Article
Chemistry, Organic
Yang Gao, Xue Song, Ru-Jie Yan, Wei Du, Ying-Chun Chen
Summary: The introduction of an alpha-vinyl group can alter the regioselectivity of the chiral secondary amine-catalyzed reaction, leading to the formation of diverse cyclic annulation products with new structural motifs.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2021)
Article
Chemistry, Physical
Yahya Nural, Ergin Keles, Burcu Aydiner, Nurgul Seferoglu, Hasan Atabey, Zeynel Seferoglu
Summary: The molecular structures of two new naphthoquinone-imidazole based dyes containing indole and pyrene moiety were confirmed, and their anion selectivity and sensitivity were studied. The interaction mechanisms between the dyes were verified by various spectroscopic methods, and the acid dissociation constants were determined for each dye relating to protonated carbonyl group and nitrogen atoms.
JOURNAL OF MOLECULAR LIQUIDS
(2021)
Article
Chemistry, Multidisciplinary
Ping Yang, Jia-Bao Luo, Li-Lei Zhang, Ying-Si Wang, Xiao-Bao Xie, Qing-Shan Shi, Xin-Guo Zhang
Summary: A series of novel hybrids based on fluoroquinolone skeleton were synthesized by introducing 1,3,4-oxadiazole derivatives to ciprofloxacin or norfloxacin at the C-7 site. In vitro antibacterial evaluation showed that some of the hybrids exhibited increased activity against Staphylococcus aureus and methicillin-resistant S. aureus, with some demonstrating bactericidal effects on standard bacteria. Molecular docking study revealed high binding affinity of certain hybrids to type IV topoisomerase.
Article
Biochemistry & Molecular Biology
Patricia Gonzalez Periche, Amanda Ramdular, Naga V. S. D. K. Bhupathiraju, Teja Kalidindi, Delissa S. Johnson, Nagavarakishore Pillarsetty, David R. Mootoo
Summary: This study describes the synthesis and cytotoxicity of THF containing 4-deoxyannonmontacin (4-DAN), as well as its analogues comprising carbohydrate and thiophene substitutes. Different analogues showed significant cytotoxicity against human prostate cancer cell lines.
CARBOHYDRATE RESEARCH
(2022)
Article
Pharmacology & Pharmacy
Imen Khelifi, Audrey Tourrette, Daycem Khelifi, Thomas Efferth, El Akrem Hayouni, Riadh Ksouri, Jalloul Bouajila
Summary: The study evaluated the potential of 1,4-naphthoquinones for skin application using bigel technology for drug delivery, showing good efficacy in inhibiting elastase activity and cytotoxicity towards melanoma cells. M1 and M2 exhibited different release profiles in the bigels, with M1 showing faster and more efficient release.
CURRENT DRUG DELIVERY
(2021)
Article
Biochemistry & Molecular Biology
Monica Martinez-Estevez, Soledad Garcia-Fontan, Saray Argibay-Otero, Inmaculada Prieto, Ezequiel M. Vazquez-Lopez
Summary: In this study, the reaction between [Ru2Cl2(mu-Cl)(2)(eta(6)-p-cymene)(2)] and two thiosemicarbazones was investigated. The resulting cationic complexes were isolated and characterized. The study revealed the presence of two isomers in the triflate salts and only one isomer in the chloride. X-ray crystallography confirmed this finding. The coordination of the thiosemicarbazone ligand to the ruthenium center was also demonstrated.
Article
Biochemistry & Molecular Biology
Aso Hameed Hasan, Sonam Shakya, Faiq H. S. Hussain, Sankaranarayanan Murugesan, Subhash Chander, Mohammad Rizki Fadhil Pratama, Shajarahtunnur Jamil, Basundhara Das, Subhrajit Biswas, Joazaizulfazli Jamalis
Summary: Acetylcholinesterase inhibitors are commonly prescribed medications for the treatment of Alzheimer's disease and dementia. In this study, a series of novel compounds were designed, synthesized, and tested for their ability to inhibit acetylcholinesterase activity. The results showed that these compounds exhibited significant inhibition and low cytotoxicity.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Chemistry, Applied
Pattamaporn Wosawat, Thanaset Senawong, Nattawut Suchaichit, Natcha P. Suchaichit, Kwanjai Kanokmedhakul, Somdej Kanokmedhakul, Panawan Moosophon
Summary: A new compound isolated from the stems of Diospyros ehretioides showed significant cytotoxicity against several cancer cell lines. Some compounds exhibited promising anti-cancer activity.
NATURAL PRODUCT RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Sravani Sana, Velma Ganga Reddy, T. Srinivasa Reddy, Ramya Tokala, Rahul Kumar, Suresh K. Bhargava, Nagula Shankaraiah
Summary: The study introduces a novel class of compounds with moderate to interesting cytotoxicity against various cancer cell lines, with compound 18i showing the highest potency and specificity towards A549 (lung cancer) cells. Flow cytometry analysis revealed that 18i induced G2/M phase cell cycle arrest, indicating potential anticancer activity. The most active compound, 18i, demonstrated enhanced microtubule disruption and significant antitumor effects through multiple mechanisms, including apoptosis induction, ROS generation, and inhibition of cellular migration.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Mohammed A. S. Abourehab, Alaa M. Alqahtani, Faisal A. Almalki, Dana M. Zaher, Ashraf N. Abdalla, Ahmed M. Gouda, Eman A. M. Beshr
Summary: In this study, eight new hybrids of NSAIDs were synthesized and evaluated for their antiproliferative activities against cancer cell lines. The results showed that three hybrids exhibited significant inhibitory effects on cell growth and induced early apoptotic events. Molecular docking results indicated higher binding free energies towards COX-2, suggesting their potential as anticancer candidates.
Article
Biochemistry & Molecular Biology
Mai A. E. Mourad, Ayman Abo Elmaaty, Islam Zaki, Ahmed A. E. Mourad, Amal Hofni, Ahmed E. Khodir, Esam M. Aboubakr, Ahmed Elkamhawy, Eun Joo Roh, Ahmed A. Al-Karmalawy
Summary: A novel series of naphtho[2',3':4,5]thiazolo[3,2-a]pyrimidine hybrids were synthesized and evaluated for their inhibitory effects on topo IIa and EGFR as well as their ability to induce apoptosis. The compounds 6i, 6a, and 6c exhibited superior cytotoxic activity compared to doxorubicin and erlotinib against the tested cancer cells. Molecular analysis suggested that these hybrids could inhibit topo IIa and EGFR activities and cause cell cycle arrest and increased levels of p53, caspase-7, caspase-9, and Bax/Bcl-2 ratio.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Yuqi Tan, Danmei Tian, Cong Li, Yanhui Chen, Yiran Shen, Jia Li, Jinshan Tang
Summary: A new pentacyclic triterpenoid and a new benzoxepin-5-one, along with 26 known compounds, were isolated from the roots of Arnebia euchroma. These compounds showed potential cytotoxicity towards human lung adenocarcinoma cells and inhibitory effects on key enzymes regulating glucose and lipid metabolism. Among them, three compounds displayed moderate inhibitory effects on the enzymes and no obvious cytotoxicity, suggesting their potential for the development of new agents for the treatment of metabolic diseases.
Article
Pharmacology & Pharmacy
Jose Garces-Garces, Marta Redrado, Angela Sastre-Santos, Maria Concepcion Gimeno, Fernando Fernandez-Lazaro
Summary: A new family of perylenediimide (PDI) silver and copper complexes have been synthesized, and the coordination of metal center does not significantly affect their photophysical properties. The coordination of silver or copper greatly enhances the antiproliferative activity of the ligands, suggesting a synergistic effect between the two fragments. Colocalization experiments reveal that the metal complexes are mainly internalized inside the cells, with partial mitochondrial localization.
Article
Chemistry, Multidisciplinary
Muhammad Tariq Riaz, Parham Taslimi, Muhammad Yaqub, Mariya al-Rashida, Rima D. Alharthy, Ahmed El-Gokha, Zahid Shafiq
Summary: Heterocyclic ketene aminals were used to synthesize diaza-benzo[a]anthracenedione derivatives through a one pot three-component cascade reaction. 2-Hydroxy-1,4-naphthoquinone and aromatic aldehydes were reacted with heterocyclic ketene aminals via a solvent-free tandem [3+2+1] annulation catalyzed by Et3N, yielding novel fused tetracyclic compounds. These compounds were found to be potent inhibitors of acetylcholinesterase and butyrylcholinesterase enzymes.
Review
Chemistry, Physical
Meena Devi, Parvin Kumar, Rahul Singh, Laxmi Narayan, Ashwani Kumar, Jayant Sindhu, Sohan Lal, Khalid Hussain, Devender Singh
Summary: The 1,4-naphthoquinone skeleton is an important component found in many biologically active natural products and chemotherapy agents. 1,4-naphthoquinones with electron donor amino substituents on specific positions have the potential to act as anion sensors and have various biological and industrial applications. 2,3-diamino-1,4-naphthoquinone is a promising bacteriostatic agent.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Tanaya Chatterjee, Gaurav Das, Barun K. Chatterjee, Jesmita Dhar, Surajit Ghosh, Pinak Chakrabarti
BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS
(2020)
Article
Biology
Miriam Stoeber, Damien Jullie, Joy Li, Soumen Chakraborty, Susruta Majumdar, Nevin A. Lambert, Aashish Manglik, Mark von Zastrow
Article
Chemistry, Multidisciplinary
Krishnangsu Pradhan, Gaurav Das, Chirantan Kar, Nabanita Mukherjee, Juhee Khan, Tanushree Mahata, Surajit Barman, Surajit Ghosh
Article
Chemistry, Multidisciplinary
Saswat Mohapatra, Gaurav Das, Varsha Gupta, Prasenjit Mondal, Masashi Nitani, Yutaka Ie, Shreyam Chatterjee, Yoshio Aso, Surajit Ghosh
Summary: In this study, the organic molecule BBT was shown to modulate mitochondrial ROS generation by affecting complex I activity, leading to apoptotic cell death and potentially inhibiting cancer cell relapse. The unique electron acceptor ability of BBT and its activation of stress-dependent pathways highlight its potential as an anticancer agent.
Article
Chemistry, Medicinal
Soumen Chakraborty, Jeffrey F. DiBerto, Abdelfattah Faouzi, Sarah M. Bernhard, Anna M. Gutridge, Steven Ramsey, Yuchen Zhou, Davide Provasi, Nitin Nuthikattu, Rahul Jilakara, Melissa N. F. Nelson, Wesley B. Asher, Shainnel O. Eans, Lisa L. Wilson, Satyanarayana M. Chintala, Marta Filizola, Richard M. van Rijn, Elyssa B. Margolis, Bryan L. Roth, Jay P. McLaughlin, Tao Che, Dalibor Sames, Jonathan A. Javitch, Susruta Majumdar
Summary: The study investigated the structure-activity relationships of the major alkaloids in kratom, mitragynine and 7-hydroxymitragynine, through synthesizing analogs and conducting experiments. The synthesized analogs demonstrated potential analgesic effects in both G-protein assays and animal experiments.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Physical
Batakrishna Jana, Surajit Barman, Rajsekhar Roy, Gaurav Das, Nabanita Mukherjee, Anindyasundar Adak, Surajit Ghosh
Summary: The study investigates the effect of an exchangeable GTP/GDP binding antimitotic tetrapeptide on its binding affinity to tubulin and its anticancer potential, showing that the substitution of proline with multifluorine substituted proline enhances its effects.
JOURNAL OF PHYSICAL CHEMISTRY B
(2021)
Article
Multidisciplinary Sciences
Tanaya Chatterjee, Gaurav Das, Surajit Ghosh, Pinak Chakrabarti
Summary: The study revealed that gold nanoparticles have an impact on the structure and function of protein L-isoaspartyl methyltransferase (PIMT), with AuNS100 showing the best efficacy. AuNS100 not only stabilized PIMT, but also enhanced its activity and reduced the neurotoxicity induced by Aβ42 on neuronal cells.
SCIENTIFIC REPORTS
(2021)
Article
Chemistry, Applied
Samrat Dev, Souvik Pandey, Suvendu Maity, Debarpan Mitra, Gaurav Das, Nabendu Murmu, Chittaranjan Sinha
Summary: A phenylazo appended ortho-vanillin Schiff base scaffold (HAZ) has been utilized as a colorimetric sensor for selective detection of Cu2+ in semi-aqueous medium. The structure of HAZ and Cu (II) complex [Cu(AZ)(2)] is characterized using spectroscopic data and X-ray diffraction measurement. Additionally, the probe is tested for cytotoxicity on MDA-MB 231 breast cancer cells.
APPLIED ORGANOMETALLIC CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Mukul Bikash Maity, Debojit Talukdar, Basudeb Dutta, Gurupada Bairy, Nabendu Murmu, Gaurav Das, Chittaranjan Sinha
Summary: Strategic design of a Rhodamine-based chemosensor probe allowed for the highly sensitive recognition of ions/molecules at low concentrations, with implications for health and sustainability. The probe exhibited a significant increase in fluorescent intensity in the presence of Analytical Group IIIA ions, and was effective for cell imaging and inhibiting breast cancer cell proliferation.
INORGANICA CHIMICA ACTA
(2023)
Article
Biochemistry & Molecular Biology
Tanaya Chatterjee, Gaurav Das, Barun K. Chatterjee, Surajit Ghosh, Pinak Chakrabarti
Summary: The oligomeric form of amyloid-beta peptide (A beta 42) is crucial in Alzheimer's disease pathogenesis and cognitive deficits. It is believed that soluble oligomers are more toxic than fibrils. Protein-L-isoaspartyl methyltransferase (PIMT) repairs aberrant isoAsp residues and inhibits A beta 42 fibrillization. PIMT affects the conformation, size, and toxicity of A beta 42 oligomers, and has a neuroprotective role against A beta O-induced toxicity.
ACS CHEMICAL NEUROSCIENCE
(2023)
Article
Nanoscience & Nanotechnology
Rousunara Khatun, Ritwik Modak, Abu Saleh Musha Islam, Dolan Moni, Nayim Sepay, Rimi Mukherjee, Gaurav Das, Nabendu Murmu, Mahammad Ali
Summary: A manganese(III) complex, [Mn-III(L)(SCN)(enH)](NO3)& BULL;H2O, was synthesized and characterized. The interaction of the complex with DNA was studied, and the binding constant of the complex with ct-DNA was determined. Competitive displacement reactions of dyes from dye-ct-DNA conjugates by the complex were analyzed. The complex showed anticancer potential in breast cancer cells through a minor groove binding interaction with ct-DNA.
ACS APPLIED BIO MATERIALS
(2023)
Article
Nanoscience & Nanotechnology
Mallayasamy Siva, Kiran Das, Subhabrata Guha, Subramaniyam Sivagnanam, Gaurav Das, Abhijit Saha, Adele Stewart, Biswanath Maity, Priyadip Das
Summary: In this study, we designed and synthesized two phenanthro[9,10-d]imidazole-based ligands and their corresponding zinc complexes. These complexes were encapsulated in liposomes for cellular uptake and showed potential for breast cancer treatment through inducing DNA fragmentation, arresting the cell cycle, decreasing proliferation, and promoting apoptosis. The study demonstrates the promise of liposomal formation for developing imaging probes and efficient anticancer drugs.
ACS APPLIED BIO MATERIALS
(2023)
Article
Plant Sciences
Michel-Gael F. Guefack, Debojit Talukdar, Rimi Mukherjee, Subhabrata Guha, Debarpan Mitra, Depanwita Saha, Gaurav Das, Francois Damen, Victor Kuete, Nabendu Murmu
Summary: Hypericum roeperianum, a traditional medicinal spice, has been found to possess anticancer properties. It inhibits breast cancer progression by regulating mitochondrial apoptosis and epithelial-mesenchymal transition (EMT). The crude extract induces apoptosis and inhibits cell migration by affecting multiple molecular markers. Additionally, it modulates the PI3K/Akt/mToR signaling pathway to suppress EMT. The in vitro and in vivo experiments support the potential use of Hypericum roeperianum in breast cancer therapy.
JOURNAL OF ETHNOPHARMACOLOGY
(2024)
Article
Chemistry, Medicinal
Anindyasundar Adak, Gaurav Das, Varsha Gupta, Juhee Khan, Nabanita Mukherjee, Prasenjit Mondal, Rajsekhar Roy, Surajit Barman, Prabir Kumar Gharai, Surajit Ghosh
Summary: Protein-protein interactions are crucial in microtubule dynamics and cancer therapeutics. The study found that para-fluorophenylalanine-modified stapled peptides are the most potent inhibitors of microtubule polymerization, with potential for inhibiting melanoma growth.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Multidisciplinary
Gaurav Das, Surojit Ghosh, Shubham Garg, Satyajit Ghosh, Aniket Jana, Ramkamal Samat, Nabanita Mukherjee, Rajsekhar Roy, Surajit Ghosh
Article
Chemistry, Organic
Faiza Diaba, Gisela Trenchs
Summary: The first violet light-mediated synthesis of gamma- and delta-lactams from N-alkenyl trichloroacetamides is reported in this paper. The reactions are conducted in tetrahydrofuran or 2-methyltetrahydrofuran as the sole solvent without catalysts or additives, under non-anhydrous conditions in an air atmosphere where the solvent serves as the radical initiator.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Feroze Hussain, Sajjad Ahmed, Ashiq Hussain Padder, Qazi Naveed Ahmed
Summary: This study reports a novel and efficient one-pot synthesis method for mixed phosphorotrithioates, which does not require supplementary additives and shows broad applicability.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Hyunjin Oh, Ikyon Kim
Summary: A new 1,2,4-triazole-pyrrolo[1,2-a]pyrazine hybrid system, 6-acylpyrrolo[1,2-a][1,2,4]triazolo[5,1-c]pyrazine, was synthesized using a catalyst-free method. This method involved sequential exposure of pyrrole-2-carbonitrile-derived substrates to DMF-DMA and acyl hydrazide, resulting in the formation of acylated pyrazine and 1,2,4-triazole rings, enabling the installation of various substituents at specific positions on the core skeleton.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Ming Yan, Si-fan Wang, Yong-po Zhang, Jin-zhong Zhao, Zhuo Tang, Guang-xun Li
Summary: Here we developed an efficient photocatalytic approach for the convenient preparation of sulfinamides. The reaction allows for the gram-scale preparation of sulfinamides and the one-pot synthesis of various sulfonyl amides.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Farzaneh Bandehali-Naeini, Zahra Tanbakouchian, Noushin Farajinia-Lehi, Nicolas Mayer, Morteza Shiri, Martin Breugst
Summary: Two tandem catalytic systems were developed for the synthesis of novel 3,4-disubstituted maleimides using the same Ugi adducts. Different maleimide structures can be synthesized using either Pd or Cu catalysis.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Tanya Raghava, Anjan Chattopadhyay, Subhadeep Banerjee, Nivedita Sarkar
Summary: Amine substitution of two ortho fluorine atoms of tetrafluoroterephthalonitrile through SNAr chemistry is easily achievable. But further fluorine substitution is only possible under forcing conditions, yielding valuable fluorophores for bioimaging.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Review
Chemistry, Organic
Anju Chadha, Santosh Kumar Padhi, Selvaraj Stella, Sowmyalakshmi Venkataraman, Thangavelu Saravanan
Summary: Alcohol dehydrogenases are enzymes that use cofactors for oxidation or reduction reactions of alcohols or carbonyl compounds. They are utilized in green chemistry and have applications in the production of pharmaceuticals. Recombinant enzymes have solved the challenge of producing purified enzymes in large quantities. Engineered alcohol dehydrogenases have been used in asymmetric synthesis in industry. Various methods have been established for regenerating expensive cofactors to make the enzymatic process more efficient and economically viable.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
