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
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
Chemistry, Multidisciplinary
Liridona Useini, Marija Mojic, Markus Laube, Peter Loennecke, Jonas Dahme, Menyhart B. Sarosi, Sanja Mijatovic, Danijela Maksimovic-Ivanic, Jens Pietzsch, Evamarie Hey-Hawkins
Summary: Carborane analogues of mefenamic acid have stronger antitumor potential compared to the parent organic compound, inhibiting COX to reduce inflammation and pain, thereby showing potential applications for treating postoperative surgery and heavy menstrual bleeding.
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
Multidisciplinary Sciences
Rani Maharani, Orin Inggriani Napitupulu, Jelang M. Dirgantara, Ace Tatang Hidayat, Dadan Sumiarsa, Desi Harneti, Nurlelasari, Unang Supratman, Koichi Fukase
Summary: Synthesized cyclic c-PLAI analogues exhibited enhanced antimicrobial properties against most bacteria and fungi, especially those containing cationic lysine residues. Analogues containing a combination of lysine and aromatic residues showed broad-spectrum antimicrobial activity.
ROYAL SOCIETY OPEN SCIENCE
(2021)
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
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
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
Agriculture, Multidisciplinary
Lei Wang, Wenqi Fan, Li Cui, Na Yang, Xiao Zhang, Shujing Yu, Yonghong Li, Baolei Wang
Summary: In this study, a series of novel compounds were synthesized and tested for their biological activities. Some of these compounds showed favorable insecticidal, fungicidal, and herbicidal activities. These compounds have potential applications in controlling pests and diseases in agriculture, and they exhibit certain advantages compared to existing insecticides and fungicides. The structure-activity relationships of these compounds were summarized and discussed, and predictive models were constructed to gain insights into their bioactivity profiles. These findings have practical implications for the discovery and development of novel xanthine natural product-based pesticides.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
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, 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, 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
Biochemistry & Molecular Biology
Wen Ren, Rebecca Vairin, Jacob D. Ward, Ricardo Francis, Jenny VanNatta, Ruoli Bai, Pouguiniseli E. Tankoano, Yuling Deng, Ernest Hamel, Mary Lynn Trawick, Kevin G. Pinney
Summary: The oxetane functional group can offer potential advantages as a ketone surrogate in therapeutic agents. The replacement of the bridging ketone moiety with an oxetane group in OXi8006 has expanded our knowledge on structure-activity relationships and provided insights on the incorporation of oxetane within this class of molecules.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Dana R. Renk, Marcel Skraban, Dirk Bier, Annette Schulze, Erika Wabbals, Franziska Wedekind, Felix Neumaier, Bernd Neumaier, Marcus Holschbach
Summary: A series of 18 derivatives of 4-hydroxy-N-(4-methoxy-7-morpholin-4-yl-1,3-benzothiazol-2-yl)-4-methylpiperidine-1-carboxamide were designed and synthesized with high affinity and selectivity for human adenosine A(2A) receptors, particularly the fluorine-containing derivatives. Interestingly, binding values to rat A(2A) receptors were found to be higher compared to human receptors.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Plant Sciences
Yang Li, Wan-Li Tan, Kai Guo, Xiao-Wei Gao, Jun Wei, Dong Yi, Chun Zhang, Qin Wang
Summary: Falcarinol analogues (R)-2d and (R)-2i have shown neuroprotective effects on PC12 cells injured by NaN3, possibly through protecting against oxidative stress. Additionally, both falcarinol (1a) and its analogue (R)-2i exhibited potential L-type calcium channel-blocking activity, suggesting a possible mechanism for neuroprotection involving inhibition of calcium overload.
JOURNAL OF NATURAL PRODUCTS
(2021)
Article
Pharmacology & Pharmacy
Hussein N. Rubaiy, Melanie J. Ludlow, Karsten Siems, Katherine Norman, Richard Foster, Dietmar Wolf, John A. Beutler, David J. Beech
BRITISH JOURNAL OF PHARMACOLOGY
(2018)
Meeting Abstract
Oncology
Corena V. Shaffer, April L. Risinger, John A. Beutler, Susan L. Mooberry
Article
Biochemistry & Molecular Biology
Fatma Tosun, John A. Beutler, Tanya T. Ransom, Mahmut Miski
Article
Oncology
Corena V. Grant, Chase M. Carver, Shayne D. Hastings, Karthik Ramachandran, Madesh Muniswamy, April L. Risinger, John A. Beutler, Susan L. Mooberry
BREAST CANCER RESEARCH AND TREATMENT
(2019)
Article
Plant Sciences
Ana S. C. Valdeira, Emad Darvishi, Girma M. Woldemichael, John A. Beutler, Kirk R. Gustafson, Jorge A. R. Salvador
JOURNAL OF NATURAL PRODUCTS
(2019)
Article
Biochemistry & Molecular Biology
Sarah A. Long, Shan Huang, Anusha Kambala, Ling Ren, Jennifer Wilson, Michael Goetz, Xiaojiang Hao, Xiaosheng Yang, Ekaterina I. Goncharova, Libin Jia, Amy LeBlanc, Chand Khanna, Curtis J. Henrich, John A. Beutler
Summary: A high-throughput screening method was developed to identify compounds selectively inhibiting the in vitro growth of highly metastatic osteosarcoma cells, leading to the discovery of lovastatin and the limonoid toosendanin. Cerivastatin was identified as a particularly potent and selective agent, inducing apoptosis in metastatic osteosarcoma cells. These statins and limonoids may present new opportunities for studying osteosarcoma metastasis.
CHEMICAL BIOLOGY & DRUG DESIGN
(2021)
Article
Biochemistry & Molecular Biology
Fatma Tosun, Feyyaz Mihoglugil, John A. A. Beutler, Esra Eroglu Ozkan, Mahmut Miski
Article
Chemistry, Medicinal
Zhenhua Wu, Jean-Simon Suppo, Sarka Tumova, Jonathan Strope, Fernando Bravo, Melody Moy, Ethan S. Weinstein, Cody J. Peer, William D. Figg, William J. Chain, Antonio M. Echavarren, David J. Beech, John A. Beutler
ACS MEDICINAL CHEMISTRY LETTERS
(2020)
Article
Chemistry, Organic
Dongdong Wang, Wei Jiang, Chang-Kwon Kim, Heidi R. Bokesch, Girma M. Woldemichael, Berkley E. Gryder, John F. Shern, Jammed Khan, Barry R. O'Keefe, John A. Beutler, Kirk R. Gustafson
Summary: Neopetrothiazide (1) is a pentacyclic isoquinoline quinone isolated from a Neopetrosia sp. sponge. The structure elucidation was achieved through NMR experiments, revealing its unique thiazide-fused structural scaffold and 14 contiguous nonprotonated centers.
Article
Cell Biology
Patricia C. Cortelo, Daniel P. Demarque, Renata G. Dusi, Lorena C. Albernaz, Raimundo Braz-Filho, Ekaterina I. Goncharova, Heidi R. Bokesch, Kirk R. Gustafson, John A. Beutler, Laila S. Espindola
Summary: The study conducted high-throughput cytotoxicity screening on 702 extracts from 95 plant species in the Brazilian Cerrado biome, identifying 22 active extracts with significant cytotoxic activity against cancer cells. A molecular networking strategy annotated 27 compounds present in 17 active extracts, providing valuable chemical information for further studies on potential anticancer agents in plants.
Article
Plant Sciences
Fatma Tosun, Erdi C. Aytar, John A. Beutler, Jennifer A. Wilson, Mahmut Miski
Summary: Preliminary 2-day cancer cell screening assays showed strong cytotoxic activity in the dichloromethane extract of Heptaptera cilicica roots, resulting in the isolation of eleven sesquiterpene coumarin ethers with potent and selective cytotoxic activities. Revised spectroscopic data for 14'-acetoxybadrakemone and complete NMR spectroscopic assignments for colladonin and colladin were reported.
RECORDS OF NATURAL PRODUCTS
(2021)
Article
Chemistry, Medicinal
David P. Stockdale, John A. Beutler, David F. Wiemer
Summary: The stilbene moiety is commonly found in natural products and compounds with this structure exhibit a wide range of biological activity. However, the cis/trans isomerization of stilbenes is a potential limitation for developing useful drugs. In this study, analogues of two bioactive stilbenes were synthesized, in which a 1,2,3-triazole ring replaced the stilbene double bond, aiming to address this drawback while preserving the biological activity. The new analogue showed strong anti-proliferative activity against 60 cell lines, which correlated well with the compound that inspired its synthesis.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Meeting Abstract
Pharmacology & Pharmacy
Hussein Nori Rubaiy, Dietmar Wolf, John A. Beutler, David J. Beech
BRITISH JOURNAL OF PHARMACOLOGY
(2020)
Meeting Abstract
Chemistry, Multidisciplinary
Chloe Schroeder, Patrick Dey, John Beutler, David Wiemer
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY
(2018)
Article
Biochemistry & Molecular Biology
Graziella Tocco, Francesca Esposito, Pierluigi Caboni, Antonio Laus, John A. Beutler, Jennifer A. Wilson, Angela Corona, Stuart F. J. Le Grice, Enzo Tramontano
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2020)
