New pyrazolyl-thiazolidinone/thiazole derivatives as celecoxib/dasatinib analogues with selective COX-2, HER-2 and EGFR inhibitory effects: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis, molecular modelling and ADME studies

Two new series of pyrazolyl-thiazolidinone/thiazole derivatives 16a–b and 18a–j were synthesised, merging the scaffolds of celecoxib and dasatinib. Compounds 16a, 16b and 18f inhibit COX-2 with S.I. 134.6, 26.08 and 42.13 respectively (celecoxib S.I. = 24.09). Compounds 16a, 16b, 18c, 18d and 18f in...

Whakaahuatanga katoa

Ngā taipitopito rārangi puna kōrero

Ngā kaituhi matua:	Wael A. A. Fadaly, Taha H. Zidan, Nesma M. Kahk, Fatma E. A. Mohamed, Marwa M. Abdelhakeem, Rehab G. Khalil, Mohamed T. M. Nemr
Hōputu:	Artigo
Reo:	Inglês
I whakaputaina:	Taylor & Francis Group 2023-12-01
Rangatū:	Journal of Enzyme Inhibition and Medicinal Chemistry
Ngā marau:	Pyrazole Thiazole COX-2 inhibition HER-2 inhibition EGFR inhibition
Urunga tuihono:	https://www.tandfonline.com/doi/10.1080/14756366.2023.2281262
Ngā Tūtohu:	Tāpirihia he Tūtohu Kāore He Tūtohu, Me noho koe te mea tuatahi ki te tūtohu i tēnei pūkete!