185457-34-5Relevant academic research and scientific papers
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines
Ge, Yang,Yang, Haijun,Wang, Changyuan,Meng, Qiang,Li, Lei,Sun, Huijun,Zhen, Yuhong,Liu, Kexin,Li, Yanxia,Ma, Xiaodong
, p. 765 - 772 (2016/12/27)
A family of phosphoryl-substituted diphenylpyrimidine derivatives (Pho-DPPYs) were synthesized and biologically evaluated as potent BTK inhibitors in this study. Compound 7b was found to markedly inhibit BTK activity at concentrations of 0.82?nmol/L, as well as to suppress the proliferations of B-cell leukemia cell lines (Ramos and Raji) expressing high levels of BTK at concentrations of 3.17?μM and 6.69?μM. Moreover, flow cytometry analysis results further indicated that 7b promoted cell apoptosis to a substantial degree. In a word, compound 7b is a promising BTK inhibitor for the treatment of B-cell lymphoblastic leukemia.
Phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with enhanced activity against pancreatic cancer cell lines
Liu, He,Wu, Bin,Ge, Yang,Huang, Jiaxin,Song, Shijie,Wang, Changyuan,Yao, Jihong,Liu, Kexin,Li, Yanxia,Li, Yongming,Ma, Xiaodong
, p. 6313 - 6321 (2017/11/16)
A family of phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) were synthesized as potent focal adhesion kinase (FAK) inhibitors. The PA-DPPY derivatives could significantly inhibit the FAK enzymatic activity at concentrations lower than 10.69 nM. Among them, compounds 7a and 7e were two of the most active FAK inhibitors, possessing IC50 values of 4.25 nM and 4.65 nM, respectively. In particular, compound 7e also displayed strong activity against AsPC cell line, with an IC50 of 1.66 μM, but show low activity against the normal HPDE6-C7 cells (IC50 > 20 μM), indicating its low cell cytotoxicity. Additionally, flow cytometry analysis showed that after treatment with 7e (8 μM, 72 h), both AsPC and Panc cells growth were almost totally inhibited, with a cell viability rate of 16.8% and 18.1%, respectively. Overall, compound 7e may be served as a valuable FAK inhibitor for the treatment of pancreatic cancer.
Synthetic Strategy and Performances of a UV-Curable Poly Acryloyl Phosphinate Flame Retardant by Carbene Polymerization
Yu, Jia,Li, Minglei,Yu, Yong,Gao, Yanjing,Liu, Jiancheng,Sun, Fang
, p. 1958 - 1970 (2015/12/12)
A route to synthesize poly ethyl (4-acrylamidebenzyl) phosphinate (PPAC) was discussed and the optimal route was determined. Diethyl benzylphosphonate was synthesized by Arbuzov reaction, then, a nitryl was introduced onto the aromatic ring by the nitration reaction of ethyl benzylphosphonate. Subsequently the carbene polymerization of the product was carried out. Finally, the nitryls were reduced and amidated to introduce the acryloyl group into the prepolymer to obtain the target product (PPAC). PPAC can rapidly photopolymerize under UV light irradiation. The addition of PPAC decreased the smoke production rate (SPR), CO2 production (CO2P), and CO production (COP) of the UV-cured resin.
Catalytic antibody regulated prodrug therapy
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, (2008/06/13)
Catalytic antibodies capable of catalysing activation of a carbamate (-O-CO-NH-) containing prodrug suitable for Antibody Directed Abzyme Prodrug Therapy (ADAPT) by catalysing breakdown of the prodrug at the carbamate position by a non-spontaneous reaction mechanism. The non-spontaneous reaction preferably has a BAc2 mechanism and the prodrug is a preferably a nitrogen mustard aryl carbamate. The invention also includes relevant immunogens, screens for catalytic activity using short transition state analogues and ADAPT systems.
