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
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, 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
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, 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)
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)
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, 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.
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)
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
Aarzoo Kamboj, Binita Sihag, Deshkanwar Singh Brar, Arshpreet Kaur, Deepak B. Salunke
Summary: Malaria is a preventable and treatable disease, but can be fatal if ignored. Current means to overcome malaria include ACT and RTS, S/AS01 vaccine, but they have limitations. Researchers are exploring the use of natural products containing beta-carboline scaffold to design new drugs to combat this deadly disease.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Syed Nasir Abbas Bukhari, Mohamed Abdelwahab Abdelgawad, Muhammad Wahab Amjad, Muhammad Usman Munir, Fatima Akbar Sheikh
Summary: This study synthesized a series of novel oxime derivatives and tested their inhibitory activity against COX-1, COX-2, and LOX-5 enzymes. Results showed that these oxime derivatives effectively inhibited the activity of COX-1 and COX-2, with compounds containing methoxymethoxy or hydroxy substituents exhibiting the strongest effects, while compounds with a long alkyl chain ether group showed the strongest inhibition against 5-LOX. Furthermore, these derivatives demonstrated the ability to inhibit nitric oxide generation and LPS-induced inflammatory factor production in macrophages. Molecular docking studies revealed the inhibitory mechanism of these compounds and the importance of various interactions.
MEDICINAL CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Shalini, Vipan Kumar
Summary: The development of hybrid molecules in cancer chemotherapy has shown promising results, with many entering clinical trials or the drug market in recent years. The collaboration between chemistry, biology, and pharmacology has greatly contributed to the advancement of hybrid chemotherapeutics.
EXPERT OPINION ON DRUG DISCOVERY
(2021)
Review
Chemistry, Medicinal
Sumit Kumar, Bharvi Sharma, Vishu Mehra, Vipan Kumar
Summary: 1H-1,2,3-triazole, obtained through the Click Reaction, has become a favorite among synthetic/medicinal chemists for its ability to mimic different functional groups and enhance targeted biological activities. Triazole derivatives have shown potential in accelerating the development of new scaffolds and are essential in biomolecular mimetics and fragment-based drug design.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Organic
Rayees Ahmad Naikoo, Rupesh Kumar, Vipan Kumar, Gaurav Bhargava
Summary: Functionalized tricyclicpyrimidinones are a class of condensed heterocyclic systems found in potentially active molecules. Researchers worldwide have explored various synthetic methods for constructing appropriately functionalized tricyclicpyrimidinones. This review article summarizes reports on substituted and functionalized tricyclic pyrimidinones since 2000.
SYNTHETIC COMMUNICATIONS
(2021)
Article
Microbiology
Matt D. Johansen, Shalini, Sumit Kumar, Clement Raynaud, Diana H. Quan, Warwick J. Britton, Philip M. Hansbro, Vipan Kumar, Laurent Kremer
Summary: The designed and synthesized isatin-isoniazid hybrids exhibit high antimycobacterial activity against tuberculosis, well-tolerated with good selectivity in kidney cells, and are effective in infected macrophages, indicating their potential as promising antitubercular compounds for further evaluation in preclinical settings.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Biochemistry & Molecular Biology
Anu Saini, Sumit Kumar, Raghu Raj, Shefali Chowdhary, Mathieu Gendrot, Joel Mosnier, Isabelle Fonta, Bruno Pradines, Vipan Kumar
Summary: A library of 1H-1,2,3-triazole-tethered 4-aminoquinoline-benzoxaborole hybrids was synthesized and screened for anti-plasmodial efficacy, with the inclusion of quinoline core resulting in enhanced activities. The most potent conjugate exhibited lower cross resistance with Chloroquine against both chloroquine-susceptible 3D7 and chloroquine-resistant W2 strains of P. falciparum.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Anu Rani, Anny Sharma, Jenny Legac, Philip J. Rosenthal, Parvesh Singh, Vipan Kumar
Summary: Quinoline-isoniazid-phthalimide triads synthesized for evaluating antiplasmodial efficacy against chloroquine-resistant P. falciparum and cytotoxicity on Vero cells showed promising results with some compounds having IC50 in the range of 11-30 nM and high selectivity index, indicating their potential as templates for new antiplasmodial drugs.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Anu Rani, Amandeep Singh, Jashanpreet Kaur, Gurjit Singh, Rajbir Bhatti, Njabulo Gumede, Prishani Kisten, Parvesh Singh, Sumanjit, Vipan Kumar
Summary: This study elucidates the synthesis of novel AChE and BuChE inhibitory compounds and validates their pharmacological activities. Additionally, the investigation reveals the potential of these compounds in ameliorating behavioral and neurochemical changes in mice.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Bharvi Sharma, Sumit Kumar, Preeti, Matt D. Johansen, Laurent Kremer, Vipan Kumar
Summary: In this study, a library of isatin-derived bis(heteronuclear hydrazones) were designed, synthesized, and evaluated for their antimycobacterial activity. Compounds with isoniazid core and polar-donating groups at the C-5 position of isatin showed the most promising antibacterial activity against tuberculosis, while being non-cytotoxic to host cells.
CHEMICAL BIOLOGY & DRUG DESIGN
(2022)
Article
Chemistry, Analytical
Sarbjeet Kaur, Shalini, Bilal Ahmad Shiekh, Vipan Kumar, Inderpreet Kaur
Summary: A new compound TNFC was synthesized and confirmed by various experimental methods, and then successfully applied as a receptor for Cu2+ in differential pulse voltammetric and potentiometric sensors for quantification.
JOURNAL OF ELECTROANALYTICAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Bharvi Sharma, Vipan Kumar
Summary: Ferrocene, with its inherent stability, excellent redox properties, and low toxicity, plays an important role in bioorganometallic chemistry. The development of remarkable antimalarial and anticancer drugs from ferrocene demonstrates its significant contribution to medicinal chemistry. Incorporating ferrocene into organic compounds and natural products can influence the mode of action and biological activities, highlighting its potential in designing safer and promising drugs.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Sumit Kumar, Anu Saini, Ankush Kumar, Raghu Raj, Vipan Kumar
Summary: A series of 1H-1,2,3-triazole linked 7-chloroquinoline-chalcones and 7-chloroquinoline-pyrazolines were synthesized and evaluated for their antimycobacterial and cytotoxic activities. One compound with O-methoxy and p-methoxy substituents exhibited moderate activity and was noncytotoxic.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Shefali Chowdhary, Shalini, Amandeep Arora, Vipan Kumar
Summary: Isatin is recognized as an attractive therapeutic fragment in drug design and development, particularly for developing new anticancer scaffolds. It also has potential in treating Neglected Tropical Diseases (NTDs).
Correction
Chemistry, Analytical
Sarbjeet Kaur, Shalini, Bilal Ahmad Shiekh, Vipan Kumar, Inderpreet Kaur
JOURNAL OF ELECTROANALYTICAL CHEMISTRY
(2022)
Article
Chemistry, Physical
Shubham Lata, Sourav Taru Saha, Mandeep Kaur, Paul Awolade, Oluwakemi Ebenezer, Parvesh Singh, Vipan Kumar, Vipan Kumar
Summary: This study designed and synthesized a series of tetrahydro-beta-carboline-naphthalimide hybrids. Through evaluating their growth inhibitory potential against breast cancer cell lines and studying their interactions with estrogen receptor, the success rate and potential of hybridization technique in cancer treatment were demonstrated.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Editorial Material
Chemistry, Medicinal
Parvesh Singh, Vipan Kumar