51767-39-6Relevant articles and documents
The novel behaviour of dialkyl phosphites toward 1,4-benzoquinone monoimines
Boulos, Leila Sadek,Arsanious, Mona Hizkial Nasr
, p. 4711 - 4720 (1993)
Diethyl phosphite 2a reacts with N- (phenylsulfonyl) - 1,4 - benzoquinone monoimine 1a to give 1,4-diethyl [(2-hydroxy-5-[(phenylsulfonyl) amino ] phenyl] [sphosphonate 3a, diethyl (1-hydroxy - 4- [ ( phenylsulfonyl ) imino ] -2,5-cyclohexadiene )] phosph
Design, synthesis and biological evaluation of sulfonamide-substituted diphenylpyrimidine derivatives (Sul-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with antitumor activity
Qu, Menghua,Liu, Zhihao,Zhao, Dan,Wang, Changyuan,Zhang, Jianbin,Tang, Zeyao,Liu, Kexin,Shu, Xiaohong,Yuan, Hong,Ma, Xiaodong
, p. 3989 - 3996 (2017/07/05)
A class of sulfonamide-substituted diphenylpyrimidines (Sul-DPPYs) were synthesized to improve activity against the focal adhesion kinase (FAK). Most of these new Sul-DPPYs displayed moderate activity against the FAK enzyme with IC50 values of less than 100?nM; regardless, they could effectively inhibit several classes of refractory cancer cell lines with IC50 values of less than 10?μM, including the pancreatic cancer cell lines (AsPC-1, Panc-1 and BxPC-3), the NSCLC-resistant H1975 cell line, and the B lymphocyte cell line (Ramos cells). Results of flow cytometry indicated that inhibitor 7e promoted apoptosis of pancreatic cancer cells in a dose-dependent manner. In addition, it almost completely induced the apoptosis at a concentration of 10?μM. Compound 7e may be selected as a potent FAK inhibitor for the treatment of pancreatic cancer.
Reaction of N-sulfonyl derivatives of 1,4-benzoquinone monoimine with substituted hydrazines
Konovalova,Avdeenko,Goncharova,D’yakonenko,Shishkina
, p. 644 - 649 (2016/07/06)
Reaction direction of N-sulfonyl derivatives of 1,4-benzoquinone monoimine with substituted hydrazines depends on the redox potential of the quinone imine and on the basicity of the hydrazine. Aryl (alkyl)hydrazines of high basicity favor the reduction of
Reaction of N-sulfonyl-1,4-benzoquinone imines with sodium azide
Konovalova,Avdeenko,Shelyazhenko,Pirozhenko,Mikhailichenko,Yusina
, p. 15 - 24 (2017/01/11)
Depending on the conditions and the order of addition of the reactants, reactions of N-sulfonyl-1,4-benzoquinone imines with sodium azide afforded N-(3-azido-4-hydroxyphenyl)alkane(arene)sulfonamides, N-(3-azido-4-oxocyclohexa-2,5-dienylidene)alkane(arene
PROCESS FOR SYNTHESIZING KETO-BENZOFURAN DERIVATIVES
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Paragraph 0221-0224, (2014/02/16)
The invention relates to a process for synthesizing benzofuran derivatives, in particular dronedarone of formula (D), comprising a step of Friedel-Crafts acylation starting from a sulfonamido-benzofuran ester intermediate.
KETOBENZOFURAN DERIVATIVES, METHOD FOR SYNTHESIZING SAME, AND INTERMEDIATES
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Paragraph 0224-0228, (2013/03/26)
The present disclosure relates to ketobenzofuran derivatives of the general formula (I): as well as to a method of synthesizing the same by coupling a quinonimine and an enaminone by a Nenitzescu reaction and to the intermediates of the synthesis thereof.
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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Paragraph 0980, (2013/04/10)
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 252; 253, (2013/04/13)
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
Design, synthesis, and in vitro antitumor evaluation of novel phenylaminopyrimidine derivatives
Zheng, Youguang,Zheng, Ming,Liu, Yi,Xue, Yunsheng,Zhang, Ling,An, Lin,Liu, Ling,Ji, Min
, p. 340 - 350 (2013/07/28)
Two series of novel phenylaminopyrimidine derivatives were designed and synthesized. All target compounds were determined against the human acute monocytic leukemia cell line U937 and the human chronic myeloid leukemia cell line K562 in vitro. Some of the
Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part II
Xu, Fuming,Zhang, Lei,Jia, Yuping,Wang, Xuejian,Li, Xiaoguang,Wen, Qingli,Zhang, Yingjie,Xu, Wenfang
, p. 191 - 200 (2013/10/01)
A novel series of 4-amino-2-(thio)phenol derivatives were well synthesized. The preliminary biological test revealed that several compounds displayed high specific protein kinase and angiogenesis inhibitory activities compared with previous work mainly because of the substitution of sulfonamide structure for amide fragment. Among which, compound 5i was identified to inhibit protein kinase B/AKT (IC50 = 1.26 μM) and ABL tyrosine kinase (IC 50 = 1.50 μM) effectively. Meanwhile, compound 5i demonstrated competitive in vitro antiangiogenic activities to Pazopanib in both human umbilical vein endothelial cell (HUVEC) tube formation assay and the rat thoracic aorta rings test.