New indazole-indolizine-triazine hybrid molecules with farnesyltransferase inhibitory activity

Autor: Liliana Ciurlă-Lucescu, Elena Bîcu, Dalila Belei, Alina Ghinet
Jazyk: angličtina
Rok vydání: 2024
Předmět:
Zdroj: Results in Chemistry, Vol 7, Iss , Pp 101451- (2024)
Druh dokumentu: article
ISSN: 2211-7156
DOI: 10.1016/j.rechem.2024.101451
Popis: A new series of indazole-indolizine-triazine hybrid molecules was obtained by [3 + 2] cycloaddition reaction between newly synthesized nitrogen ylides with indazole skeleton and previously reported dipolarophile 2‐ethynyl‐4,6‐dimethoxy‐1,3,5‐triazine and fully characterized. The biological evaluation of hybrids revealed good antitumor growth inhibitory activity against UO-31 renal cancer cell line for the (1H-indazole-1-yl)(1-(4,6-dimethoxy-1,3,5-triazin-2-yl)-7-methylindolizin-3-yl)methanone derivative 7a. Also, for the same compound, a moderate farnesyltransferase inhibitory activity (IC50 = 52.50 ± 16.07 µM) was observed. However, the best result as farnesyltransferase inhibitor of the series was registered for the 5-bromoindazole substituted analogue 7e (IC50 = 27.08 ± 4.93 µM).
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