Results 11 to 20 of about 3,294 (234)

Design, Synthesis, Chemical and Biochemical Insights Into Novel Hybrid Spirooxindole-Based p53-MDM2 Inhibitors With Potential Bcl2 Signaling Attenuation [PDF]

Frontiers in Chemistry, 2021
The tumor resistance to p53 activators posed a clinical challenge. Combination studies disclosed that concomitant administration of Bcl2 inhibitors can sensitize the tumor cells and induce apoptosis.
Yasmine M. Abdel Aziz, Gehad Lotfy, Mohamed M. Said, El Sayed H. El Ashry, El Sayed H. El Tamany, Saied M. Soliman, Marwa M. Abu-Serie, Mohamed Teleb, Sammer Yousuf, Alexander Dömling, Luis R. Domingo, Assem Barakat   +11 more
doaj   +3 more sources

Synthesis, Biological and In Silico Evaluation of Pure Nucleobase-Containing Spiro (Indane-Isoxazolidine) Derivatives as Potential Inhibitors of MDM2–p53 Interaction [PDF]

Molecules, 2019
Nucleobase-containing isoxazolidines spiro-bonded to an indane core have been synthesized in very good yields by regio- and diastereoselective 1,3-dipolar cycloaddition starting from indanyl nitrones and N-vinylnucleobases by using environmentally benign
Loredana Maiuolo, Vincenzo Algieri, Beatrice Russo, Matteo Antonio Tallarida, Monica Nardi, Maria Luisa Di Gioia, Zahra Merchant, Pedro Merino, Ignacio Delso, Antonio De Nino   +9 more
doaj   +3 more sources

Asymmetric Synthesis of Spirooxindoles via Nucleophilic Epoxidation Promoted by Bifunctional Organocatalysts [PDF]

Molecules, 2018
Taking into account the postulated reaction mechanism for the organocatalytic epoxidation of electron-poor olefins developed by our laboratory, we have investigated the key factors able to positively influence the H-bond network installed inside the ...
Martina Miceli, Andrea Mazziotta, Chiara Palumbo, Elia Roma, Eleonora Tosi, Giovanna Longhi, Sergio Abbate, Paolo Lupattelli, Giuseppe Mazzeo, Tecla Gasperi   +9 more
doaj   +7 more sources

Diastereoselective Three-Component 1,3-Dipolar Cycloaddition to Access Functionalized β-Tetrahydrocarboline- and Tetrahydroisoquinoline-Fused Spirooxindoles [PDF]

Molecules
A chemselective catalyst-free three-component 1,3-dipolar cycloaddition has been described. The unique polycyclic THPI and THIQs were creatively employed as dipolarophiles, which led to the formation of functionalized β-tetrahydrocarboline- and ...
Yongchao Wang, Yu Chen, Shengli Duan, Yiyang Cao, Wenjin Sun, Mei Zhang, Delin Zhao, Donghua Hu, Jianwei Dong   +8 more
doaj   +2 more sources

Palladium-catalyzed difluorocarbene transfer enables access to enantioenriched chiral spirooxindoles [PDF]

Nature Communications
We disclose herein an unprecedented Pd-catalyzed difluorocarbene transfer reaction, which assembles a series of structurally interesting chiral spiro ketones with generally over 90% ee.
Zhiwen Nie, Keqin Wu, Xiaohang Zhan, Weiran Yang, Zhong Lian, Shaoquan Lin, Shou-Guo Wang, Qin Yin   +7 more
doaj   +2 more sources

Silica/APTPOSS anchored on MnFe2O4 as an efficient nanomagnetic composite for the preparation of spiro-pyrano [2, 3-c] chromene derivatives [PDF]

BMC Chemistry
The synthesis of Octakis [3- (3-amino propyl triethoxysilane) propyl] octa-silsesquioxane (APTPOSS), a derivative of polyhedral oligomeric silsesquioxane, was utilized to produce an efficient nanocomposite.
Samira Moein-Najafabadi, Javad Safaei-Ghomi   +1 more
doaj   +2 more sources

Deciphering Tryptophan Oxygenation: Key Modulators of 2-Oxindole Formation in MarE. [PDF]

Angew Chem Int Ed Engl
This study reveals that MarE, a heme‐dependent aromatic oxygenase, favors dioxygenation of β‐methyl‐l‐tryptophan in the absence of ascorbate and demonstrates how structural and redox tuning shifts its reactivity toward selective monooxygenation, yielding a 2‐oxindole scaffold. These findings offer new insights into enzyme‐controlled indole oxidation in
Nguyen RC, Shin I, Liu A.
europepmc   +3 more sources

In Vitro and In Silico Evaluation of Isatin-Derived Spirooxindoles as Antituberculosis Drug Candidates. [PDF]

Chem Biol Drug Des
Two compounds, A16 and A17, were active against multidrug‐resistant Mycobacterium tuberculosis isolates (PT‐12 and PT‐20), overcoming key resistance mutations in katG and rpoB, while cytotoxicity assays confirmed that they are non‐toxic. A17 exhibited the highest antituberculosis activity, with molecular docking suggesting enoyl‐[acyl‐carrier‐protein ...
de Lima FR, de Oliveira Viana J, de Castro AC, Cristiano R, Perelló MA, Czeczot AM, Bizarro CV, Machado P, Basso LA, Lima-Junior CG, Rodrigues-Junior VDS, Weber KC.   +11 more
europepmc   +2 more sources

Ultrafast and efficient continuous flow organic synthesis with a modified extruder-grinder system [PDF]

Scientific Reports
The study introduces a groundbreaking continuous system that combines an extruder and grinder to enable catalyst-free and solvent-free reactions under mild conditions.
Omid Hosseinchi Qareaghaj, Mohammad Ghaffarzadeh, Najmedin Azizi   +2 more
doaj   +2 more sources

Electrochemical Enantioselective Oxidation of Indoles via Chiral Phosphoric Acid Catalysis in Cooperation with H₃PO₄ in Aqueous Media. [PDF]

Angew Chem Int Ed Engl
A binary organic–inorganic acid cooperative catalytic system has been developed to achieve highly enantioselective electrochemical oxidative rearrangement of indoles. The use of electricity as an oxidant in this case showed several advantages including environmental benignity and improved enantiocontrol.
Tan X, Zhou Z, Shao M, Sun J.
europepmc   +2 more sources