39213-05-3Relevant academic research and scientific papers
Synthesis, biological evaluation, and physicochemical property assessment of 4-substituted 2-phenylaminoquinazolines as Mer tyrosine kinase inhibitors
Wang, Sheng-Biao,Cui, Mu-Tian,Wang, Xiao-Feng,Ohkoshi, Emika,Goto, Masuo,Yang, De-Xuan,Li, Linna,Yuan, Shoujun,Morris-Natschke, Susan L.,Lee, Kuo-Hsiung,Xie, Lan
, p. 3083 - 3092 (2016)
Current results identified 4-substituted 2-phenylaminoquinazoline compounds as novel Mer tyrosine kinase (Mer TK) inhibitors with a new scaffold. Twenty-one 2,4-disubstituted quinazolines (series 4-7) were designed, synthesized, and evaluated against Mer
Discovery and SAR of Novel Disubstituted Quinazolines as Dual PI3Kalpha/mTOR Inhibitors Targeting Breast Cancer
Al-Ashmawy, Aisha A. K.,Elokely, Khaled M.,Perez-Leal, Oscar,Rico, Mario,Gordon, John,Mateo, George,Omar, Abdelsattar M.,Abou-Gharbia, Magid,Childers, Wayne E.
, p. 2156 - 2164 (2020)
The dual PI3Kα/ m TOR inhibitors represent a promising molecularly targeted therapy for cancer. Here, we documented the discovery of new 2,4-disubstituted quinazoline analogs as potent dual PI3Kα/sm TOR inhibitors. Our structure based chemistry endeavor yielded six excellent compounds 9e, 9f, 9g, 9k, 9m, and 9o with single/double digit nanomolar IC50 values against both enzymes and acceptable aqueous solubility and stability to oxidative metabolism. One of those analogs, 9m, possessed a sulfonamide substituent, which has not been described for this chemical scaffold before. The short direct synthetic routes, structure-Activity relationship, in vitro 2D cell culture viability assays against normal fibroblasts and 3 breast cancer cell lines, and in vitro 3D culture viability assay against MCF7 cells for this series are described.
Synthesis of novel 1,5-disubstituted pyrrolo[1,2-: A] quinazolines and their evaluation for anti-bacterial and anti-oxidant activities
Kazemi, Shaghayegh Sadat,Keivanloo, Ali,Nasr-Isfahani, Hossein,Bamoniri, Abdolhamid
, p. 92663 - 92669 (2016)
A new series of 1,5-disubstituted pyrrolo[1,2-a]quinazoline derivatives were prepared from 2-chloro-4-substituted quinazolines, propargyl alcohol, and secondary amines through novel multi-component reactions. These one-pot reactions, carried out in the presence of a palladium-copper catalyst, provide an efficient method for the synthesis of functionalized pyrrolo[1,2-a]quinazolines in good-to-high yields. A number of synthesized compounds were screened for their in vitro anti-bacterial activity against Gram-positive and Gram-negative bacteria using a well-diffusion method. Also the anti-oxidant activity of the products was evaluated using the DPPH (2,2-diphenyl-2-picrylhydrazyl) assays.
POTENT AND SELECTIVE INHIBITORS OF CYTOCHROME P450
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Paragraph 0107, (2021/08/13)
Inhibitors of the enzyme cytochrome P450 (CYP), including 1B1 (CYP1B1), 1A1 (CYP1A1) and 19A1 (CYP19A1) are provided, and are useful in medical applications. Disclosed are highly potent and selective compounds that can be used in chemoprevention to ameliorate malignant changes induced by CYP, or to aid in treatment, including restoration of chemotherapeutic efficacy.
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase
Malagu, Karine,Duggan, Heather,Menear, Keith,Hummersone, Marc,Gomez, Sylvie,Bailey, Christine,Edwards, Peter,Drzewiecki, Jan,Leroux, Frederic,Quesada, Mar Jimenez,Hermann, Gesine,Maine, Stephanie,Molyneaux, Carrie-Anne,Le Gall, Armelle,Pullen, James,Hickson, Ian,Smith, Lisa,Maguire, Sharon,Martin, Niall,Smith, Graeme,Pass, Martin
scheme or table, p. 5950 - 5953 (2010/07/05)
We describe a novel series of potent inhibitors of the kinase activity of mTOR. The compounds display good selectivity relative to other PI3K-related kinase family members and, in cellular assays, inhibit both mTORC1 and mTORC2 complexes and exhibit good antiproliferative activity.
INHIBITORS OF THE HEDGEHOG PATHWAY
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Page/Page column 209, (2008/12/07)
The present invention is directed to a compound of Formula (I) or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula (I) to treat cancer.
MEDICINAL USE OF RECEPTOR LIGANDS
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Page/Page column 44-45, (2008/06/13)
Compounds of formula (I) are ligands of the melanin concentrating hormone-1 receptor (MCH-1 R), useful in the treatment of diseases responsive to modulation of melanin concentrating hormone (MCH) activity, for example feeding disorders and diseases for which obesity is a risk factor (I): wherein ring B is selected from specific substituted phenyl or benz-fused 5-membered N-containing heterocycles defined in the specification; R, is attached to a ring carbon of ring B, and represents hydrogen, F, Cl, or -OCH3; X is =CH- or =N-; L, is -CH2- or -CH2CH2- ; L2 is a bond, -CH2- or -CO-; R2 is H or C,-C3 alkyl, or -N(R2) L,- is selected from specific cyclic amino linker radicals as defined in the specification; ring A is selected from specific N- containing heterocyclic rings as defined in the specification.
2-4-DIAMINOQUINAZOLINES AS ANTITHROMBOTIC AGENTS
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, (2008/06/13)
2,4-diaminoquinazolines are employed as antithrombotic agents and have the following general formula: SPC1Wherein R 1 and R 2 are monovalent groups independently selected from the group consisting of EQU1 wherein R 4 and R 5 independently are selected from the group consisting of hydrogen, alkyl, and cycloalkyl, with the proviso that both R 4 and R 5 cannot be cycloalkyl, EQU2 wherein R 6, R 7, and R 8 independently are selected from the group consisting of hydrogen and alkyl, and A is a divalent organic group having from two to about six carbon atoms such that the two nitrogen atoms are separated by at least two carbon atoms, and C. heterocyclic-amino, andR 3 is a monovalent group selected from the group consisting of hydrogen, halogen, and alkyl.
