAU - Laneri, Sonia
AU  - Laneri S
AD  - Department of Pharmacy, University of Naples "Federico II", Via D. Montesano, 49, 
      80131 Naples, Italy.
FAU - Novellino, Ettore
AU  - Novellino E
AD  - Department of Pharmacy, University of Naples "Federico II", Via D. Montesano, 49, 
      80131 Naples, Italy.
FAU - Greco, Giovanni
AU  - Greco G
AD  - Department of Pharmacy, University of Naples "Federico II", Via D. Montesano, 49, 
      80131 Naples, Italy.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20200516
PL  - Switzerland
TA  - Molecules
JT  - Molecules (Basel, Switzerland)
JID - 100964009
RN  - 0 (GABA Modulators)
RN  - 0 (Indoles)
RN  - 0 (KEAP1 protein, human)
RN  - 0 (Kelch-Like ECH-Associated Protein 1)
RN  - 0 (Ligands)
RN  - 0 (Receptor, Adenosine A2B)
RN  - 0 (Receptors, GABA)
RN  - 0 (Receptors, GABA-A)
RN  - 0 (TSPO protein, human)
RN  - EC 2.3.2.27 (MDM2 protein, human)
RN  - EC 2.3.2.27 (Mdm2 protein, mouse)
RN  - EC 2.3.2.27 (Proto-Oncogene Proteins c-mdm2)
RN  - Q3JTX2Q7TU (Diazepam)
SB  - IM
MH  - Animals
MH  - Diazepam/*analogs & derivatives/pharmacology
MH  - *Drug Design
MH  - GABA Modulators/*chemical synthesis/pharmacology
MH  - Humans
MH  - Indoles/*chemical synthesis/pharmacology
MH  - Kelch-Like ECH-Associated Protein 1/agonists/antagonists & inhibitors/metabolism
MH  - Ligands
MH  - Mice
MH  - Protein Binding
MH  - Proto-Oncogene Proteins c-mdm2/antagonists & inhibitors/chemistry/metabolism
MH  - Receptor, Adenosine A2B/chemistry/metabolism
MH  - Receptors, GABA/chemistry/metabolism
MH  - Receptors, GABA-A/chemistry/*metabolism
MH  - Structure-Activity Relationship
PMC - PMC7287756
OTO - NOTNLM
OT  - A2B adenosine receptor (A2B AR)
OT  - Kelch-like ECH-associated protein 1 (Keap1)
OT  - murine double Minute 2 (MDM2) protein
OT  - translocator protein (TSPO)
OT  - type A gamma-aminobutyric acid (GABAA) chloride channel
COIS- The authors declare no conflict of interest
EDAT- 2020/05/21 06:00
MHDA- 2021/02/13 06:00
PMCR- 2020/05/16
CRDT- 2020/05/21 06:00
PHST- 2020/04/20 00:00 [received]
PHST- 2020/05/14 00:00 [revised]
PHST- 2020/05/15 00:00 [accepted]
PHST- 2020/05/21 06:00 [entrez]
PHST- 2020/05/21 06:00 [pubmed]
PHST- 2021/02/13 06:00 [medline]
PHST- 2020/05/16 00:00 [pmc-release]
AID - molecules25102331 [pii]
AID - molecules-25-02331 [pii]
AID - 10.3390/molecules25102331 [doi]
PST - epublish
SO  - Molecules. 2020 May 16;25(10):2331. doi: 10.3390/molecules25102331.