N. S. Volkova, A. A. Larenkov, N. S. Boutakova, E. K. Beloglazkina, A. E. Machulkin, “Synthesis of a pteroic-based conjugate with ibuprofen moiety and macrocyclic chelator DOTA-GA”, Mendeleev Commun., 2025, Volume 35, Issue 6,Pages <nobr>670

Communications

Synthesis of a pteroic-based conjugate with ibuprofen moiety and macrocyclic chelator DOTA-GA

N. S. Volkova^a, A. A. Larenkov^b, N. S. Boutakova^a, E. K. Beloglazkina^a, A. E. Machulkin^a

^a Department of Chemistry, M. V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation
^b Burnasyan Federal Medical Biophysical Center of Federal Medical Biological Agency, 123098 Moscow, Russian Federation

Abstract: Conjugate containing fragments of pteroic acid, anti-inflammatory drug ibuprofen, macrocyclic chelator DOTA-GA and (His-Glu)₂ moiety has been synthesized. Key structural motifs of this compound were introduced to optimize the pharmacokinetic characteristics of the pteroic acid-based conjugate. The complexation of the conjugate with radioactive lutetium-177 provided radiochemical yield of >99% and radiochemical purity of 97.6%.

Keywords: folate receptors, conjugates, delivery, peptide, pteroic acid, peptide synthesis, DOTA-GA.

Received: 14.03.2025
Accepted: 04.07.2025

Language: English

DOI: 10.71267/mencom.7764

	*Supplementary materials:*
		Supplementary_data_1.pdf	3.2 Mb