Holota, S; Kryshchyshyn, A; Derkach, H; Trufin, Y; Demchuk, I; Gzella, A; Grellier, P; Lesyk, R in [Holota, Serhii; Kryshchyshyn, Anna; Trufin, Yaroslava; Demchuk, Inna; Lesyk, Roman] Danylo Halytsky Lviv Natl Med Univ, Dept Pharmaceut Organ & Bioorgan Chem, 69 Pekarska, UA-79010 Lvov, Ukraine; [Derkach, Halyna] Ivano Frankivsk Natl Med Univ, Dept Chem, 2 Halytska, UA-76018 Ivano Frankivsk, Ukraine; [Gzella, Andrzej] Poznan Univ Med Sci, Dept Organ Chem, Grunwaldzka 6, PL-60780 Poznan, Poland; [Grellier, Philippe] CNRS, MNHN, UMR 7245, Team APE,Natl Museum Nat Hist, CP 52,57 Rue Cuvier, F-75005 Paris, France; [Lesyk, Roman] Univ Informat Technol & Management Rzeszow, Fac Med, Dept Publ Hlth Dietet & Lifestyle Disorders, Sucharskiego 2, PL-35225 Rzeszow, Poland; [Holota, Serhii] Lesya Ukrainka Eastern European Natl Univ, Dept Organ Chem & Pharm, Volya Ave 13, UA-43025 Lutsk, Ukraine published Synthesis of 5-enamine-4-thiazolidinone derivatives with trypanocidal and anticancer activity in 2019.0, Cited 46.0. Recommanded Product: 61-82-5. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.
A series of novel 2-(5-aminomethylene-4-oxo-2-thioxothiazolidin-3-yl)-3-phenylpropionic acid ethyl esters has been synthesized. Target compounds were evaluated for their trypanocidal activity towards Trypanosoma brucei brucei and Trypanosoma brucei gambiense. Several hit-compounds (8, 10, 12) inhibited growth of the parasites at sub-micromolar concentrations (IC50 0.027-1.936 mu M) and showed significant selectivity indices (SI= 108-1396.2) being non-toxic towards the human primary fibroblasts. The screening of anticancer activity in vitro within NCI DTP protocol allowed to identify active 2-(5-{[5-(2,4-dichlorobenzyl)-thiazol-2-ylamino]methylene}- 4-oxo-2-thioxothiazolidin-3-yl)-3-phenylpropionic acid ethyl ester 14 that demonstrated inhibition against all 59 human tumor cell lines with the average GI(50) value of 2.57 mu M. It was established that the activity type (antitrypanosomal or anticancer) as well as its level depends on the character of enamine fragment in the C5 position of thiazolidinone core.
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Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics