14538-46-6Relevant academic research and scientific papers
Synthesis and anticancer evaluation of certain γ-aryloxymethyl-α- methylene-γ-phenyl-γ-butyrolactones
Wang, Tai-Chi,Lee, Kuan-Han,Chen, Yeh-Long,Liou, Shorong-Shii,Tzeng, Cherng-Chyi
, p. 2773 - 2776 (1998)
Certain-γ-aryloxymethyl-α-methylene-γ-phenyl-γ-butyrolactones were synthesized and evaluated for their anticancer activity. These compounds demonstrated a strong growth inhibitory activity against leukemia cell lines but are relatively inactive against no
Antiarrhythmic Hit to Lead Refinement in a Dish Using Patient-Derived iPSC Cardiomyocytes
Cashman, John R.,Ryan, Daniel,McKeithan, Wesley L.,Okolotowicz, Karl,Gomez-Galeno, Jorge,Johnson, Mark,Sampson, Kevin J.,Kass, Robert S.,Pezhouman, Arash,Karagueuzian, Hrayr S.,Mercola, Mark
, p. 5384 - 5403 (2021/05/29)
Ventricular cardiac arrhythmia (VA) arises in acquired or congenital heart disease. Long QT syndrome type-3 (LQT3) is a congenital form of VA caused by cardiac sodium channel (INaL) SCN5A mutations that prolongs cardiac action potential (AP) and enhances INaL current. Mexiletine inhibits INaL and shortens the QT interval in LQT3 patients. Above therapeutic doses, mexiletine prolongs the cardiac AP. We explored structure-activity relationships (SAR) for AP shortening and prolongation using dynamic medicinal chemistry and AP kinetics in human-induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs). Using patient-derived LQT3 and healthy hiPSC-CMs, we resolved distinct SAR for AP shortening and prolongation effects in mexiletine analogues and synthesized new analogues with enhanced potency and selectivity for INaL. This resulted in compounds with decreased AP prolongation effects, increased metabolic stability, increased INaL selectivity, and decreased avidity for the potassium channel. This study highlights using hiPSC-CMs to guide medicinal chemistry and "drug development in a dish".
Synthesis of benzofurans from the cyclodehydration of α-phenoxy ketones mediated by Eaton’s reagent
Ma, Lin,Ma, Zhanwei,Zhang, Min,Zhou, Min
, p. 426 - 436 (2020/03/23)
Cyclodehydration of α-phenoxy ketones promoted by Eaton’s reagent (phosphorus pentoxide–methanesulfonic acid) is used to prepare 3-substituted or 2,3-disubstituted benzofurans with moderate to excellent yields under mild conditions. The method provides a facile access to benzofurans from readily available starting materials such as phenols and α-bromo ketones. The reaction is highly efficient, which is attributed to the good reactivity and fluidity of Eaton’s reagent. The reaction can be applied to prepare naphthofurans, furanocoumarins, benzothiophenes, and benzopyrans.
Synthesis and evaluation of novel α-substituted chalcones with potent anti-cancer activities and ability to overcome multidrug resistance
Riaz, Sharon,Iqbal, Maheen,Ullah, Rahim,Zahra, Rida,Chotana, Ghayoor Abbas,Faisal, Amir,Saleem, Rahman Shah Zaib
, p. 123 - 135 (2019/03/19)
A series of forty α-substituted chalcones were synthesized and screened for their antiproliferative activities against HCT116 (colorectal) and HCC1954 (breast) cancer cell lines. Compounds 5a and 5e were found to be the most potent compounds with GI5
Exogenous-oxidant-free electrochemical oxidative C-H sulfonylation of arenes/heteroarenes with hydrogen evolution
Yuan, Yong,Yu, Yi,Qiao, Jin,Liu, Pan,Yu, Banying,Zhang, Wukun,Liu, Huilin,He, Min,Huang, Zhiliang,Lei, Aiwen
supporting information, p. 11471 - 11474 (2018/10/20)
An efficient and environmentally benign electrochemical oxidative radical C-H sulfonylation of arenes/heteroarenes was developed in this work. A series of significant diarylsulfones were prepared under mild catalyst- and exogenous-oxidant-free reaction conditions, which efficiently avoid the issues of desulfonylation or over-reduction of sulfonyl groups.
Discovery of oxime-bearing naphthalene derivatives as a novel structural type of Nrf2 activators
Chang, Ken-Ming,Liang, Fong-Pin,Chen, I-Li,Yang, Shyh-Chyun,Juang, Shin-Hun,Wang, Tai-Chi,Chen, Yeh-Long,Tzeng, Cherng-Chyi
, p. 3852 - 3859 (2015/08/03)
Abstract Recent studies have demonstrated that oxidative stress insult is one of major causes of tumor formation. Therefore, identify the effective anti-oxidative agents as a preventive approach to stop cancer progression has widely explored. Although, ma
Modification and biological evaluation of novel 4-hydroxy-pyrone derivatives as non-peptidic HIV-1 protease inhibitors
He, Meizi,Yang, Ning,Sun, Chunlai,Yao, Xiaojian,Yang, Ming
experimental part, p. 200 - 209 (2012/03/10)
In this study, we have modified 4-hydroxy-pyran-2-ones, especially introduced heteroatoms (S or O) into the substituents, and detected their interactions with the binding pockets of HIV-1 protease (PR). The results indicated that the ethoxyl groups at C-2
Novel one-pot synthesis of 3-Phenylnaphtho[2,3-b]furan and 3-phenylbenzofurans under microwave irradiation and solvent-free conditions
Wang, Zhongxing,Gu, Jinzhong,Jing, Huanwang,Liang, Yongmin
experimental part, p. 4079 - 4087 (2009/12/24)
A one-pot synthesis of functionalized benzofurans has been developed via O-alkylation, carbon-carbon coupling/cyclization, and dehydration/olefination tandem reactions from phenacyl bromide and phenols under microwave irradiation and solvent-free conditio
Use of a scientific microwave apparatus for rapid optimization of reaction conditions in a monomode function and then substrate screening in a multimode function
Leadbeater, Nicholas E.,Schmink, Jason R.
, p. 6764 - 6773 (2008/02/07)
Recently, a new apparatus has become available, which aims to bring together in one unit the advantages of a monomode and a multimode microwave device. We have assessed the applicability of the apparatus toward rapid optimization of reaction conditions in a monomode function and then substrate screening in a multimode function. We have also probed the effects of differences in microwave absorptivity of reaction mixtures on the product conversions in screening multiple substrates simultaneously in a multimode microwave apparatus. We find that when the microwave absorptivity of a reaction mixture is dictated by the solvent, there is little effect on the heating profile of varying the substrate in a screening run. However, this is not the case when reactions involving non-microwave absorbant solvents are used. In this case the characteristics of the substrate can affect significantly the outcome of the reaction.
CHEMICAL COMPOUNDS
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Page 110, (2010/02/06)
Compounds of formula (I):wherein variable groups are as defined within; for use in the inhibition of 11betaHSD1 are described
