Article
Biochemistry & Molecular Biology
Fumihiro Kawagoe, Sayuri Mototani, Atsushi Kittaka
Summary: Different components of the structure of vitamin D-3 play unique roles in expressing its biological activities. Organic chemists have focused on D-ring-modified vitamin D analogues and studied their synthesis methods and biological properties.
Article
Chemistry, Multidisciplinary
Jiaxin Xie, Zhong Zheng, Xin Liu, Nan Zhang, Shinyoung Choi, Chuan He, Guangbin Dong
Summary: This study reports on the synthesis of phainanoids, a new class of dammarane-type triterpenoids with potent immunosuppressive activities and unique structural features. Efficient approaches have been established for the synthesis of key structural components. The asymmetric synthesis of (+)-phainanoid A has been achieved and novel estrone-derived analogues have also been prepared. The compounds show specific inhibition of lymphocyte proliferation, providing preliminary structure-activity relationship information.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Biochemistry & Molecular Biology
Sumei Ren, Minmin Zhang, Yujie Wang, Jia Guo, Junfei Wang, Yingxia Li, Ning Ding
Summary: Novel cabazitaxel analogues with potent cytotoxicity against various cell lines were synthesized and evaluated. In vivo assessment on SCID mice showed two analogues had similar antitumor activity to cabazitaxel, with one potentially serving as a strong drug candidate based on preliminary studies.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Yong Qu, Tian-Yi Zhou, Feng-Wei Guo, Mei-Yan Wei, Guang-Ying Chen, Yu-Cheng Gu, Chang-Yun Wang, Chang-Lun Shao
Summary: Inflammation is associated with various diseases and there is a need for better anti-inflammatory drugs. This study synthesized and characterized eight enantiopure isomers of yaequinolone alkaloids. The synthesized compounds showed significant anti-inflammatory activities, surpassing the effectiveness of indomethacin. Additionally, certain compounds displayed inhibition of IL-6 production, indicating their potential as new anti-inflammatory agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Michal Jurasek, Jan Valecka, Ivan Novotny, Zdenek Kejik, Jan Fahnrich, Anna Maresova, Jan Tauchen, Petr Bartunek, Bohumil Dolensky, Milan Jakubek, Pavel B. Drasar, Jarmila Kralova
Summary: New cationic analogues of BODIPY-Cholesterol have been discovered, with faster internalization and slightly different intracellular localization levels compared to traditional TF-Chol, showing potential for monitoring cholesterol changes in cells.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Shintaro Kusaka, Kazuki Yamamoto, Motoko Shinohara, Yusuke Minato, Satoshi Ichikawa
Summary: An alternative total synthesis of capuramycin and its analogues has been achieved, with a suggestion that a specific analogue may serve as a lead structure for further development due to its equivalent antibacterial activity against Mycobacterium smegmatis and Mycobacterium avium.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Aticha Thiraporn, Nongluk Saikachain, Rungtiwa Khumjiang, Chatchai Muanprasat, Kwanruthai Tadpetch
Summary: The convergent total syntheses of three 14-membered macrolide natural products have been achieved. Key synthetic features include Shiina macrolactonization, Wittig or Still-Gennari olefination, and selective reduction of propargylic alcohol. Cross metathesis was also highlighted as an efficient tool. The synthetic macrolides were evaluated for their cytotoxic activity and inhibitory effect on CFTR-mediated chloride secretion.
CHEMISTRY-AN ASIAN JOURNAL
(2022)
Article
Biochemistry & Molecular Biology
Kazuhiro Okamoto, Aoi Ishikawa, Ryotaro Okawa, Kazuki Yamamoto, Toyotaka Sato, Shin-ichi Yokota, Kazuhiro Chiba, Satoshi Ichikawa
Summary: This study successfully simplified the chemical structures of Muraymycins and caprazamycins through structure based drug design, leading to the discovery of a novel compound scaffold with sub-micromolar MraY inhibitory activity. This scaffold shows potential for further optimization of antibacterial activities in the future.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Xiao Zhang, Weiwei Yu, Xiaoyong Xu, Xusheng Shao, Zhong Li
Summary: A serendipitous reaction of introducing nitro group from nitromethylene was observed in the studies on dihydroxy intermediate synthesis. Dinitration structures with nitromethylene analogues were prepared under mild conditions by using a metal-free catalyst B(OH)3, instead of expected dihydroxy compounds. The extra nitro group was suggested to be from starting material.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Organic
Brittney A. Haney, Cassandra L. Schrank, William M. Wuest
Summary: This study explores isosteric substitutions within the scaffold of retinoids to improve the therapeutic viability against MRSA. A new class of analogs containing azaborine substituents instead of naphthalene moiety has been proposed to address issues such as low solubility and high affinity for binding proteins. The synthesis, antimicrobial activity, and physiochemical properties of these analogs are described in this study.
TETRAHEDRON LETTERS
(2021)
Article
Chemistry, Medicinal
Michael P. Badart, Emma M. Barnes, Andrew P. Cording, Selena C. L. Gilmer, Ian D. Billinghurst, Veera V. Shivaji R. Edupuganti, Guillaume Lessene, Abigail R. Bland, Rebekah L. Bower, Zohaib Rana, Scott A. Ferguson, Helen K. Opel Reading, Gregory M. Cook, Rhonda J. Rosengren, Kurt L. Krause, Allan B. Gamble, John C. Ashton, Bill C. Hawkins
Summary: A second-generation enantiospecific synthesis of spiroleucettadine was described, with a focus on the anti-proliferative activity of synthetic samples compared to natural sources. Efforts to alter the structure at specific positions led to the synthesis of analogues showing similar anti-proliferative profiles against lung cancer cell lines.
Article
Chemistry, Medicinal
Junmin Dong, Xuan Pan, Ying Yang, Guangyan Zhang, Zhiyan Xiao, Zhanzhu Liu
Summary: Newly synthesized exiguamine A analogues demonstrated potent inhibitory activities against IDO1, with compound 21f showing high selectivity for IDO1 and no cytotoxicity. Further optimization and evaluation of compound 21f is warranted.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Benjamin Owen, Monica de Gaetano, Andrew Gaffney, Catherine Godson, Patrick J. Guiry
Summary: The researchers synthesized BCP-containing synthetic lipoxin A4 mimetics and found that one of them exhibited high anti-inflammatory activity.
Article
Chemistry, Multidisciplinary
Mao Xie, Huixian Wu, Jing Bian, Shutong Huang, Yuanzheng Xia, Yujun Qin, Zhiming Yan
Summary: This study designed and synthesized a series of capsaicin analogues and found that some of them exhibited stronger antioxidant activity than quercetin. Among the compounds, the representative compound 3k showed great protective effects against H2O2-induced oxidative damage at low concentrations, reduced intracellular ROS accumulation, increased GSH levels, and improved mitochondrial membrane potential in SY5Y cells treated with H2O2, thus playing a role in preventing neuronal cell death.
Article
Chemistry, Multidisciplinary
Christian Paul Bold, Melanie Gut, Jasmine Schurmann, Daniel Lucena-Agell, Jurg Gertsch, Jose Fernando Diaz, Karl-Heinz Altmann
Summary: The study describes the convergent synthesis of analogues of the marine macrolide (-)-zampanolide, incorporating an embedded N-substituted morpholine moiety. Among the three investigated morpholino-zampanolides, the N-acetyl and N-benzoyl derivatives both showed nanomolar antiproliferative activity, while the N-tosyl derivative had significantly reduced activity.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Chemistry, Multidisciplinary
Simon Gueckel, Josef B. G. Gluyas, Samantha G. Eaves, Parvin Safari, Dmitry S. Yufit, Alexandre N. Sobolev, Martin Kaupp, Paul J. Low
CHEMISTRY-A EUROPEAN JOURNAL
(2019)
Editorial Material
Oncology
Hinrich Gronemeyer
INTERNATIONAL JOURNAL OF CANCER
(2020)
Editorial Material
Oncology
Hinrich Gronemeyer
INTERNATIONAL JOURNAL OF CANCER
(2020)
Article
Multidisciplinary Sciences
Maha Siouda, Audrey D. Dujardin, Laetitia Barbollat-Boutrand, Marco A. Mendoza-Parra, Benjamin Gibert, Maria Ouzounova, Jebrane Bouaoud, Laurie Tonon, Marie Robert, Jean-Philippe Foy, Vincent Lavergne, Serge N. Manie, Alain Viari, Alain Puisieux, Gabriel Ichim, Hinrich Gronemeyer, Pierre Saintigny, Peter Mulligan
Correction
Biochemistry & Molecular Biology
Angela Nebbioso, Fabio Manzo, Marco Miceli, Mariarosaria Conte, Lucrezia Manente, Alfonso Baldi, Antonio De Luca, Dante Rotili, Sergio Valente, Antonello Mai, Alessandro Usiello, Hinrich Gronemeyer, Lucia Altucci
Article
Chemistry, Inorganic & Nuclear
Simon Guckel, Parvin Safari, Seyed Mohammad Bagher Hosseini Ghazvini, Michael R. Hall, Josef B. G. Gluyas, Martin Kaupp, Paul J. Low
Summary: The spectroelectrochemically generated infrared and near-infrared spectra of two homo-bimetallic cations were analyzed using density functional theory calculations, revealing differences in electronic localization between the Fe(II)-Fe(III) mixed-valence cation and the more delocalized Ru(II) cation.
Editorial Material
Oncology
Hinrich Gronemeyer, Nicole Y. Souren
INTERNATIONAL JOURNAL OF CANCER
(2021)
Editorial Material
Oncology
Hinrich Gronemeyer
INTERNATIONAL JOURNAL OF CANCER
(2022)
Review
Oncology
Yasenya Kasikci, Hinrich Gronemeyer
Summary: Cancer genetics and genomics have provided insights into tumor development and heterogeneity. However, current cancer research may overlook complexity and individual diversity. A systems approach that reconstructs altered information networks and identifies key regulators is suggested. Individualized strategies are favored, as interindividual variability within patient cohorts is too high to extract common polygenic network information. A multinational and multidisciplinary effort is needed to develop dynamic regulatory networks and propose targeted therapies based on altered information transfer in individual cancers.
INTERNATIONAL JOURNAL OF CANCER
(2022)
Article
Chemistry, Multidisciplinary
Parvin Safari, Simon Gueckel, Josef B. G. Gluyas, Stephen A. Moggach, Martin Kaupp, Paul J. Low
Summary: The electronic structure and spectroscopic properties of ligand-bridged, bimetallic 'mixed-valence' complexes are determined by electronic couplings and orbital overlaps between the metal centers. The population distribution and dominant electronic structure can be biased by the steric and electronic properties of the bridge.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Article
Cell Biology
A. Huyghe, G. Furlan, J. Schroeder, E. Cascales, A. Trajkova, M. Ruel, F. Studer, M. Larcombe, Y. Bo Yang Sun, F. Mugnier, L. De Matteo, A. Baygin, J. Wang, Y. Yu, N. Rama, B. Gibert, J. Kielbassa, L. Tonon, P. Wajda, N. Gadot, M. Brevet, M. Siouda, P. Mulligan, R. Dante, P. Liu, H. Gronemeyer, M. Mendoza-Parra, J. M. Polo, F. Lavial
Summary: Coordinated changes of cellular plasticity and identity are critical for pluripotent reprogramming and oncogenic transformation. This study provides insights into the partitioned control of cellular plasticity and identity for both regenerative and cancer biology.
NATURE CELL BIOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Daniel P. Harrison, Varshini J. Kumar, Johanna N. Noppers, Josef B. G. Gluyas, Alexandre N. Sobolev, Stephen A. Moggach, Paul J. Low
Summary: This article describes a convenient modification to established synthetic routes for the preparation of complexes, as well as the differences in oxidation processes between iron and ruthenium analogues. The study also reveals limited differences in the gross electronic structures of Cp vs. Cp* derivatives in both iron and ruthenium series through redox properties and spectroelectrochemical investigations.
NEW JOURNAL OF CHEMISTRY
(2021)
Article
Oncology
Akinchan Kumar, Yasenya Kasikci, Alaa Badredine, Karim Azzag, Marie L. Quintyn Ranty, Falek Zaidi, Nathalie Aragou, Catherine Mazerolles, Bernard Malavaud, Marco A. Mendoza-Parra, Laurence Vandel, Hinrich Gronemeyer
Summary: Prostate cancer shows diverse patient-specific network alterations, with different signaling pathways affected by mutations and altered gene expression. In individual cases, deregulated pathways share common factors and have synergistic effects on cancer progression, providing a paradigm for identifying druggable key deregulated factors within regulatory networks for personalized therapies.
AMERICAN JOURNAL OF CANCER RESEARCH
(2021)
Article
Biology
Matthias Blum, Pierre-Etienne Cholley, Valeriya Malysheva, Samuel Nicaise, Julien Moehlin, Hinrich Gronemeyer, Marco Antonio Mendoza-Parra
LIFE SCIENCE ALLIANCE
(2020)
Article
Mathematical & Computational Biology
Pierre-Etienne Cholley, Julien Moehlin, Alexia Rohmer, Vincent Zilliox, Samuel Nicaise, Hinrich Gronemeyer, Marco Antonio Mendoza-Parra
NPJ SYSTEMS BIOLOGY AND APPLICATIONS
(2018)
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)