In-Vitro Antiproliferative Activity of New Tetrahydroisoquinolines (THIQs) on Ishikawa Cells and their 3D Pharmacophore Models

ISSN: 1875-628X (Online)
ISSN: 1570-1808 (Print)

Volume 14, 12 Issues, 2017

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Letters in Drug Design & Discovery

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G. Perry
University of Texas
San Antonio, TX

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In-Vitro Antiproliferative Activity of New Tetrahydroisoquinolines (THIQs) on Ishikawa Cells and their 3D Pharmacophore Models

Letters in Drug Design & Discovery, 11(4): 428-436.

Author(s): Suresh Kumar V. K. Eyunni, Madhavi Gangapuram and Kinfe K Redda.

Affiliation: College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, Florida 32307, USA.


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 IC50 values are 1.41, 0.91, 0.74 and 0.36 µM respectively. This study helped us to evaluate the risk of developing endometrial cancer in the design of nonsteroid 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.


Antiproliferative agents, Ishikawa Cell lines, Tetrahydroisoquinolines, Pharmacophore Models.

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Article Details

Volume: 11
Issue Number: 4
First Page: 428
Last Page: 436
Page Count: 9
DOI: 10.2174/1570180811666131203002502
Price: $58
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