193354-13-1Relevant articles and documents
Synthesis and antiproliferative activities of isoindigo and azaisoindigo derivatives
Bouchikhi, Fadoua,Anizon, Fabrice,Moreau, Pascale
, p. 755 - 762 (2008)
In the course of structure-activity relationship studies, diversely substituted 1-(β- d-acetylatedglucopyranosyl)isoindigo derivatives were prepared from indolines. New 7′-azaisoindigo analogues were also synthesized by coupling a glycosylated isatine and a 7-azaindolin-2-one derivative. Compounds containing a 7′-azaisoindigo framework have never been described before. To get an insight into the substitution pattern required for the best biological potencies, their antiproliferative activities were evaluated toward a human buccal carcinoma cell line (KB) and two human myeloid leukaemia cell lines (K562, HL60).
Compounds for preventing or treating lipid metabolism-related diseases
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Paragraph 0585-0588, (2021/10/27)
The present invention relates to the field of biomedicines, and in particular to a structure capable of binding LC3 and a structure capable of binding a lipid droplet linked together by a covalent linkage, thereby forming a 'LC3 binding moiety - lipid dro
Synthesis, Biological, and Computational Evaluation of Novel 1,3,5-Substituted Indolin-2-one Derivatives as Inhibitors of Src Tyrosine Kinase
Kilic-Kurt, Zühal,Bakar, Filiz,?lgen, Süreyya
, p. 715 - 729 (2015/10/12)
Several substituted indolin-2-one derivatives were synthesized and evaluated for their activities against Src kinase. Several compounds showed activity against Src, with IC50 values in the low micromolar range. Among them, compound 2f showed the most significant activity with an IC50 value of 1.02 μM. Molecular docking studies have been performed for evaluation of the binding modes of compound 2f into the Src active site. The docking structure of compound 2f disclosed that the indole NH forms a hydrogen bond with the carbonyl of Met341. These results suggest that our novel compound 2f is a promising compound for the further development of indole-based drugs targeting Src kinase. A novel series of indole-2-one derivatives were synthesized and evaluated for their Src inhibitory activities. Compound 2f was found as the most promising compound with an IC50 value of 1.02 μM. Molecular docking studies were performed to disclose the binding mode for compound 2f.