Abstract
A range of isatin-thiazolidinone hybrid analogues were synthesized and their cytotoxicity was evaluated against several cancer cell lines in vitro. The acute toxicity studies in mice models revealed that these analogues possess low systemic toxicity and are safe up to 1600mg/Kg. Among the compounds synthesized, 5-(2-nitrobenzylidene)-2-(isatin-3- azino)-thiazolidin-4-one (CI) has been shown to be the most active, highly promising compound which induced S phase arrest in cell cycle in a time dependent manner. Our initial analysis indicate that incorporation of electron withdrawing group at ortho position of the ring favors over the meta and para positions for eliciting its cytostatic effect. Overall, the in vitro biological evaluation suggests that the growth inhibitory effect of CI is promising and can be studied further.
Keywords: Isatin, thiazolidinone, cancer, cytotoxicity, cell cycle arrest, Isatin-Thiazolidinone Hybrid, Anti-Proliferative Agents, Phosphorylation, threonine, Alzheimer's, anti-proliferative effects, tyrosine kinases, p-glycoprotein, mitochondria, spectrophotometer, tetramethylsilane (TMS), DMEM, DMSO, 3-Thiosemicarbazone, 5-(2-Nitrobenzylidene), 4-Fluorobenzylidene, 4-Hydroxybenzylidene, isopropyl alcohol, ELISA microplate reader, cyclocondensation, NCI ADR Res, benzylidene ring, pharmacological screening, Trivandrum
Medicinal Chemistry
Title: Synthesis and In Vitro Evaluation of Some Isatin-Thiazolidinone Hybrid Analogues as Anti-Proliferative Agents
Volume: 6 Issue: 5
Author(s): P. K. Ramshid, Sankar Jagadeeshan, Anand Krishnan, Mary Mathew, S. Asha Nair and M. Radhakrishna Pillai
Affiliation:
Keywords: Isatin, thiazolidinone, cancer, cytotoxicity, cell cycle arrest, Isatin-Thiazolidinone Hybrid, Anti-Proliferative Agents, Phosphorylation, threonine, Alzheimer's, anti-proliferative effects, tyrosine kinases, p-glycoprotein, mitochondria, spectrophotometer, tetramethylsilane (TMS), DMEM, DMSO, 3-Thiosemicarbazone, 5-(2-Nitrobenzylidene), 4-Fluorobenzylidene, 4-Hydroxybenzylidene, isopropyl alcohol, ELISA microplate reader, cyclocondensation, NCI ADR Res, benzylidene ring, pharmacological screening, Trivandrum
Abstract: A range of isatin-thiazolidinone hybrid analogues were synthesized and their cytotoxicity was evaluated against several cancer cell lines in vitro. The acute toxicity studies in mice models revealed that these analogues possess low systemic toxicity and are safe up to 1600mg/Kg. Among the compounds synthesized, 5-(2-nitrobenzylidene)-2-(isatin-3- azino)-thiazolidin-4-one (CI) has been shown to be the most active, highly promising compound which induced S phase arrest in cell cycle in a time dependent manner. Our initial analysis indicate that incorporation of electron withdrawing group at ortho position of the ring favors over the meta and para positions for eliciting its cytostatic effect. Overall, the in vitro biological evaluation suggests that the growth inhibitory effect of CI is promising and can be studied further.
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Cite this article as:
K. Ramshid P., Jagadeeshan Sankar, Krishnan Anand, Mathew Mary, Asha Nair S. and Radhakrishna Pillai M., Synthesis and In Vitro Evaluation of Some Isatin-Thiazolidinone Hybrid Analogues as Anti-Proliferative Agents, Medicinal Chemistry 2010; 6 (5) . https://dx.doi.org/10.2174/157340610793358909
DOI https://dx.doi.org/10.2174/157340610793358909 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
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