- Imidazo[1,2-a]pyridines linked with thiazoles/thiophene motif through keto spacer as potential cytotoxic agents and NF-κB inhibitors
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A series of new imidazo[1,2-a]pyridine linked with thiazole/thiophene motif through a keto spacer were synthesized and tested for their cytotoxic potential against three human cancer cell lines including A549, HeLa and U87-MG using MTT assay. Compounds A2
- Vasu, Kamala K.,Digwal, Chander Singh,Pandya, Amit N.,Pandya, Dhaivat H.,Sharma, Jayesh A.,Patel, Sneha,Agarwal, Milee
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- Convenient synthesis of novel phenylpyrimido[1,2-c]-thienopyrimidinones as IL-6/STAT3 inhibitors
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New phenylpyrimido[1,2-c]thienopyrimidinones 4A and 4B were easily prepared in good yields by the one-pot reaction of formamidine derivatives 2 of 4-aminothienopyrimidine 1 with phenylacetyl chlorides. The application of this convenient and reliable method could be used for the synthesis of a variety of pyrimido[1,2-c]thienopyrimidinone derivatives of biological importance. Some of the compounds synthesized showed strong IL-6/STAT3 inhibition.
- Park, Jae Hoo,Hong, So Young,Kim, Jungah,Lee, Hyuck Joo,Lee, Hyun Ho,Kim, Ka Young,Lee, Seung Woong,Oh, Hyun-Mee,Rho, Mun-Chul,Lee, Beom-Gyu,Song, Yang-Heon
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Read Online
- Preparation method of 6-bromoimidazo[1.2-a]pyridine-3-formaldehyde
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The invention relates to a preparation method of 6-bromoimidazo[1.2-a]pyridine-3-formaldehyde. The method comprises the following steps: 1, adding 2-amino-5-bromopyridine and N,N-dimethylformamide dimethyl acetal into a reactor to react, and stirring to react to obtain an N,N-dimethyl-N'-2-(5-bromo-pyridine)yl-formamidine intermediate; 2, adding the N,N-dimethyl-N'-2-(5-bromo-pyridine)yl-formamidine intermediate obtained in the step 1 into a solvent, adding chloroacetaldehyde, and carrying out a reaction to obtain a solid mixture; 3, dissolving the solid mixture in ethyl acetate, washing withwater and saturated edible salt water, drying with anhydrous sodium sulfate, filtering, and removing ethyl acetate to obtain a 6-bromoimidazo[1.2-a]pyridine-3-formaldehyde crude product; and 4, recrystallizing the 6-bromoimidazo[1.2-a]pyridine-3-formaldehyde crude product, and filtering to obtain a 6-bromoimidazo[1.2-a]pyridine-3-formaldehyde pure product. According to the preparation method, thereaction raw materials are easy to obtain, the price is reasonable, the reaction conditions are mild, operation is easy, aftertreatment is simple, and the product is stable in quality and high in purity.
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Paragraph 0027-0040
(2021/01/29)
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- SUBSTITUTED IMIDAZOLES FOR THE INHIBITION OF TGF-BETA AND METHODS OF TREATMENT
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This disclosure relates to low molecular weight substituted imidazoles that inhibit the TGF-b signaling pathway. More specifically, this disclosure relates to methods of using said imidazoles for the treatment of diseases related to the TGF-b signaling pathways including, but not limited to, atherosclerosis, Marfan syndrome, Loeys-Dietz syndrome, obesity, diabetes, multiple sclerosis, keratoconus, idiopathic pulmonary fibrosis, Alzheimer's Disease, chronic kidney disease, and scleroderma.
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Paragraph 0052
(2020/03/15)
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- Prospective evaluation and success of a machine learning hit-to-lead drug development program against phosphatidylinositol 3-kinase α
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As a result of the rapidly increasing cost of drug development, efficient methods for early identification of compounds with a high probability of clinical success are needed. Herein, we describe a cheminformatics protocol which dramatically increases quality candidate identification and should reduce the attrition rate of compounds entering the clinic, increasing the cost-effectiveness of drug development. Against the oncology target phosphatidylinositol 3-kinase α, all five compounds synthesized from the protocol were found to have low nanomolar activity. We therefore propose that our protocol can be used as a tool for reducing the synthetic burden required for hit-to-lead optimization.
- Kaiser, Thomas M.,Dentmon, Zackery W.,Burger, Pieter B.,Shi, Qi,Snyder, James P.,Du, Yuhong,Fu, Haian,Liotta, Dennis C.
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- Metal-Free Aerobic Oxidative Selective C-C Bond Cleavage in Heteroaryl-Containing Primary and Secondary Alcohols
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A transition-metal-free aerobic oxidative selective C-C bond-cleavage reaction in primary and secondary heteroaryl alcohols is reported. This reaction was highly efficient and tolerated various heteroaryl alcohols, generating a carboxylic acid derivative and a neutral heteroaromatic compound. Experimental studies combined with density functional theory calculations revealed the mechanism underlying the selective C-C bond cleavage. This strategy also provides an alternative simple approach to carboxylation reaction.
- Xia, Anjie,Qi, Xueyu,Mao, Xin,Wu, Xiaoai,Yang, Xin,Zhang, Rong,Xiang, Zhiyu,Lian, Zhong,Chen, Yingchun,Yang, Shengyong
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supporting information
(2019/05/07)
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- PHOSPHOTIDYLINOSITOL 3-KINASE INHIBITORS
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This disclosure relates to phosphoinositide 3-kinases (PI3Ks) inhibitors such as N-(5-(imidazo[1,2-a]pyridin-6-yl)pyridin-3-yl)sulfonamide derivatives and uses related thereto. In certain embodiments, the disclosure relates to methods of treating PI3K associated diseases or conditions comprising administering an effective amount of a compound disclosed herein to a subject in need thereof. In certain embodiments, the subject is at risk of, exhibiting symptoms of, suffering from, or diagnosed with cancer or a hematological malignancy.
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Page/Page column 43
(2017/12/05)
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- TGF-Beta Inhibitors
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Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.
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Paragraph 0984-0985
(2016/09/26)
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- AMIDO-BENZYL SULFONE AND SULFOXIDE DERIVATIVES
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The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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Page/Page column 140; 141
(2013/09/12)
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- PYRIDINYL AND PYRIMIDINYL SULFOXIDE AND SULFONE DERIVATIVES
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Disclosed are certain pyridinyl and pyrimidinyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds and methods of treatment using such compounds.
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Page/Page column 92
(2013/09/12)
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- AMIDO-BENZYL SULFONE AND SULFONAMIDE DERIVATIVES
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Disclosed are certain amido-benzyl sulfone and sulfonamide compounds, pharmaceutical compositions comprising such compounds, land methods of treatment using such compounds.
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Page/Page column 67
(2013/09/12)
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- AMIDO-BENZYL SULFOXIDE DERIVATIVES
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The present invention relates to certain amido-benzyl sulfoxide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment of an NAMPT-mediated disease or condition in a subject, selected from solid or liquid tumor, rheumat
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Paragraph 0205
(2013/09/12)
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- ALKYL-AND DI-SUBSTITUTED AMIDO-BENZYL SULFONAMIDE DERIVATIVES
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The present invention relates to certain alkyl- and di-substituted amido-benzyl sulfonamide compounds, pharmaceutical compositions comprising such compounds, and to methods of treatment of NAMPT-mediated disorders, such as diabetes, rheumatoid arthritis,
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Paragraph 0213
(2013/09/12)
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- New adenosine receptor ligands and uses thereof
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The present invention provides new compounds with high affinity for adenosine A2A receptors. It also provides antagonists of adenosine A2A receptors and their use as medicaments for the treatment and/or prophylaxis of diseases and di
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Page/Page column 14
(2010/08/07)
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- PYRIDOSULFONAMIDE DERIVATIVES AS PI3 KINASE INHIBITORS
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Invented is a method of inhibiting the activity/function of PB kinases using pyridosulfonamide derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridosulfonamide derivatives.
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Page/Page column 65
(2009/05/30)
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- CYCLOHEXYLALANINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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The present invention is directed to novel cyclohexylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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Page/Page column 66
(2010/02/15)
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- PHENYLALANINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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