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

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

Content Provider	PubMed Central
Author	Eyunni, Suresh Kumar V. K. Madhavi, Gangapuram Redda, Kinfe K.
Copyright Year	2014
Abstract	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 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.
Related Links	http://dx.doi.org/10.2174/1570180811666131203002502
Ending Page	436
Page Count	9
Starting Page	428
File Format	PDF
ISSN	15701808
Journal	Letters in drug design & discovery
Issue Number	4
Volume Number	11
Language	English
Publisher Date	2014-03-31
Access Restriction	Open
Subject Keyword	Molecular Medicine Drug Discovery Pharmaceutical Science Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Molecular Medicine Pharmaceutical Science

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