Results 111 to 120 of about 5,363,495 (332)

Synthesis, Tautomeric States and Crystal Structure of (Z)-Ethyl 2-Cyano-2-(3H-Quinazoline-4-ylidene) Acetate and (Z)-Ethyl 2-Cyano-2-(2-Methyl-3H-Quinazoline-4-ylidene) Acetate

Molecules, 2005
The new compounds (Z)-ethyl 2-cyano-2-(3H- and 2-methyl-3H-quinazoline-4-ylidene) acetate (1 and 2, respectively) were synthesized by multi-step reactions.
K Shakhidoyatov, N. Abdullaev, B. Tashkhodjaev, K. Turgunov, A. Tojiboev, B. Rasulev, M. Tulyasheva   +6 more
doaj   +1 more source

Aza-Peptide Epoxides:  A New Class of Inhibitors Selective for Clan CD Cysteine Proteases

, 2016
Aza-peptide epoxides, a new class of irreversible protease inhibitors, are specific for the clan CD cysteine proteases. The inhibitors have second-order rate constants up to 105 M-1 s-1, with the most potent epoxides having the S,S stereochemistry.
Karen Ellis James (2439814), Zhao Zhao Li (2268157), Guy S. Salvesen (182933), Alan J. Barrett (3016326), Juliana L. Asgian (2001355), Wendy Carter (3016329), Jowita Mikolajczyk (2527192), James C. Powers (2268154)   +7 more
core   +1 more source

Quantum‐Trained AI Enables Inverse Design of Organic Frontier Orbitals at Billion‐Scale

Advanced Science, EarlyView.
Quantum‐trained AI links molecular substructures to frontier‐orbital energetics and enables interpretable screening across nearly one billion GDB‐13 molecules. By combining fragment‐ and ring‐level insights with donor–acceptor energy alignment against ITIC, the framework narrows an immense chemical space to a small set of promising candidates and ...
Yeongnam Ko, Se Jin Kim, Ki Chul Kim
wiley   +1 more source

DNA Modification by 4-Aza-3-ene-1,6-diynes:  DNA Cleavage, pH-Dependent Cytosine-Specific Interactions, and Cancer Cell Cytotoxicity^†

, 2016
The (Z)-hex-1,5-diyne-3-ene reactive core common to the enediyne antitumor antibiotics undergoes a Bergman cyclization after proper activation to afford reactive diradical intermediates that are responsible for initiating DNA cleavage.
Dalip Kumar (467427), Wendi M. David (2453752), Sean M. Kerwin (2180086), Wirote Tuntiwechapikul (2946165), Miguel Salazar (2693188)   +4 more
core   +1 more source

Chemotherapy‐Activated GSK3β‐DNMT1 Signaling Upregulates CD47 to Evade Macrophage Phagocytosis and Drive Temozolomide Resistance in Glioblastoma

Advanced Science, EarlyView.
Temozolomide treatment activates GSK3β, driving DNMT1 phosphorylation, destabilization, and CD47 promoter hypomethylation in glioblastoma. This epigenetic shift upregulates CD47, enabling TMZ‐treated GBM cells to evade macrophage phagocytosis, survive chemotherapy, and acquire resistance.
Jie Li, Shuai Ying, Yi Zhang, Jingjing Wang, Quan Wan, Lingli Gong, Daxing Xu, Zhenkun Yang, Hongnian Lu, Ying Yin, Xiangming Fang, Zhening Pu   +11 more
wiley   +1 more source

A Modular Synthesis of C5‐Sulfenyl Thiazoles via an Intermolecular Pummerer Rearrangement: An Underexplored Scaffold for Medicinal Chemistry

Angewandte Chemie, EarlyView.
Modular access to underexplored C5‐sulfenyl thiazoles via an intermolecular Pummerer rearrangement is reported. The methodology exhibits a broad functional group tolerance enabling the seamless design of trisubstituted thiazole cores bearing a sulfur handle for further elaboration.
Joe L. Smy, Theo C. Webb, Barnaby W. Greenland, S. Mark Roe, John Spencer, Storm Hassell‐Hart   +5 more
wiley   +2 more sources

A hydrogel miscible azelaic acid‐ionic liquids for the treatment of acne vulgaris: Enhanced solubility and skin retention

MedComm – Biomaterials and Applications
Azelaic acid (AzA) is a natural dicarboxylic acid used to treat acne vulgaris but is greatly limited by poor aqueous solubility. This study aims to enhance the solubility and skin retention of AzA by ionic liquids (ILs).
Zhezheng Fang, Xianzi Zheng, Yanyun Ma, Wei Wu, Yi Lu   +4 more
doaj   +1 more source

Establishment of a high-throughput detection system for DNA demethylating agents

Epigenetics, 2018
Epigenetic alterations underlie various human disorders, including cancer, and this has resulted in the development of drugs targeting epigenetic alterations.
Eriko Okochi-Takada, Naoko Hattori, Akihiro Ito, Tohru Niwa, Mika Wakabayashi, Kana Kimura, Minoru Yoshida, Toshikazu Ushijima   +7 more
doaj   +1 more source

Spiro Cyclohexadienones from the Reaction of Phenolic Enaminone Derivatives with Hypervalent Iodine Reagents

Molecules, 2000
Phenolic enamino compounds, prepared from 2-(4-hydroxyphenyl)-ethylamine and the corresponding β-keto carbonyl compounds, afford spiro cyclohexadienone derivatives on reaction with hypervalent iodine reagents.
Anastasios Varvoglis, Spyros Spyroudis, Ioannis Papoutsis, Anna Asmanidou   +3 more
doaj   +1 more source

Polyalkoxy Nitrones as Chiral Building Blocks in Asymmetric Synthesis

Molecules, 1999
Optically active nitrones derived from both aldoses and dialdoses add metallated heterocycles in a stereocontrolled way depending on the nature of the Lewis acid used as a precomplexing agent of the nitrone.
Tomás Tejero, Pedro Merino
doaj   +1 more source