Optimized Synthesis and Characterization of Thiazolidine-2, 4-Dione for Pharmaceutical Application

Pinheiro, Danilo da Silva; Santos, Edson Nascimento dos; Consolini, Gabriela; Aguiar, Márcio José; Silva, Renan Rodrigues de Oliveira; Vieira, Rodrigo de Oliveira; Palma, Mauri Sérgio Alves

doi:10.15406/mojboc.2017.01.00022

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Cited by 8 publications

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“…Os reagentes foram adquiridos das empresas Merck KGaA (Darmstadt, Alemanha), Labsynth (Diadema, Brasil) e Oakwood Chemicals (Columbia, EUA), e foram utilizados sem prévia purificação. Vale ressaltar que a TZD foi previamente sintetizada a partir de um procedimento adaptado descrito na literatura (PINHEIRO et al, 2017).…”

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Síntese da Pioglitazona e Lobeglitazona em batelada e microrreator capilar

Silva

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Section: Produtos Químicosunclassified

Síntese da Pioglitazona e Lobeglitazona em batelada e microrreator capilar

Silva

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Novel benzothiazole/benzothiazole thiazolidine‐2,4‐dione derivatives as potential FOXM1 inhibitors: In silico, synthesis, and in vitro studies

Abusharkh,

Comert Onder,

Çınar

et al. 2024

Archiv der Pharmazie

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The oncogenic transcription factor FOXM1 overexpressed in breast and other solid cancers, is a key driver of tumor growth and progression through complex interactions, making it an attractive molecular target for the development of targeted therapies. Despite the availability of small‐molecule inhibitors, their limited specificity, potency, and efficacy hinder clinical translation. To identify effective FOXM1 inhibitors, we synthesized novel benzothiazole derivatives (KC10–KC13) and benzothiazole hybrids with thiazolidine‐2,4‐dione (KC21–KC36). These compounds were evaluated for FOXM1 inhibition. Molecular docking and molecular dynamics simulation analysis revealed their binding patterns and affinities for the FOXM1‐DNA binding domain. The interactions with key amino acids such as Asn283, His287, and Arg286, crucial for FOXM1 inhibition, have been determined with the synthesized compounds. Additionally, the molecular modeling study indicated that KC12, KC21, and KC30 aligned structurally and interacted similarly to the reference compound FDI‐6. In vitro studies with the MDA‐MB‐231 breast cancer cell line demonstrated that KC12, KC21, and KC30 significantly inhibited FOXM1, showing greater potency than FDI‐6, with IC50 values of 6.13, 10.77, and 12.86 µM, respectively, versus 20.79 µM for FDI‐6. Our findings suggest that KC12, KC21, and KC30 exhibit strong activity as FOXM1 inhibitors and may be suitable for in vivo animal studies.

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