Design, Molecular Docking, Synthesis, Anticancer and Anti-Hyperglycemic Assessments of Thiazolidine-2,4-diones Bearing Sulfonylthiourea Moieties as Potent VEGFR-2 Inhibitors and PPARγ Agonists

Autor: Mohamed A. Abdelgawad, Khaled El-Adl, Sanadelaslam S. A. El-Hddad, Mostafa M. Elhady, Nashwa M. Saleh, Mohamed M. Khalifa, Fathalla Khedr, Mohamed Alswah, AbdElAziz A. Nayl, Mohammed M. Ghoneim, Nour E. A. Abd El-Sattar
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Pharmaceuticals, Vol 15, Iss 2, p 226 (2022)
Druh dokumentu: article
ISSN: 1424-8247
DOI: 10.3390/ph15020226
Popis: Newly designed thiazolidine-2,4-diones 3–7a–c were synthesized, and their anticancer activities were screened against three cancer lines. They showed potent activities against HepG2 compared to the other HCT116 and MCF-7 tumor cell lines. Compounds 7c and 6c were detected as highly effective derivatives against MCF-7 (IC50 = 7.78 and 8.15 µM), HCT116 (IC50 = 5.77 and 7.11 µM) and HepG2 (IC50 = 8.82 and 8.99 µM). The highly effective derivatives 6a–c and 7a–c were tested against VERO normal cell lines. All derivatives were evaluated for their VEGFR-2 inhibitory actions and demonstrated high to low activities, with IC50 values varying from 0.08 to 0.93 µM. Moreover, derivatives 5a–c, 6a–c and 7a–c were assessed to verify their in vitro binding affinities to PPARγ and insulin-secreting activities. Finally, docking studies were performed to explore their affinities and binding modes toward both VEGFR-2 and PPARγ receptors.
Databáze: Directory of Open Access Journals
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