Literature DB >> 20667627

Synthesis and primary cytotoxicity evaluation of new 5-benzylidene-2,4-thiazolidinedione derivatives.

Vijay Patil1, Kalpana Tilekar, Sonali Mehendale-Munj, Rhea Mohan, C S Ramaa.   

Abstract

In the present work, ten novel derivatives (3a-3j) of 5-benzylidene-2,4-thiazolidinediones were synthesized and their structures were determined by analytical and spectral (FTIR, (1)H NMR, (13)C NMR) methods. The newly synthesized compounds were evaluated for their antiproliferative activity at Tata Memorial's Advanced Center for Treatment, Research and Education in Cancer (ACTREC), India, in a panel of 7 cancer cell lines using four concentrations at 10-fold dilutions. Sulforhodamine B (SRB) protein assay was used to estimate cell stability or growth. Though the compounds showed varying degrees of cytotoxicity in the tested cell lines, most marked effect was observed by compound 3e in MCF7 (breast cancer), K562 (leukemia) and GURAV (nasopharyngeal cancer) cell lines with log(10) GI(50) values of -6.7, -6.72 and -6.73 respectively. Copyright (c) 2010 Elsevier Masson SAS. All rights reserved.

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Year:  2010        PMID: 20667627     DOI: 10.1016/j.ejmech.2010.07.014

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  20 in total

1.  Structure guided design and synthesis of furyl thiazolidinedione derivatives as inhibitors of GLUT 1 and GLUT 4, and evaluation of their anti-leukemic potential.

Authors:  Kalpana Tilekar; Neha Upadhyay; Jessica D Hess; Lucasantiago Henze Macias; Piotr Mrowka; Renato J Aguilera; Franz-Josef Meyer-Almes; Cristina V Iancu; Jun-Yong Choe; C S Ramaa
Journal:  Eur J Med Chem       Date:  2020-07-02       Impact factor: 6.514

2.  Discovery of novel N-substituted thiazolidinediones (TZDs) as HDAC8 inhibitors: in-silico studies, synthesis, and biological evaluation.

Authors:  Neha Upadhyay; Kalpana Tilekar; Niklas Jänsch; Markus Schweipert; Jessica D Hess; Luca Henze Macias; Piotr Mrowka; Renato J Aguilera; Jun-Yong Choe; Franz-Josef Meyer-Almes; C S Ramaa
Journal:  Bioorg Chem       Date:  2020-05-15       Impact factor: 5.275

3.  Multi-target weapons: diaryl-pyrazoline thiazolidinediones simultaneously targeting VEGFR-2 and HDAC cancer hallmarks.

Authors:  Neha Upadhyay; Kalpana Tilekar; Sabreena Safuan; Alan P Kumar; Markus Schweipert; Franz-Josef Meyer-Almes; Ramaa C S
Journal:  RSC Med Chem       Date:  2021-07-27

4.  A green, multicomponent, regio- and stereo-selective 1,3-dipolar cycloaddition of azides and azomethine ylides generated in situ with bifunctional dipolarophiles using PEG-400.

Authors:  Jayant Sindhu; Harjinder Singh; J M Khurana
Journal:  Mol Divers       Date:  2014-02-28       Impact factor: 2.943

5.  Synthesis and Hypoglycemic and Anti-inflammatory Activity Screening of Novel Substituted 5-[Morpholino(Phenyl)Methyl]-Thiazolidine-2,4-Diones and Their Molecular Docking Studies.

Authors:  Srikanth Kumar Karumanchi; Lakshmana Rao Atmakuri; V Basaveswara Rao Mandava; Srikala Rajala
Journal:  Turk J Pharm Sci       Date:  2019-11-11

6.  Synthesis, HIV-1 RT inhibitory, antibacterial, antifungal and binding mode studies of some novel N-substituted 5-benzylidine-2,4-thiazolidinediones.

Authors:  Radhe Shyam Bahare; Swastika Ganguly; Kiattawee Choowongkomon; Supaporn Seetaha
Journal:  Daru       Date:  2015-01-24       Impact factor: 3.117

Review 7.  Recent pharmacological developments on rhodanines and 2,4-thiazolidinediones.

Authors:  Ravinder Singh Bhatti; Sakshi Shah; Pawan Krishan; Jagir S Sandhu
Journal:  Int J Med Chem       Date:  2013-05-02

Review 8.  Biological potential of thiazolidinedione derivatives of synthetic origin.

Authors:  Sumit Tahlan; Prabhakar Kumar Verma
Journal:  Chem Cent J       Date:  2017-12-08       Impact factor: 4.215

9.  Synthesis and antibacterial activity of new (2,4-dioxothiazolidin-5-yl/ylidene)acetic acid derivatives with thiazolidine-2,4-dione, rhodanine and 2-thiohydantoin moieties.

Authors:  Nazar Trotsko; Urszula Kosikowska; Agata Paneth; Monika Wujec; Anna Malm
Journal:  Saudi Pharm J       Date:  2018-02-02       Impact factor: 4.330

10.  Permuted 2,4-thiazolidinedione (TZD) analogs as GLUT inhibitors and their in-vitro evaluation in leukemic cells.

Authors:  Kalpana Tilekar; Neha Upadhyay; Markus Schweipert; Jessica D Hess; Lucasantiago Henze Macias; Piotr Mrowka; Franz-Josef Meyer-Almes; Renato J Aguilera; Cristina V Iancu; Jun-Yong Choe; C S Ramaa
Journal:  Eur J Pharm Sci       Date:  2020-08-12       Impact factor: 5.112

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