56271-33-1Relevant articles and documents
Amino acid conjugates of aminothiazole and aminopyridine as potential anticancer agents: Synthesis, molecular docking and in vitro evaluation
Ali, Tahir,Imran, Muhammad,Li, Jing Bo,Li, Shupeng,Nadeem, Humaira,Naz, Shagufta,Sarwar, Sadia,Shah, Fawad Ali,Tan, Zhen
, p. 1459 - 1476 (2021/04/19)
Purpose: The development of resistance to available anticancer drugs is increasingly becoming a major challenge and new chemical entities could be unveiled to compensate this therapeutic failure. The current study demonstrated the synthesis of 2-aminothiazole [S3 (a-d) and S5(a-d)] and 2-aminopyridine [S4(a-d) and S6(a-d)] derivatives that can target multiple cellular networks implicated in cancer development. Methods: Biological assays were performed to investigate the antioxidant and anticancer potential of synthesized compounds. Redox imbalance and oxidative stress are hallmarks of cancer, therefore, synthesized compounds were preliminarily screened for their antioxidant activity using DPPH assay, and further five derivatives S3b, S3c, S4c, S5b, and S6c, with significant antioxidant potential, were selected for investigation of in vitro anticancer potential. The cytotoxic activities were evaluated against the parent (A2780) and cisplatin-resistant (A2780CISR) ovarian cancer cell lines. Further, Molecular docking studies of active compounds were performed to determine binding affinities. Results: Results revealed that S3c, S5b, and S6c displayed promising inhibition in cisplatin-resistant cell lines in comparison to parent cells in terms of both resistance factor (RF) and IC50 values. Moreover, S3c proved to be most active compound in both parent and resistant cell lines with IC50 values 15.57 μM and 11.52 μM respectively. Our docking studies demonstrated that compounds S3c, S5b, and S6c exhibited significant binding affinity with multiple protein targets of the signaling cascade. Conclusion: Anticancer activities of compounds S3c, S5b, and S6c in cisplatin-resistant cell lines suggested that these ligands may contribute as lead compounds for the development of new anticancer drugs.
NOVEL TRF1 MODULATORS AND ANALOGUES THEREOF
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, (2020/03/26)
Novel TRF1 modulators and analogues thereof. There is provided compounds of Formula I, wherein R, R1, R2 and X have meanings written in the description. Such compounds are useful as TRF1 inhibitors and, for that reason, as medicaments, in the treatment of cancer, particularly high cancer stem cell cancer like glioblastoma and lung cancer, and can be also useful for the development of additional TRF1 inhibitors and increasing knowledge about TRF1 activity.
Kinetic investigation of the cyclopropanation process of fullerene C60 by halogenmethyl ketones under the conditions of the Bingel reaction
Biglova, Yulya N.,Garifullin, Rustem N.,Mustafin, Akhat G.,Sakhautdinov, Ilshat M.,Sakhautdinova, Gulnaz F.
, p. 7277 - 7285 (2020/06/18)
The kinetics of the Bingel reaction with halogenmethyl ketones and C60 fullerene has been studied in streaming mode by sampling the reaction mixture at different time intervals and separating the components using HPLC. A quantum-chemical simulation of this cyclopropanation process has been carried out with the DFT method. The activation parameters of the cycloaddition process were determined theoretically and experimentally and correlated with each other. It has been revealed that the use of chloromethyl ketone as the cyclopropanation agent is preferable to its brominated analogue, and a two-fold excess of the substrate with respect to fullerene is the best option for the selective synthesis of mono-adducts.
