23918-29-8Relevant academic research and scientific papers
Polymer complexes. LXVI, thermal, spectroscopic studies and supramolecular structure of N-[β-(ethylamino)] acrylamide polymer complexes
El-Sonbati,Diab,El-Bindary,El-Mogazy
, p. 1044 - 1057 (2016)
Novel polymeric complexes with a potentially bidentate ligand N-[β-(ethylamino)] acrylamide (EA), formed by amidation of 1,2-diaminoethane with acryloyl chloride were synthesized and characterized on the basis of elemental analyses, IR,1H NMR, UV-Vis, magnetic susceptibility measurements, ESR, molar conductance and thermal analysis. Molecular docking was used to predict the binding between EA ligand (keto and enol forms) and the receptor of prostate cancer mutant 2q7k-hormone and the receptor of breast cancer mutant 3hb5-oxidoreductase. The molecular and electronic structures of the different forms of the ligand are optimized theoretically and the quantum chemical parameters are calculated. The molar conductance data reveal that all the polymer complexes are non-electrolytes. Ligand (EA) has been shown to behave as neutral bidentate via its nitrogen atom of NH2group and nitrogen atom of NH group in polymer complexes. On the basis of electronic spectral data and magnetic susceptibility measurements, suitable geometry has been proposed for each polymeric complex. The ESR spectral data of the Cu(II) complex showed that the metal-ligand bonds have considerable covalent character. The activation energies of the degradation of the polymer complexes were calculated.
Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold
Shan, Huifang,Ma, Xinyu,Yan, Guoyi,Luo, Meng,Zhong, Xinxin,Lan, Suke,Yang, Jie,Liu, Yuanyuan,Pu, Chunlan,Tong, Yu,Li, Rui
, (2021/04/15)
Cyclin-dependent kinases 4 and 6 (CDK4/6), which are involved in dynamic regulation of cell cycle, play an indispensable role in controlling the tumor growth. Here, based on the scaffold of palbociclib, we designed and synthesized a series of covalent CDK4/6 inhibitors that targeted amino acid Thr107. The optimized compound C-13 exhibited potent in vitro anticancer activity against CDK4/6 with high selectivity over CDK4/6. Moreover, C-13 showed significant tumor growth inhibition in MDA-MB-231 tumor xenograft model (TGI of 93.49% at dose of 40 mg/kg) without causing significant weight loss and toxicity during the treatment period.
POLYMER OF GAMMA-GLUTAMYL TRANSPEPTIDASE CATALYZING HYDROLYSIS-INDUCED CHARGE REVERSAL AND ITS APPLICATION IN THE FIELD OF DRUG DELIVERY
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Paragraph 0061-0063, (2020/07/23)
This present invention relates to a polymer of γ-glutamyl transpeptidase catalyzing hydrolysis-induced charge reversal. The polymer comprises a γ-glutamyl transpeptidase-responsive element represented by Formula (I). When the polymer is used as drug carrier for anticancer drug, it can have a long circulation time in the blood, and can realize a charge reversal from negatively charged or the neutral to positively charged around the tumor blood vessel region, so that the positively charged polymer effectively penetrates deep into the tumor tissue, fast entering into the tumor cells, and greatly improves the therapeutic effect of the drug on the tumor. This overcomes the problems of slow diffusion of traditional polymer drug carriers in tumors and weak interaction with tumor cells, and has great significance in the field of anticancer treatment in the medical field.
Biphenyl compound as immunoregulator and applications of same
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Paragraph 0406-0410, (2020/03/17)
The invention relates to a biphenyl compound as the formula (I), and a preparation method and a pharmaceutical application thereof. The groups in the formula (I) are defined as the specification. Thecompound can block the interaction between PD-1/PD-L1 si
