- The novel behaviour of dialkyl phosphites toward 1,4-benzoquinone monoimines
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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
- Boulos, Leila Sadek,Arsanious, Mona Hizkial Nasr
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- Design, synthesis and biological evaluation of sulfonamide-substituted diphenylpyrimidine derivatives (Sul-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with antitumor activity
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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.
- Qu, Menghua,Liu, Zhihao,Zhao, Dan,Wang, Changyuan,Zhang, Jianbin,Tang, Zeyao,Liu, Kexin,Shu, Xiaohong,Yuan, Hong,Ma, Xiaodong
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p. 3989 - 3996
(2017/07/05)
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- Reaction of N-sulfonyl derivatives of 1,4-benzoquinone monoimine with substituted hydrazines
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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
- Konovalova,Avdeenko,Goncharova,D’yakonenko,Shishkina
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p. 644 - 649
(2016/07/06)
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- Reaction of N-sulfonyl-1,4-benzoquinone imines with sodium azide
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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
- Konovalova,Avdeenko,Shelyazhenko,Pirozhenko,Mikhailichenko,Yusina
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- PROCESS FOR SYNTHESIZING KETO-BENZOFURAN DERIVATIVES
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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.
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Paragraph 0221-0224
(2014/02/16)
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- 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
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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.
- Xu, Fuming,Zhang, Lei,Jia, Yuping,Wang, Xuejian,Li, Xiaoguang,Wen, Qingli,Zhang, Yingjie,Xu, Wenfang
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p. 191 - 200
(2013/10/01)
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- KETOBENZOFURAN DERIVATIVES, METHOD FOR SYNTHESIZING SAME, AND INTERMEDIATES
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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.
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Paragraph 0224-0228
(2013/03/26)
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- DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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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.
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Paragraph 0980
(2013/04/10)
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- DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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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.
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Page/Page column 252; 253
(2013/04/13)
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- Design, synthesis, and in vitro antitumor evaluation of novel phenylaminopyrimidine derivatives
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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
- Zheng, Youguang,Zheng, Ming,Liu, Yi,Xue, Yunsheng,Zhang, Ling,An, Lin,Liu, Ling,Ji, Min
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p. 340 - 350
(2013/07/28)
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- Synthesis and SAR of selective small molecule neuropeptide y Y2 receptor antagonists
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Highly potent and selective small molecule neuropeptide Y Y2 receptor antagonists are reported. The systematic SAR exploration of a hit molecule N-(4-ethoxyphenyl)-4-[hydroxy(diphenyl)methyl]piperidine-1-carbothioamide, identified from HTS, led to the discovery of highly potent NPY Y2 antagonists 16 (CYM 9484) and 54 (CYM 9552) with IC50 values of 19 nM and 12 nM respectively.
- Mittapalli, Gopi Kumar,Vellucci, Danielle,Yang, Jun,Toussaint, Marion,Brothers, Shaun P.,Wahlestedt, Claes,Roberts, Edward
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scheme or table
p. 3916 - 3920
(2012/07/03)
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- Synthesis and thiocyanation of N-Alkyl(trifluoromethyl)sulfonyl 1,4-benzoquinone monoimines
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New N-alkyl(trifluoromethyl)sulfonyl 1,4-benzoquinone monoimines were synthesized, and their thiocyanation gave 5-alkyl(trifluoromethyl)sulfonylamino- 1,3-benzoxathiol-2-ones. An intermediate thiocyanation product, 5-trifluoromethylsulfonylamino-1,3-benzo
- Avdeenko,Konovalova,Mikhailichenko,Shelyazhenko,Pirozhenko,Yagupol'skii
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experimental part
p. 510 - 519
(2011/07/29)
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- Synthesis of 5-substituted 2,3-dihydrobenzofurans in a one-pot oxidation/cyclization reaction
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Variously substituted 2,3-dihydrobenzofurans have been synthesized according to a sequential one-pot oxidation/cyclization procedure between para-aminophenol derivatives and an azadiene.
- Baragona, Fabien,Lomberget, Thierry,Duchamp, Christian,Henriques, Natali,Lo Piccolo, Eugenio,Diana, Patrizia,Montalbano, Alessandra,Barret, Roland
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experimental part
p. 8731 - 8739
(2011/12/02)
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- CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS
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The present invention relates to compounds useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).
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Page/Page column 11-12
(2009/06/27)
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- CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS
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The present invention relates to compounds useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acq
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Page/Page column 13
(2009/06/27)
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- CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS
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The present invention relates to compounds useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).
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Page/Page column 13
(2009/06/27)
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- HETEROCYCLIC BETA-3 ADRENERGIC RECEPTOR AGONISTS
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This invention provides compounds of Formula I having the structure U, V, W, X, and Y are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.
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- Serine peptidase modulators
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The present invention relates to new compounds having modulatory (inhibitory and stimulatory) activity on serine peptidases and proteases in general and dipeptidyl peptidase IV, prolyl oligopeptidase (PO), dipeptidyl peptidase II (DPP II), fibroblast activation protein α (FAPα), lysosomal Pro—X carboxypeptidase and elastase in particular. These new compounds can be used for the treatment of a variety of disease states in which these peptidases are involved.
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- A convenient reductive deamination (hydrodeamination) of aromatic amines
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Reductive deamination (hydrodeamination) of aromatic amines can be conveniently carried out by amination of the corresponding arylamine methanesulfonamides using chloroamine under alkaline conditions. The intermediate aryl methanesulfonylhydrazines directly eliminate methanesulfinic acid, affording diazenes which extrude nitrogen affording the desired deaminated products. Both sulfonamide formation and reduction reactions occur in high yield and are compatible with a variety of functional groups.
- Wang,Guziec Jr.
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p. 8293 - 8296
(2007/10/03)
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- Structure-activity relationship of diaryl phosphonate esters as potent irreversible dipeptidyl peptidase IV inhibitors.
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The previously reported diphenyl 1-(S)-prolylpyrrolidine-2(R, S)-phosphonate (5) was used as a lead compound for the development of potent and irreversible inhibitors of dipeptidyl peptidase IV (DPP IV, EC 3.4.14.5). The synthesis of a series of diaryl 1-
- Belayev, Alexander,Zhang, Xuemei,Augustyns, Koen,Lambeir, Anne-Marie,Meester, Ingrid De,et al.
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p. 1041 - 1052
(2007/10/03)
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- Reactions of Phosphites with 1,4-Benzoquinone Monoimines
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Trimethyl phosphite (2a) reacts with N-(phenylsulfonyl)-1,4-benzoquinone monoimine (1a) to give the respective phosphonate 3c, phosphates 3d, 3e and the alkylated products 3a and 3b.The reaction of triethyl phosphite (2b) with the same quinone imine 1a yi
- Boulos, Leila Sadek,Hennawy, Ibtisam Tadros,Arsanious, Mona Hazkial Nasr
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p. 351 - 354
(2007/10/02)
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- DERIVATIVES OF 3-AMINOPROPANE-1,2-DIOL
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Derivatives of 3-aminopropane-1,2-diol of the formula STR1 in which Ar represents optionally substituted aryl,n represents the number 0 or 1, andalk represents alkylene having 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom, or, if n is zero, the phenyl radical, being separated from one another by at least two carbon atoms, andR 1 and R. sub.2, independently of one another, each represents hydrogen or lower alkyl, or together they represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene,and salts of such compounds, processes for their manufacture, medicaments containing the new compounds and their use for the treatment of Angina pectoris and cardiac arrhythmia, and as blood pressure-reducing agents, as well as for the treatment of reactive or endogenic states of depression.
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- Derivatives of 3-aminopropane-1,2-diol
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Derivatives of 3-aminopropane-1,2-diol of the formula STR1 in which Ar represents optionally substituted aryl, n represents the number 0 or 1, and alk represents alkylene having 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom, or, if n is zero, the phenyl radical, being separated from one another by at least two carbon atoms, and R1 and R2, independently of one another, each represents hydrogen or lower alkyl, or together they represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene, and salts of such compounds, processes for their manufacture, medicaments containing the new compounds and their use for the treatment of Angina pectoris and cardiac arrhythmia, and as blood pressure-reducing agents, as well as for the treatment of reactive or endogenic states of depression.
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