Article
Biochemistry & Molecular Biology
Emilia P. T. Leitao, Osvaldo S. Ascenso, Tania Santos de Almeida, Ignacio Gonzalez, Inmaculada Hernandez, Jose Quintana, Francisco Estevez, Patricia Rijo
Summary: A series of hydroxylated chalcone derivatives with different substitution patterns were prepared, and it was found that the naphthylchalcone containing a methoxy group in position 6 ' of the A ring exhibited the highest cytotoxicity against human leukaemia cells.
BIOORGANIC CHEMISTRY
(2021)
Review
Chemistry, Organic
Yogesh Murti, Devender Pathak, Kamla Pathak
Summary: Flavonoids are a diverse family of aromatic compounds in nature with reported biological activities, making them potential targets for nutraceuticals and pharmaceuticals. Green Chemistry advancements have enabled eco-friendly synthesis of chalcones, a precursor to flavonoids, reducing hazards to human health and the environment. Bulk production of various flavonoids using green chemistry techniques has been successfully achieved in the pharmaceutical field.
CURRENT ORGANIC CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Rui Pereira, Artur M. S. Silva, Daniela Ribeiro, Vera L. M. Silva, Eduarda Fernandes
Summary: This review article provides an overview of the chemical structure, chemical properties, and synthesis methods of bis-chalcones. It also emphasizes the anti-inflammatory activity of bis-chalcones and their mechanisms of action.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Laurene Minsat, Cedric Peyrot, Fanny Brunissen, Jean-Hugues Renault, Florent Allais
Summary: A series of phloretin analogs were synthesized through a green method, showing potential higher activity than phloretin itself, with some molecules demonstrating lower EC50 values than phloretin.
Article
Biochemistry & Molecular Biology
Miraj Fatima, Samina Aslam, Ansa Madeeha Zafar, Ali Irfan, Misbahul Ain Khan, Muhammad Ashraf, Shah Faisal, Sobia Noreen, Gamal A. Shazly, Bakht Ramin Shah, Yousef A. Bin Jardan
Summary: This research focuses on the synthesis of furan chalcone compounds and their potential for inhibiting bacterial urease enzyme. The results show that these compounds exhibit promising urease inhibition activity, with 1-phenyl-3-[5-(2,5-dichlorophenyl)-2-furyl]-2-propen-1-one and 1-phenyl-3-[5-(2'-chlorophenyl)-2-furyl] -2-propen-1-one displaying the highest activity.
Article
Chemistry, Physical
Hamza Annath, Jinesh C. Manayil, Jillian Thompson, Andrew C. Marr, Robert Raja
Summary: A comparative study of catalytic active sites in amorphous and crystalline aluminophosphates and their iron-containing analogues revealed that secondary porosity generated via soft templating and large mesopores significantly improve mass-transport and conversion of carbonyls. The active acidic sites play a crucial role in activating carbonyl groups and enhancing catalytic performance. Amorphous aluminophosphate (5) showed promising potential in industrial and pharmaceutical applications, outperforming hierarchical porous FeAlPO-5.
APPLIED CATALYSIS A-GENERAL
(2021)
Article
Chemistry, Medicinal
Daniel Insuasty, Stephanie Garcia, Rodrigo Abonia, Braulio Insuasty, Jairo Quiroga, Manuel Nogueras, Justo Cobo, Gabriela L. Borosky, Kenneth K. Laali
Summary: A series of quinoline-based compounds were synthesized and evaluated for their cytotoxic activity against cancer cells, with two compounds showing promising anticancer effects with lower GI(50) values than reference drugs. Docking studies revealed strong binding energies in proteins involved in key carcinogenic pathways.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Multidisciplinary
M. Fatih Polat, Derya Aktas Anil, Gizem Ozkemahli, Burcin Turkmenoglu, Ceylan Hepokur, Serdar Burmaoglu, Oztekin Algul
Summary: A novel series of trimethoxy chalcones with CF3 or F substituents at different positions of ring B were designed and synthesized. These compounds were characterized using IR, NMR spectral data, and elemental analyses. Their cytotoxicity against A549, HEPG2, MCF7, and L929 cells was evaluated, and compound 13 showed the highest activity and induced cell cycle arrest at the G0/G1 phase in MCF7 cells. The apoptotic mechanisms of compound 13 involving Bax, Bcl-2, and p53 were also investigated, along with their effects on human EGFR and VEGFR-2 receptors.
Article
Chemistry, Medicinal
Syed Nasir Abbas Bukhari, Nasser Hadal Alotaibi, Waqas Ahmad, Khalid Saad Alharbi, Mohamed A. Abdelgawad, Mohammad M. Al-Sanea, Muhammad Masood Ahmad, Muhammad Wahab Amjad, Maria Abdul Ghafoor Raja, Muhammad Ajaz Hussain
Summary: The study evaluated 18 ligustrazine-containing derivatives for their inhibitory effects on five different types of cancer cells, with compounds 4a and 4b showing the strongest inhibition. The synthetic derivatives showed a multitarget approach with strong inhibitory effects on EGFR, FAK, and BRAF.
MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Svetlana A. Popova, Evgeniya V. Pavlova, Irina Yu. Chukicheva
Summary: In this study, a series of new methoxychalcone derivatives with an isobornyl fragment in ring A were synthesized via the Claisen-Schmidt condensation of O-allylated 2,4-dihydroxy-5-isobornylacetophenone with different methoxybenzaldehydes.
Review
Chemistry, Medicinal
Gayathri Rajendran, Deepu Bhanu, Baladhandapani Aruchamy, Prasanna Ramani, Nanjan Pandurangan, Kondapa Naidu Bobba, Eun Jung Oh, Ho Yun Chung, Prakash Gangadaran, Byeong-Cheol Ahn
Summary: This review summarizes the structures, synthesis methods, biological characteristics, and applications of chalcones over the past decade, and provides detailed insights into their structure-activity relationship studies. It offers guidelines for future design and synthesis of promising drug candidates, and provides important support for the development of drugs against infectious and non-infectious diseases.
Review
Biochemistry & Molecular Biology
Nicolas Giacoletto, Frederic Dumur
Summary: Over the past several decades, photopolymerization research has been actively developing, with bis-chalcones found to be promising photosensitizers for different polymerization reactions. This review provides an overview of the various bis-chalcones reported to date and their applications in different fields.
Article
Chemistry, Medicinal
Bathelemy Ngameni, Kamdoum Cedric, Armelle T. Mbaveng, Musa Erdogan, Ingrid Simo, Victor Kuete, Arif Dastan
Summary: A new series of O-substituted chalcone derivatives with different substituents were designed, synthesized, and characterized, showing promising cytotoxic effects against leukemia and colon adenocarcinoma cells in preliminary cytotoxicity tests.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Applied
Min Huang, Manman Sun, Lanxin Zhang, Xuebo Yang, Yuntao Shi, Kun Xing, Hongguang Deng, Zhenwei Zhang, Dan Liu, Linxiang Zhao
Summary: This article presents an efficient new synthesis method for a peroxisome proliferator-activated receptor delta agonist fonadelpar. The method utilizes Claisen-Schmidt condensation and an optimized process to prepare the drug candidate with fewer steps and higher yield.
ORGANIC PROCESS RESEARCH & DEVELOPMENT
(2022)
Article
Chemistry, Multidisciplinary
Zhe Xiang, Xi Zhao, Guoxiang Wang, Chenze Qi, Sujing Zhou, Jinjing Li, Yong Gao
Summary: In this study, an efficient and recyclable platform for interfacial catalytic reaction was constructed using pH-responsive n-decane-in-water Pickering emulsions. The prepared emulsions showed high stability and rapid demulsification at low pH. The catalytic platform exhibited a far higher reaction efficiency compared to ordinary n-decane-water systems. This study demonstrates the potential application of Pickering emulsions in heterogeneous reactions.
JOURNAL OF INDUSTRIAL AND ENGINEERING CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Alba L. Montoya, Eileni R. Gil, Emily L. Heydemann, Igor L. Estevao, Bianca E. Luna, Cameron C. Ellis, Sohan R. Jankuru, Belkisyole Alarcon de Noya, Oscar Noya, Maria Paola Zago, Igor C. Almeida, Katja Michael
Summary: Chagas disease (CD) can be accurately diagnosed by detecting Trypanosoma cruzi in patients' blood using PCR. However, parasite-derived biomarkers are of great interest for serological diagnosis and early evaluation of chemotherapeutic efficacy. In this study, researchers discovered that Galf beta 1,3Manp alpha 1,2-[Galf beta 1,3]Manp alpha is an immunodominant glycotope and developed NGP32b as a potential novel biomarker for CCD.
Article
Chemistry, Organic
Jorge Trilleras, Jairo Quiroga, Angelina Hormaza
Summary: The synthesis and structural diversification of N-heterocycles systems using conventional Claisen-Schmidt condensation reactions and [2+3] cycloaddition reactions have been conducted. This protocol offers a new approach for the synthesis of 3-(substituted aroyl)-4-heteroaryl pyrrole derivatives.
Article
Chemistry, Organic
Justo Cobo, Sebastian Molina, Adolfo Sanchez, Manuel Nogueras, Braulio Insuasty, Fabian Orozco-Lopez
Summary: This study investigated the reactivity of 6-iminophosphoranepyrimidines with DMAD and ethyl propiolate as dienophiles. Pyrimidine derivatives with a viable 2-azadienic moiety can undergo [4+2]/retro-[4+2] and [2+2]/retro-[2+2] reactions, while those without this structure can only undergo [2+2]/retro-[2+2] reactions involving the phosphazene moiety.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2022)
Article
Chemistry, Physical
Diana Becerra, Jaime Portilla, Justo Cobo, Juan-Carlos Castillo, Mario A. Macias
Summary: A series of N -(5-pyrazolyl)imines were synthesized in high yields through a solvent-free condensation reaction under microwave irradiation. The X-ray diffraction analyses of these compounds revealed the influence of substituents on the electronic delocalization between phenyl and pyrazole rings, affecting molecular conformations and supramolecular assembly. The resonance effect and acidic character of hydrogen atoms were found to play a role in the formation of short intermolecular hydrogen bonds in these molecules. The study also showed that dispersion forces act in higher proportions in more planar molecules for crystal formation.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Medicinal
Ivan Diaz, Sofia Salido, Manuel Nogueras, Justo Cobo
Summary: A series of novel pyrimidine-quinolone hybrids were designed and synthesized as inhibitors of lactate dehydrogenase A (hLDHA) using a computer-aided approach. By evaluating the inhibitory activity of different synthesized hybrids, new compounds with promising activity were successfully designed, and a preliminary structure-activity relationship was established.
Article
Chemistry, Organic
Jorge Trilleras, Alfredo Perez-Gamboa, Jairo Quiroga
Summary: We report the unexpected aromatic nucleophilic substitution reaction products on 2-amino-4,6-dichloropyrimidine-5-carbaldehyde under mild and environmentally friendly conditions, due to the influence of structural factors of the starting pyrimidine and a high concentration of alkoxide ions. This method allows the synthesis of pyrimidine-based compound precursors of N-heterocyclic systems.
Article
Biochemistry & Molecular Biology
Lina Fernanda Castano, Jairo Quiroga, Rodrigo Abonia, Daniel Insuasty, Oscar M. Vidal, Rosalia Sena, Vivian Rubio, Gloria Puerto, Manuel Nogueras, Justo Cobo, Juan Guzman, Alberto Insuasty, Braulio Insuasty
Summary: A series of sulfonamides and chalcone-sulfonamide hybrids were synthesized and evaluated for their anticancer and antituberculosis activities. Some of the compounds showed potential activity against cancer and tuberculosis, but further optimization is needed.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Immunology
Sayonara M. Viana, Alba L. Montoya, Augusto M. Carvalho, Brunele S. de Mendonca, Susana Portillo, Janet J. Olivas, Nasim H. Karimi, Igor L. Estevao, Uriel Ortega-Rodriguez, Edgar M. Carvalho, Walderez O. Dutra, Rosa A. Maldonaldo, Katja Michael, Camila de Oliveira, Igor C. Almeida
Summary: This study evaluated the seroreactivity of TL patients across its clinical spectrum using a chemiluminescent immunoassay and found that NGP28b exhibited high sensitivity and specificity, especially with SC sera, in the diagnosis of TL.
EMERGING MICROBES & INFECTIONS
(2022)
Article
Chemistry, Multidisciplinary
Diana M. Ardila, Diego F. Rodriguez, Alirio Palma, Ivan Diaz Costa, Justo Cobo, Christopher Glidewell
Summary: Three new hybrids of 4-styrylquinoline-benzimidazole have been synthesized and characterized. The structures of these compounds have been determined and comparisons with related compounds have been made.
ACTA CRYSTALLOGRAPHICA SECTION C-STRUCTURAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Diana R. Vera, Diana M. Ardila, Alirio Palma, Justo Cobo, Christopher Glidewell
Summary: Four new 2,4-distyrylquinolines and one 2-styryl-4-[2-(thiophen-2-yl)vinyl]quinoline have been synthesized and characterized. Different orientations of the styryl units in relation to the quinoline nucleus were observed. The structure of the compounds was analyzed and compared with related compounds.
ACTA CRYSTALLOGRAPHICA SECTION C-STRUCTURAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Daniela Fonseca, Andres F. Perez-Torres, Justo Cobo, Jhon Zapata-Rivera, John J. Hurtado, Mario A. Macias
Summary: This study investigated the recrystallization of complex [Co(DNB)(2)] in different solvents and found that mono or trinuclear molecules can be obtained depending on the solvent used. X-ray crystallography and DFT calculations revealed that this behavior is influenced by the closeness of the solvents' HOMOs to the Co(ii) ions' SOMOs and the formation of intermolecular hydrogen bonds between the carboxylate group of the ligands and the solvent.