PMID- 25506297
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20200930
IS  - 1570-1808 (Print)
IS  - 1570-1808 (Linking)
VI  - 11
IP  - 4
DP  - 2014
TI  - In-vitro Antiproliferative Activity of New Tetrahydroisoquinolines (THIQs) on 
      Ishikawa Cells and their 3D Pharmacophore Models.
PG  - 428-436
AB  - The antiproliferative activities of new substituted tetrahydroisoquinolines 
      (THIQs) are described. Their cytotoxicities against Ishikawa human endometrial 
      cell line were determined after 72 h drug expose employing Celtiter-Glo assay at 
      concentrations ranging from 0.01 to 100,000 nM. The antiproliferative activities 
      of the compounds understudy were compared to tamoxifen (TAM). In-vitro results 
      indicated that most of the compounds showed better activity than TAM. The most 
      active compounds obtained in this study were 1, 2, 3 and 22 whose IC(50) values 
      are 1.41, 0.91, 0.74 and 0.36 muM respectively. This study helped us to evaluate 
      the risk of developing endometrial cancer in the design of non-steroid estrogen 
      receptor modulators with no agonistic effects on uterus. In-silico pharmacophore 
      hypotheses were generated using GALAHAD and PHASE and the best models with a 
      probable bioactive conformation(s) for these compounds were proposed. These 
      conformations and the alignments of the molecular structures give us an insight 
      in designing compounds with better biological activity.
FAU - Eyunni, Suresh Kumar V K
AU  - Eyunni SK
AD  - College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, 
      Tallahassee, Florida 32307.
FAU - Gangapuram, Madhavi
AU  - Gangapuram M
AD  - College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, 
      Tallahassee, Florida 32307.
FAU - Redda, Kinfe K
AU  - Redda KK
AD  - College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, 
      Tallahassee, Florida 32307.
LA  - eng
GR  - G12 MD007582/MD/NIMHD NIH HHS/United States
PT  - Journal Article
PL  - United Arab Emirates
TA  - Lett Drug Des Discov
JT  - Letters in drug design & discovery
JID - 101208443
PMC - PMC4264606
MID - NIHMS580134
OTO - NOTNLM
OT  - Antiproliferative agents
OT  - Ishikawa Cell lines
OT  - Pharmacophore Models
OT  - Tetrahydroisoquinolines
COIS- CONFLICT OF INTEREST The authors confirm that this article content has no 
      conflicts of interest.
EDAT- 2014/12/17 06:00
MHDA- 2014/12/17 06:01
PMCR- 2014/12/12
CRDT- 2014/12/16 06:00
PHST- 2014/12/16 06:00 [entrez]
PHST- 2014/12/17 06:00 [pubmed]
PHST- 2014/12/17 06:01 [medline]
PHST- 2014/12/12 00:00 [pmc-release]
AID - 10.2174/1570180811666131203002502 [doi]
PST - ppublish
SO  - Lett Drug Des Discov. 2014;11(4):428-436. doi: 10.2174/1570180811666131203002502.