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One-Pot Synthesis of Novel 2-Imino-5-Arylidine-Thiazolidine Analogues and Evaluation of Their Anti-Proliferative Activity against MCF7 Breast Cancer Cell Line

An efficient surface-mediated synthetic method to facilitate access to a novel class of thiazolidines is described. The rationale behind the design of the targeted thiazolidines was to prepare stable thiazolidine analogues and evaluate their anti-proliferative activity against a breast cancer cell l...

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Autores principales: Aziz, Marian N., Patel, Arzoo, Iskander, Amany, Chini, Avisankar, Gout, Delphine, Mandal, Subhrangsu S., Lovely, Carl J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8840064/
https://www.ncbi.nlm.nih.gov/pubmed/35164106
http://dx.doi.org/10.3390/molecules27030841
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author Aziz, Marian N.
Patel, Arzoo
Iskander, Amany
Chini, Avisankar
Gout, Delphine
Mandal, Subhrangsu S.
Lovely, Carl J.
author_facet Aziz, Marian N.
Patel, Arzoo
Iskander, Amany
Chini, Avisankar
Gout, Delphine
Mandal, Subhrangsu S.
Lovely, Carl J.
author_sort Aziz, Marian N.
collection PubMed
description An efficient surface-mediated synthetic method to facilitate access to a novel class of thiazolidines is described. The rationale behind the design of the targeted thiazolidines was to prepare stable thiazolidine analogues and evaluate their anti-proliferative activity against a breast cancer cell line (MCF7). Most of the synthesized analogues exhibited increased potency ranging from 2–15-fold higher compared to the standard reference, cisplatin. The most active thiazolidines contain a halogenated or electron withdrawing group attached to the N-phenyl ring of exocyclic 2-imino group. However, combination of the two substituents did not enhance the activity. The anti-proliferative activity was measured in terms of IC(50) values using an MTT assay.
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spelling pubmed-88400642022-02-13 One-Pot Synthesis of Novel 2-Imino-5-Arylidine-Thiazolidine Analogues and Evaluation of Their Anti-Proliferative Activity against MCF7 Breast Cancer Cell Line Aziz, Marian N. Patel, Arzoo Iskander, Amany Chini, Avisankar Gout, Delphine Mandal, Subhrangsu S. Lovely, Carl J. Molecules Article An efficient surface-mediated synthetic method to facilitate access to a novel class of thiazolidines is described. The rationale behind the design of the targeted thiazolidines was to prepare stable thiazolidine analogues and evaluate their anti-proliferative activity against a breast cancer cell line (MCF7). Most of the synthesized analogues exhibited increased potency ranging from 2–15-fold higher compared to the standard reference, cisplatin. The most active thiazolidines contain a halogenated or electron withdrawing group attached to the N-phenyl ring of exocyclic 2-imino group. However, combination of the two substituents did not enhance the activity. The anti-proliferative activity was measured in terms of IC(50) values using an MTT assay. MDPI 2022-01-27 /pmc/articles/PMC8840064/ /pubmed/35164106 http://dx.doi.org/10.3390/molecules27030841 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Aziz, Marian N.
Patel, Arzoo
Iskander, Amany
Chini, Avisankar
Gout, Delphine
Mandal, Subhrangsu S.
Lovely, Carl J.
One-Pot Synthesis of Novel 2-Imino-5-Arylidine-Thiazolidine Analogues and Evaluation of Their Anti-Proliferative Activity against MCF7 Breast Cancer Cell Line
title One-Pot Synthesis of Novel 2-Imino-5-Arylidine-Thiazolidine Analogues and Evaluation of Their Anti-Proliferative Activity against MCF7 Breast Cancer Cell Line
title_full One-Pot Synthesis of Novel 2-Imino-5-Arylidine-Thiazolidine Analogues and Evaluation of Their Anti-Proliferative Activity against MCF7 Breast Cancer Cell Line
title_fullStr One-Pot Synthesis of Novel 2-Imino-5-Arylidine-Thiazolidine Analogues and Evaluation of Their Anti-Proliferative Activity against MCF7 Breast Cancer Cell Line
title_full_unstemmed One-Pot Synthesis of Novel 2-Imino-5-Arylidine-Thiazolidine Analogues and Evaluation of Their Anti-Proliferative Activity against MCF7 Breast Cancer Cell Line
title_short One-Pot Synthesis of Novel 2-Imino-5-Arylidine-Thiazolidine Analogues and Evaluation of Their Anti-Proliferative Activity against MCF7 Breast Cancer Cell Line
title_sort one-pot synthesis of novel 2-imino-5-arylidine-thiazolidine analogues and evaluation of their anti-proliferative activity against mcf7 breast cancer cell line
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8840064/
https://www.ncbi.nlm.nih.gov/pubmed/35164106
http://dx.doi.org/10.3390/molecules27030841
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