Antitumor activity among derivatives of the 3-chloro-4-(3-hydroxyanilino) -2,5-dihydropyrrole-2,5-dione

Abstract

Синтезовано та тестовано на протипухлинну активність (in vitro) 14 похідних 3-хлоро-4-(3гідроксіаніліно)-2,5-дигідро-1Н-2,5-піролдіону з варіюванням замісників у 1 і 3 положеннях малеїмідного циклу. 10 сполук було відібрано за результатами прескринінгу і тестовано на 52 лініях ракових клітин людини. Знайдено, що 1-(2,3-дихлорфеніл)-3-хлоро-4-(3-гідроксіаніліно)-2,5-дигідро-1Н-2,5-піролдіон та 1-бензилЗ-(3-гідроксіаніліно)-4-фенілсульфаніл-2,5-дигідро-1Н-2,5-піролдіон пригнічують ріст деяких клітинних ліній пухлин із Gho < 0,5 • 10~7 та < 10~8 М.

Application and developing of iron‐doped multi‐walled carbon nanotubes (Fe/MWCNTs) as an efficient and reusable heterogeneous nanocatalyst in the synthesis of heterocyclic compounds

“…The large number of biological activities of five‐membered nitrogen heterocyclic compounds such as inhibitors of the human immunodeficiency virus (HIV) integrase, vascular endothelial growth factor receptors (VEGFR), human mitotic kinesin Eg5, CD45 protein tyrosine phosphatase and annexin A2‐S100A10 protein interaction made the synthesis of these compounds very interesting. Besides, their anti‐tumor activity as well as being useful intermediates increasingly need new investigations.…”

Nano-TiCl4/SiO2: an efficient catalyst for the one-pot synthesis of highly substituted dihydro-2-oxopyrroles

“…The optimization of formaldehyde was carried out in EtOH (entries [14][15][16][17], and the optimal amount was obtained using 3 mmol (entry 17). As can be seen in this table (entries [17][18][19], the optimum amount of the utilized TiCl 4 /SiO 2 was 0.1 g (entry 17). Nano-TiCl 4 /SiO 2 in contrast to TiCl 4 /SiO 2 showed higher yield at a shorter time and lower concentration (entries 20, 21).…”

“…Therefore, the advancement of novel strategies for the synthesis of nitrogen-containing heterocycles in a rapid and efficient method is a chief job in the heterocyclic syntheses. The application of MCRs for the synthesis of dihydro-oxopyrrole derivatives has become a significant and attractive subject in organic syntheses since these compounds possess herbicidal [17], antitumor [18], pesticidal [19], anti-HIV [20], and antibiotic properties [21] and serve as nootropic agents [22]. Natural compounds were found to contain dihydro-2-oxopyrrole motifs, such as oteromycin [23], pyrrocidine A with potent antibiotic activity [24], talaroconvolutin A [25], quinolactacin C [26], and ypaoamide [27] (Fig.…”

Hit identification of FGFR1 inhibitors using receptor-based virtual screening

“…Synthesis of derivatives of 1-phenyl-3-phenylamino-4-(phenyl)thio-1H-pyrrole-2,5-dione was performed according to our methods [23,24]. Compound 9 was prepared by reacting 3,4-dichloro-1H-pyrrole-2,5-diones with the corresponding aniline in 79 % yield.…”