PMID- 29430288
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20201001
IS  - 1948-5956 (Print)
IS  - 1948-5956 (Electronic)
VI  - 9
IP  - 7
DP  - 2017
TI  - Synthesis and Biological Evaluations of Ring Substituted Tetrahydroisoquinolines 
      (THIQs) as Anti-Breast Cancer Agents.
PG  - 528-540
LID - 10.4172/1948-5956.1000470 [doi]
AB  - Breast cancer is a leading cause of mortality among women, resulting in more than 
      half a million deaths worldwide every year. Although chemotherapeutic drugs 
      remain the main stay of cancer treatment, it is observed that toxicity to normal 
      cells poses a limitation to their therapeutic values. Moreover, the patient 
      recovery rate from advanced breast cancer by chemotherapy is still unacceptably 
      low. Tetrahydroisoqinoline derivatives (THIQs) were reported to act as selective 
      subtype estrogen receptor antagonists/agonists and may serve as potential 
      therapeutic agents for breast cancer. In continuation of previous work we 
      systematically synthesized and characterized the tetrahydroisoquinoline (THIQs) 
      analogs. In-vitro antiproliferative activity of new substituted 
      tetrahydroisoquinoline analogs were evaluated against human ER (+) MCF-7 
      (breast), ER (-) MDA-MB-231 (breast) and Ishikawa (endometrial) cancer cell lines 
      using the CellTiter-Glo luminescent cell viability assay. The most active 
      compounds obtained in this study were 2b, 2i, and 3 g as demonstrated by their 
      activity (IC(50)=0.2 mug/mL, 0.08 mug/mL; 0.61 mug/mL, 0.09 mug/mL; 0.25 mug/mL, 0.11 
      mug/mL) against MCF-7 and Ishikawa cell lines respectively, in comparison to 
      Tamoxifen activity (IC(50)=3.99 mug/mL, 7.87 mug/ml). The newly synthesized 
      molecules were docked in the active sites of the ER-alpha (PDB: 3ERT), ER-beta (PDB: 
      1QKN) and alpha-beta tubulin taxol complex (1JFF) crystal structures to determine 
      the probable binding modes (bioactive conformations) of the active compounds.
FAU - Eyunni, Suresh Vk
AU  - Eyunni SV
AD  - College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, 
      Tallahassee, USA.
FAU - Gangapuram, Madhavi
AU  - Gangapuram M
AD  - College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, 
      Tallahassee, USA.
FAU - Mochona, Bereket
AU  - Mochona B
AD  - College of Science and Technology, Florida A&M University, Tallahassee, FL-32307, 
      USA.
FAU - Mateeva, Nelly
AU  - Mateeva N
AD  - College of Science and Technology, Florida A&M University, Tallahassee, FL-32307, 
      USA.
FAU - Redda, Kinfe K
AU  - Redda KK
AD  - College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, 
      Tallahassee, USA.
LA  - eng
GR  - G12 MD007582/MD/NIMHD NIH HHS/United States
GR  - P20 MD006738/MD/NIMHD NIH HHS/United States
PT  - Journal Article
DEP - 20170713
PL  - United States
TA  - J Cancer Sci Ther
JT  - Journal of cancer science & therapy
JID - 101526958
PMC - PMC5802351
MID - NIHMS911979
OTO - NOTNLM
OT  - Antiproliferative activity
OT  - Breast cancer
OT  - Ring substituted tetrahydroisoquinolines (THIQs)
EDAT- 2018/02/13 06:00
MHDA- 2018/02/13 06:01
PMCR- 2018/02/07
CRDT- 2018/02/13 06:00
PHST- 2018/02/13 06:00 [entrez]
PHST- 2018/02/13 06:00 [pubmed]
PHST- 2018/02/13 06:01 [medline]
PHST- 2018/02/07 00:00 [pmc-release]
AID - 10.4172/1948-5956.1000470 [doi]
PST - ppublish
SO  - J Cancer Sci Ther. 2017;9(7):528-540. doi: 10.4172/1948-5956.1000470. Epub 2017 
      Jul 13.