Article
Chemistry, Medicinal
Pei Chen, Huachao Bin, Yan Jiao, Guifeng Lin, Yun Zhang, Anjie Xia, Zhilin Pan, Jingxin Qiao, Yinping Guo, Jingming Liu, Yangli Zhou, Linli Li
Summary: A series of 6,7-dihydro-5H-pyrrolo[3,4-d]-pyrimidine derivatives have been discovered as a new class of ATR inhibitors, with compound 5g exhibiting strong inhibition against ATR kinase and displaying good anti-tumor activity.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Review
Chemistry, Multidisciplinary
Mehul P. Parmar, Ruturajsinh M. Vala, Hitendra M. Patel
Summary: In this review article, the synthesis of 5H-pyrano[2,3-d]pyrimidine scaffolds using hybrid catalysts from 1992 to 2022 is comprehensively discussed. Various catalytic systems such as organocatalysts, metal catalysts, ionic liquid catalysts, nanocatalysts, green solvents, catalyst-/solvent-free conditions, and miscellaneous catalysts are employed. The significance of this review lies in attracting leading researchers worldwide to utilize broader catalytic applications for the development of lead molecules.
Article
Chemistry, Medicinal
Yinliang Qi, Kun Wang, Bin Long, Hao Yue, Yongshuo Wu, Dexiao Yang, Minghui Tong, Xuan Shi, Yunlei Hou, Yanfang Zhao
Summary: ATR kinase is vital for the survival of replicating cells in response to DNA single-strand breaks, and it is an attractive target for anticancer drugs based on synthetic lethality. In this study, a novel series of fused pyrimidine derivatives were designed, synthesized, and evaluated as ATR inhibitors. Compound 48f showed strong efficacy as a monotherapy against ATM kinase-deficient tumor cells and exhibited synergistic activity in combination with other drugs against different cancer cell lines. Moreover, it demonstrated favorable pharmacokinetic properties and low risk of drug-drug interactions, making it a promising compound for further investigation.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Mohamed G. Abouelenein, Abd El-Hamid A. Ismail, Asmaa Aboelnaga, Mohamed A. Tantawy, Nora M. A. El-Ebiary, Samy A. El-Assaly
Summary: An eco-friendly approach was used to synthesize a series of pyrano[2,3-c]pyrazoles M1-M25 and pyrazolo[4',3':5,6]pyrano[2,3-d]pyrimidines M26-M31. The antimicrobial, antioxidant, and anti-cancer activities of these compounds were evaluated, showing promising biological activities. In silico study and DFT calculations were employed to investigate the expected mode of action and stability of the synthesized compounds, respectively.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Review
Biochemistry & Molecular Biology
Jian Yi Chai, Vaisnevee Sugumar, Mohammed Abdullah Alshawsh, Won Fen Wong, Aditya Arya, Pei Pei Chong, Chung Yeng Looi
Summary: The Hedgehog (Hh)-glioma-associated oncogene homolog (GLI) signaling pathway is highly conserved in mammals and plays crucial roles in cancer initiation and progression. GLI transcription factors are regulated by both SMO-dependent and SMO-independent mechanisms, with dysregulation leading to tumorigenesis in various cancers. Understanding the complex interplay between GLI and signaling elements could inspire new therapeutic breakthroughs for Hh-GLI-dependent cancers.
Article
Chemistry, Organic
Viacheslav Lysenko, Anton Portiankin, Tetiana Shvydenko, Kostiantyn Shvydenko, Svitlana Shishkina, Aleksandr Kostyuk
Summary: Starting from readily available aminocarbonyl compounds, the Marckwald reaction was used to prepare 6,7-dihydro-5H-pyrrolo[1,2-c]imidazoles. This two-step procedure yielded the product in high yield and can be used for bulk synthesis. Further reactions with various electrophiles yielded previously unknown functionalized derivatives. The reaction with silylformamidine in equilibrium with its carbenic form produced a C-silyl derivative. Various halogen derivatives were prepared and used as starting materials.
SYNTHETIC COMMUNICATIONS
(2023)
Article
Chemistry, Organic
Baitan Chakraborty, Umasish Jana
Summary: A method for synthesizing nine-membered rings via alkyne-carbonyl metathesis reaction is reported, resulting in the formation of unexplored 6,7-dihydro-5H-dibenzo[c,e]azonines. The use of cheap, non-toxic iron catalysts and milder conditions provides an alternative route to existing methods for synthesizing nine-membered rings.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2021)
Article
Chemistry, Organic
Dina A. Bakhotmah, Tarik E. Ali, Mohammed A. Assiri, Ibrahim S. Yahia
Summary: An unexpected efficient catalytic reaction was utilized to synthesize a series of potentially bioactive compounds with novel molecular structures. These compounds are based on a malononitrile skeleton fused with pyrazole, pyridine, chromone, pyrimidine, and pyrano[2,3-c]pyrazole systems. Elemental analysis and spectral techniques were used to confirm the structures of the products, and their cytotoxic activities were evaluated. Compounds 4 and 11 exhibited the highest cytotoxicity against various cancer cell lines.
POLYCYCLIC AROMATIC COMPOUNDS
(2022)
Editorial Material
Chemistry, Medicinal
Ram W. Sabnis
Summary: The article introduces estrogen receptors and their expression and functions in different tissues, particularly their role in breast cancer. It also mentions a new approach of using SERDs to counter resistance.
ACS MEDICINAL CHEMISTRY LETTERS
(2022)
Review
Oncology
Ashley N. Sigafoos, Brooke D. Paradise, Martin E. Fernandez-Zapico
Summary: The Hedgehog/GLI pathway is crucial during development and often dysregulated in diseases like cancer. Activation in cancer is typically through a non-canonical, ligand-independent mechanism. This pathway involves a series of components that work together to repress or activate signaling cascades.
Review
Chemistry, Multidisciplinary
Ayman Y. El-Khateeb, Sahar E. Hamed, Khaled M. Elattar
Summary: This review summarizes the research progress in the past two years on the multicomponent synthetic routes of heterocyclic compounds incorporated with a pyranopyrimidine skeleton, including various ring closures and possible reaction mechanisms. The significant biological activity of the compounds synthesized from multicomponent reactions is also discussed.
Article
Biochemistry & Molecular Biology
Xuemei Qin, Leifu Yang, Peng Liu, Lifang Yang, Linmeng Chen, Liming Hu, Mingguo Jiang
Summary: A series of novel EGFR-targeted anticancer compounds were designed and synthesized, with compound 13c showing the strongest anticancer activity. Docking study indicated that compound 13b could nicely bind to the ATP binding pocket of EGFR, and the target compounds demonstrated inhibitory activity against EGFR-TK.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Applied
Nejc Petek, Bibi Erjavec, Dejan Slapsak, Aljaz Gaber, Uros Groselj, Franc Pozgan, Sebastijan Ricko, Bogdan Stefane, Marina Klemencic, Jurij Svete
Summary: A series of new fluorescent compounds were synthesized via copper-catalyzed reactions, exhibiting interesting and promising optical properties. Some of them were successfully used for protein labeling.
Article
Multidisciplinary Sciences
Farzaneh Mohamadpour
Summary: A green synthetic approach for the photosynthesis of pyrano[2,3-d]pyrimidine scaffolds was developed using the Knoevenagel-Michael tandem cyclocondensation reaction. A novel halogenated dicyanobenzene-based photosensitizer was utilized in an aqueous solution, activated by a blue LED, and showed high energy efficiency and eco-friendliness. The study also investigated the turnover number and turnover frequency for pyrano[2,3-d]pyrimidine scaffolds.
SCIENTIFIC REPORTS
(2023)
Article
Chemistry, Multidisciplinary
Abdolkarim Zare, Elham Izadi
Summary: A novel nanomaterial, SPBHRS, was prepared by grafting an organic moiety containing 4,4'-bipyridine scaffold on rice husk-derived nano-silica. The nanomaterial was characterized by multiple techniques and utilized as an efficient and recyclable catalyst for the synthesis of pyrano[2,3-d]pyrimidine-2,4-diones and pyrano[2,3-d]pyrimidine-4-one-2-thiones through a one-pot multi-component reaction.
RESEARCH ON CHEMICAL INTERMEDIATES
(2023)
