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81.
Joseph Derosa Taeho Kang Van T. Tran Dr. Steven R. Wisniewski Dr. Malkanthi K. Karunananda Tanner C. Jankins Kane L. Xu Dr. Keary M. Engle 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2020,132(3):1217-1221
A nickel-catalyzed conjunctive cross-coupling of alkenyl carboxylic acids, aryl iodides, and aryl/alkenyl boronic esters is reported. The reaction delivers the desired 1,2-diarylated and 1,2-arylalkenylated products with excellent regiocontrol. To demonstrate the synthetic utility of the method, a representative product is prepared on gram scale and then diversified to eight 1,2,3-trifunctionalized building blocks using two-electron and one-electron logic. Using this method, three routes toward bioactive molecules are improved in terms of yield and/or step count. This method represents the first example of catalytic 1,2-diarylation of an alkene directed by a native carboxylate group. 相似文献
82.
Yuli Zhang Hieu M. Pham Jose G. Munguia-Lopez Joseph M. Kinsella Simon D. Tran 《Molecules (Basel, Switzerland)》2020,25(23)
Hydrogels have been used for a variety of biomedical applications; in tissue engineering, they are commonly used as scaffolds to cultivate cells in a three-dimensional (3D) environment allowing the formation of organoids or cellular spheroids. Egg white-alginate (EWA) is a novel hydrogel which combines the advantages of both egg white and alginate; the egg white material provides extracellular matrix (ECM)-like proteins that can mimic the ECM microenvironment, while alginate can be tuned mechanically through its ionic crosslinking property to modify the scaffold’s porosity, strength, and stiffness. In this study, a frozen calcium chloride (CaCl2) disk technique to homogenously crosslink alginate and egg white hydrogel is presented for 2.5D culture of human salivary cells. Different EWA formulations were prepared and biologically evaluated as a spheroid-like structure platform. Although all five EWA hydrogels showed biocompatibility, the EWA with 1.5% alginate presented the highest cell viability, while EWA with 3% alginate promoted the formation of larger size salivary spheroid-like structures. Our EWA hydrogel has the potential to be an alternative 3D culture scaffold that can be used for studies on drug-screening, cell migration, or as an in vitro disease model. In addition, EWA can be used as a potential source for cell transplantation (i.e., using this platform as an ex vivo environment for cell expansion). The low cost of producing EWA is an added advantage. 相似文献
83.
Mohanad A. Hussein Uyen P. N. Tran Vien T. Huynh Junming Ho Mohan Bhadbhade Herbert Mayr Thanh V. Nguyen 《Angewandte Chemie (International ed. in English)》2020,59(4):1455-1459
Tropylium bromide undergoes noncatalyzed, regioselective additions to a large variety of Michael acceptors. In this way, acrylic esters are converted into β‐bromo‐α‐cycloheptatrienylpropionic esters. The reactions are interpreted as nucleophilic attack of bromide ions at the electron‐deficient olefins and the approach of the tropylium ion to the incipient carbanion. Quantum chemical calculations were performed to elucidate the analogy to the amine‐ or phosphine‐catalyzed Rauhut–Currier reactions. Subsequent synthetic transformations of the bromo‐cycloheptatrienylated adducts are reported. 相似文献
84.
Joseph Derosa Taeho Kang Van T. Tran Steven R. Wisniewski Malkanthi K. Karunananda Tanner C. Jankins Kane L. Xu Keary M. Engle 《Angewandte Chemie (International ed. in English)》2020,59(3):1201-1205
A nickel‐catalyzed conjunctive cross‐coupling of alkenyl carboxylic acids, aryl iodides, and aryl/alkenyl boronic esters is reported. The reaction delivers the desired 1,2‐diarylated and 1,2‐arylalkenylated products with excellent regiocontrol. To demonstrate the synthetic utility of the method, a representative product is prepared on gram scale and then diversified to eight 1,2,3‐trifunctionalized building blocks using two‐electron and one‐electron logic. Using this method, three routes toward bioactive molecules are improved in terms of yield and/or step count. This method represents the first example of catalytic 1,2‐diarylation of an alkene directed by a native carboxylate group. 相似文献
85.
Van T. Tran Zi‐Qi Li Omar Apolinar Joseph Derosa Matthew V. Joannou Steven R. Wisniewski Martin D. Eastgate Keary M. Engle 《Angewandte Chemie (International ed. in English)》2020,59(19):7409-7413
We report that Ni(COD)(DQ) (COD=1,5‐cyclooctadiene, DQ=duroquinone), an air‐stable 18‐electron complex originally described by Schrauzer in 1962, is a competent precatalyst for a variety of nickel‐catalyzed synthetic methods from the literature. Due to its apparent stability, use of Ni(COD)(DQ) as a precatalyst allows reactions to be conveniently performed without use of an inert‐atmosphere glovebox, as demonstrated across several case studies. 相似文献
86.
Quach Thi Thanh Van Le Thi Vien Tran Thi Hong Hanh Phan Thi Thanh Huong Nguyen The Cuong Nguyen Phuong Thao 《Natural product research》2020,34(9):1276-1281
AbstractUsing various chromatographic separations, three new acylated flavonoid glycosides, namely barringosides G–I (1–3), were isolated from the water-soluble extract of Barringtonia racemosa branches and leaves. The structure elucidation was performed by extensive analysis of the 1D and 2D NMR and HR-QTOF-MS data. Of the isolated compounds, barringoside I (3) showed moderate inhibitory effects on LPS-induced NO production in RAW264.7 cells with an IC50 of 52.48?±?1.04?µM. 相似文献
87.
Le Hoang Vien Le Thi Hanh Tran Thi Hong Thanh Nguyen Van Nam Nguyen Hoai 《Natural product research》2020,34(8):1061-1067
AbstractFrom the MeOH extract of the Vietnamese sea cucumber Holothuria edulis, eight triterpene glycosides (1–8), including one new compound namely holothurin A5 (1), were isolated by using various chromatographic separations. Their structures were established by spectroscopic experiments including 1D, 2D NMR and HR-ESI-MS. Holothurin A5 (1) has a hydroperoxy group at C-25. To the best of our knowledge, this is the first report of this group in triterpene saponins obtained from sea cucumbers to date. In addition, the in vitro cytotoxicity against five human cancer cell lines (HepG2, KB, LNCaP, MCF7 and SK-Mel2) of all isolated compounds was also evaluated using SRB assays. 相似文献
88.
Hue Thi Buu Bui Phuong Hong Nguyen Quan Minh Pham Hoa Phuong Tran De Quang Tran Hosun Jung Quang Vinh Hong Quoc Cuong Nguyen Quy Phu Nguyen Hieu Trong Le Su-Geun Yang 《Molecules (Basel, Switzerland)》2022,27(7)
Epigenetic alterations found in all human cancers are promising targets for anticancer therapy. In this sense, histone deacetylase inhibitors (HDACIs) are interesting anticancer agents that play an important role in the epigenetic regulation of cancer cells. Here, we report 15 novel hydroxamic acid-based histone deacetylase inhibitors with quinazolinone core structures. Five compounds exhibited antiproliferative activity with IC50 values of 3.4–37.8 µM. Compound 8 with a 2-mercaptoquinazolinone cap moiety displayed the highest antiproliferative efficacy against MCF-7 cells. For the HDAC6 target selectivity study, compound 8 displayed an IC50 value of 2.3 µM, which is 29.3 times higher than those of HDAC3, HDAC4, HDAC8, and HDAC11. Western blot assay proved that compound 8 strongly inhibited tubulin acetylation, a substrate of HDAC6. Compound 8 also displayed stronger inhibition activity against HDAC11 than the control drug Belinostat. The inhibitory mechanism of action of compound 8 on HDAC enzymes was then explored using molecular docking study. The data revealed a high binding affinity (−7.92 kcal/mol) of compound 8 toward HDAC6. In addition, dock pose analysis also proved that compound 8 might serve as a potent inhibitor of HDAC11. 相似文献
89.
Dr. Tran Quang Hung Dr. Ferial Terki Dr. Souleymane Kamara Mourad Dehbaoui Prof. Salam Charar Brajalal Sinha Prof. CheolGi Kim Dr. Philippe Gandit Il'ya A. Gural'skiy Dr. Gabor Molnar Dr. Lionel Salmon Dr. Helena J. Shepherd Dr. Azzedine Bousseksou 《Angewandte Chemie (International ed. in English)》2013,52(4):1185-1188
90.
Tran Thu Ha Nguyen Hong Phong François-Xavier Le Dimet Hong Son Hoang 《Comptes Rendus Mecanique》2019,347(5):423-444
This article presents a correction method for a better resolution of the problem of estimating and predicting pollution, governed by Burgers' equations. The originality of the method consists in the introduction of an error function into the system's equations of state to model uncertainty in the model. The initial conditions and diffusion coefficients, present in the equations for pollution and concentration, and also those in the model error equations, are estimated by solving a data assimilation problem. The efficiency of the correction method is compared with that produced by the traditional method without introduction of an error function.Three test cases are presented in this study in order to compare the performances of the proposed methods. In the first two tests, the reference is the analytical solution and the last test is formulated as part of the “twin experiment”.The numerical results obtained confirm the important role of the model error equation for improving the prediction capability of the system, in terms of both accuracy and speed of convergence. 相似文献