Synthesis of Oxazole–Tetrahydropyran Hybrids and Study on Their Antiproliferative Activity Against Human Tumour Cells

Based on a previously prepared lead compound, a new series of hybrid compounds was prepared and tested against six human tumour cell lines. These new triazole linked tetrahydropyran–oxazole hybrids were prepared evaluating the impact of the LogP for the proposed modifications. The compounds exhibited good antiproliferative results when compared with standards cisplatin and 5-fluorouracil. A series of triazole linked tetrahydropyran–oxazole hybrids was synthesized based on a previously reported lead compound with selective antiproliferative activity against human tumour cell lines. The series was prepared to evaluate the impact of LogP and different modifications in the activity, and the new compounds were assayed against A549, HBL-100, HeLa, SW1573, T-47D, and WiDr cell lines. Also, the potentiality to be P-gp substrate was tested. The compounds exhibited good antiproliferative results when compared with the standards cisplatin and 5-fluorouracil. In silico studies to evaluate pharmacokinetic properties using pkCSM software were also carried out.

Bibliographic Details

Main Authors:	Quintana, Vanesa, González-Bakker, Aday, Padrón, Juan I., Martín, Víctor S., Padrón, José M., Davyt, Danilo, Valdomir, Guillermo
Other Authors:	Alexander von Humboldt Foundation
Format:	artículo biblioteca
Language:	English
Published:	John Wiley & Sons 2022-08-11
Subjects:	Antiproliferative activity, click Chemistry, LogP, oxazole, tetrahydropyran,
Online Access:	http://hdl.handle.net/10261/279160 http://dx.doi.org/10.13039/501100011033 http://dx.doi.org/10.13039/100005156 http://dx.doi.org/10.13039/501100000780
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