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Journal Bioorg. Med. Chem.

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Corrigendum to "Design, synthesis, and bioactivity of dihydropyrimidine derivatives as kinesin spindle protein inhibitors" [Bioorg. Med. Chem. 27 (2019) 115126].

Haytham O Tawfik, Tarek F El-Moselhy, Nabaweya S El-Din, Mervat H El-Hamamsy,

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115687]

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A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors.

Natalie G Barnes, Anthony W Parker, Amjed A Ahmed Mal Ullah, Patricia A Ragazzon, John A Hadfield,

A series of combretastatin derivatives were designed and synthesised by a two-step stereoselective synthesis by use of Wittig olefination followed by Suzuki cross-coupling. Interestingly, all new compounds (2a-2i) showed potent cell-based antiproliferative activities in nanomolar concentrations. Among the compounds, 2a, 2b and 2e were the most active across three cancer ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115684]

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Discovery and optimization of pyrazolopyrimidine sulfamates as ATG7 inhibitors.

Shih-Chung Huang, Sharmila Adhikari, James E Brownell, Emily F Calderwood, Jouhara Chouitar, Natalie Roy D'Amore, Dylan B England, Klaudia Foley, Sean J Harrison, Patrick J LeRoy, David Lok, Anna Lublinsky, Li-Ting Ma, Saurabh Menon, Yu Yang, Ji Zhang, Alexandra E Gould,

Autophagy is postulated to be required by cancer cells to survive periods of metabolic and/or hypoxic stress. ATG7 is the E1 enzyme that is required for activation of Ubl conjugation pathways involved in autophagosome formation. This article describes the design and optimization of pyrazolopyrimidine sulfamate compounds as potent and selective ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115681]

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Design, synthesis and biological evaluation of 4-aryl-5-aminoalkyl-thiazole-2-amines derivatives as ROCK II inhibitors.

Shuchao Ma, Linan Wang, Ben Ouyang, Meixia Fan, Junhui Qi, Lei Yao,

A series of 4-aryl-5-aminoalkyl-thiazole-2-amines were designed and synthesized, and their inhibitory activity on ROCK II was screened by enzyme-linked immunosorbent assay (ELISA). The results showed that 4-aryl-5-aminomethyl-thiazole-2-amines derivatives had certain ROCK II inhibitory activities. Compound 10l showed ROCK II inhibitory activity with IC50 value of 20 nM. ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115683]

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Lipoic acid modified antimicrobial peptide with enhanced antimicrobial properties.

Wenya Zhou, Yawei Du, Xinsong Li, Chen Yao,

RIWVIWRR-NH2 (Bac8c) is a natural antimicrobial peptide (AMP) exhibiting great antibacterial activity against Gram-negative and Gram-positive bacteria. In this work, lipoic acid was used as a fatty acid hydrophobic ligand to modify Bac8c (LA-Bac8c) to further improve its antimicrobial properties. Minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) assays ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115682]

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Potent double prodrug forms of synthetic phosphoantigens.

Nyema M Harmon, Xueting Huang, Megan A Schladetsch, Chia-Hung Christine Hsiao, Andrew J Wiemer, David F Wiemer,

Phosphoantigens are ligands of BTN3A1 that stimulate anti-cancer functions of γδ T cells, yet the potency of natural phosphoantigens is limited by low cell permeability and low metabolic stability. Derivatives of BTN3A1 ligand prodrugs were synthesized that contain an acetate-protected allylic alcohol and act as doubly protected prodrugs. A novel ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115666]

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Improved design of peptides exhibiting angiogenic activities for clinical applications.

Yuki Tominaga, Atsushi Kitagawa, Kiyoshi Nokihara,

Vascularization is one of the key steps for engraftment in regenerative medicine. Previously one of the authors had discovered peptides exhibiting significant angiogenic activities designated AGP and elucidated the active core. For neovascularization basic fibroblast growth factor is used although permeation can be envisaged. The original AGPs did not suffer ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115685]

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Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFRL858R/T790M.

Jiaan Shao, Shuangrong Liu, Xingyu Liu, Youlu Pan, Wenteng Chen,

The covalent binding nature of irreversible kinase inhibitors potentially increases the severity of "off-target" toxicity. Based on our continual strategy of chemically tuning the Michael addition acceptors, herein, we further explore the relationship among the electronic nature of Michael addition acceptors and EGFRT790M mutation selectivity as well as "off-target" toxicity ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115680]

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Erratum to "Synthesis, F-18 radiolabeling, and microPET evaluation of 3-(2,4-dichlorophenyl)-N-alkyl-N-fluoroalkyl-2,5-dimethylpyrazolo[1,5-a]pyrimidin-7-amines as ligands of the corticotropin-releasing factor type-1 (CRF1) receptor" [Bioorg. Med. Chem. 23 (2015) 4286-4302].

Jeffrey S Stehouwer, Matthew S Birnbaum, Ronald J Voll, Michael J Owens, Susan J Plott, Chase H Bourke, Michael A Wassef, Clinton D Kilts, Mark M Goodman,

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115660]

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SAR study of bisamides as cyclophilin a inhibitors for the development of host-targeting therapy for hepatitis C virus infection.

Xiaoli Li, Jinhe Han, Hye Won Lee, Yi-Seul Yoon, Yifeng Jin, Daulat B Khadka, Suhui Yang, Meehyein Kim, Won-Jea Cho,

The therapy of chronic hepatitis C virus infections has significantly improved with the development of direct-acting antivirals (DAAs), which contain NS3/4A protease, NS5A, and NS5B polymerase inhibitors. However, mutations in specific residues in these viral target genes are associated with resistance to the DAAs. Especially inhibitors of NS3/4A protease and ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115679]

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Uridine natural products: Challenging targets and inspiration for novel small molecule inhibitors.

Christine A Arbour, Barbara Imperiali,

Nucleoside derivatives, in particular those featuring uridine, are familiar components of the nucleoside family of bioactive natural products. The structural complexity and biological activities of these compounds have inspired research from organic chemistry and chemical biology communities seeking to develop novel approaches to assemble the challenging molecular targets, to gain ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(18):115661]

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Total synthesis and a systematic structure-activity relationship study of WAP-8294A2.

Delin Chen, Liwen Tian, Kathy Hiu Laam Po, Sheng Chen, Xuechen Li,

WAP-8294A2 is a cyclic peptide antibiotic with novel structure and excellent activity against Gram-positive pathogens. Herein, we report the total synthesis of complex macrocyclic peptide WAP-8294A2 (W1), ent-analogue W2, deoxy analogue W3 and de-methyl analogue W4 using a solid-phase synthetic route followed by a final stage solution-phase cyclization reaction. Exploitation ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(18):115677]

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New cannabinoid receptor antagonists as pharmacological tool.

Pedro González-Naranjo, Concepción Pérez, Rocío Girón, Eva M Sánchez-Robles, María I Martín-Fontelles, Natalia Carrillo-López, Julia Martín-Vírgala, Manuel Naves, Nuria E Campillo, Juan A Páez,

Synthesis and pharmacological evaluation of a new series of cannabinoid receptor antagonists of indazole ether derivatives have been performed. Pharmacological evaluation includes radioligand binding assays with [3H]-CP55940 for CB1 and CB2 receptors and functional activity for cannabinoid receptors on isolated tissue. In addition, functional activity of the two synthetic cannabinoids ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115672]

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Synthesis and evaluation of 17α-triazolyl and 9α-cyano derivatives of estradiol.

Edward A Wetzel, Alicia M Hanson, Callie L Troutfetter, Daniel J Burkett, Daniel S Sem, William A Donaldson,

A variety of 17α-triazolyl and 9α-cyano derivatives of estradiol were prepared and evaluated for binding to human ERβ in both a TR-FRET assay, as well as ERβ and ERα agonism in cell-based functional assays. 9α-Cyanoestradiol (5) was nearly equipotent as estradiol as an agonist for both ERβ and ERα. The ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115670]

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Induction of potent cell growth inhibition by schizophyllan/K-ras antisense complex in combination with gemcitabine.

Shogo Sasaki, Hiroto Izumi, Yasuo Morimoto, Kazuo Sakurai, Shinichi Mochizuki,

Antisense oligonucleotides (AS-ODNs) specifically hybridize with target mRNAs, resulting in interference with the splicing mechanism or the regulation of protein translation. In our previous reports, we demonstrated that β-glucan schizophyllan (SPG) can form a complex with AS-ODNs attached with oligo deoxyadenosine dA40 (AS-ODN-dA40/SPG), and that this complex can be recognized ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(18):115668]

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Galangin ameliorated pulmonary fibrosis in vivo and in vitro by regulating epithelial-mesenchymal transition.

Liqun Wang, Hongyao Liu, Qiurong He, Cailing Gan, Yali Li, Qianyu Zhang, Yuqin Yao, Fang He, Tinghong Ye, Wenya Yin,

Pulmonary fibrosis (PF) is a disease that is characterized by abnormal epithelial-mesenchymal transition (EMT) and persistent inflammatory injury, with high mortality and poor prognosis, but the current therapies are accompanied by certain adverse side effects. In this study, we investigated the role of galangin (GA), an anti-inflammatory and anti-tumoral phytochemical ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115663]

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The multifunctional dopamine D2/D3 receptor agonists also possess inhibitory activity against the full-length tau441 protein aggregation.

Iva Ziu, Irving Rettig, Dan Luo, Aloke Dutta, Theresa M McCormick, Colin Wu, Sanela Martic,

Neurodegeneration leads to variety of diseases which are linked to aberrant protein or peptide aggregation, as a one possible mechanism. Hence, small drug molecules targeting aggregation are of interest. Tau protein aggregation is one of the biomarkers of neurodegenerative diseases and is a viable drug target. Toward multifunctional inhibitors, we ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(18):115667]

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Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors.

Zhen Xiao, Cilong Chu, Lingjia Zhou, Zhihui Zhou, Qian Zhang, Feiyi Yang, Zunhua Yang, Pengwu Zheng, Shan Xu, Wufu Zhu,

A series of novel thiapyran-pyrimidine derivatives (10a-10h, 11a-11g, 12a-12f, 13a-13f, 14a-14f) were synthesized and their antiproliferative activities were tested. Most of the target compounds showed good activity on one or more cancer cell lines but low activity on human normal cell LO2. The most promising compound 13a exhibited the similar ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(19):115669]

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Design and synthesis of β-strand-fixed peptides inhibiting aggregation of amyloid β-protein.

Fumiya Tanaka, Kana Shibata, Yoko Monobe, Ken-Ichi Akagi, Yuichi Masuda,

Aggregation of 42-residue amyloid β-protein (Aβ42) can be prevented by β-sheet breaker peptides (BSBps) homologous to LVFFA residues, which are included in a β-sheet region of Aβ42 aggregates. To enhance the affinity of BSBps to the Aβ42 aggregates, we designed and synthesized β-strand-fixed peptides (BSFps) whose side chains were cross-linked ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(18):115676]

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Genetically encoding thyronine for fluorescent detection of peroxynitrite.

Shanshan Li, Bing Yang, Tomonori Kobayashi, Bingchen Yu, Jun Liu, Lei Wang,

Peroxynitrite is a highly reactive oxidant effecting cell signaling and cell death. Here we report a fluorescent protein probe to selectively detect peroxynitrite. A novel unnatural amino acid, thyronine (Thy), was genetically encoded in E. coli and mammalian cells by evolving an orthogonal tRNAPyl/ThyRS pair. Incorporation of Thy into the ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(18):115665]

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Synthesis and activity of isoleucine sulfonamide derivatives as novel botulinum neurotoxin serotype A light chain inhibitors.

Jordan C Thompson, Wendy T Dao, Alex Ku, Sandra L Rodriguez-Beltran, Martin Amezcua, Alejandra Y Palomino, Thanh Lien, Nicholas T Salzameda,

The botulinum neurotoxin (BoNT) is the most lethal protein known to man causing the deadly disease botulinum. The neurotoxin, composed of a heavy (HC) and light (LC) chain, work in concert to cause muscle paralysis. A therapeutic strategy to treat individuals infected with the neurotoxin is inhibiting the catalytic activity ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(18):115659]

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Dimeric small molecule agonists of EphA2 receptor inhibit glioblastoma cell growth.

Cody M Orahoske, Yaxin Li, Aaron Petty, Fatma M Salem, Jovana Hanna, Wenjing Zhang, Bin Su, Bingcheng Wang,

EphA2 receptor kinase could become a novel target for anti-glioblastoma treatment. Doxazosin previously identified acts like the endogenous ligand of EphA2 and induces cell apoptosis. Through lead structure modification a derivative of Doxazosin possessing unique dimeric structure showed an improvement in the activity. In the current study, we expanded the ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(18):115656]

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Boronic acid-based arginase inhibitors in cancer immunotherapy.

Bartlomiej Borek, Tadeusz Gajda, Adam Golebiowski, Roman Blaszczyk,

Arginase is an enzyme that converts l-arginine to l-ornithine and urea in the urea cycle. There are two isoforms of arginase in mammals: ARG-1 and ARG-2. l-Arginine level changes occur in patients with various types of affliction. An overexpression of arginase leads to the depletion of arginine and then to ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(18):115658]

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Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.

Aladdin M Srour, Nesreen S Ahmed, Somaia S Abd El-Karim, Manal M Anwar, Salwa M El-Hallouty,

Heterocyclic rings such as thiazole and benzimidazole are considered as privileged structures, since they constitute several FDA-approved drugs for cancer treatment. In this work, a new set of 2-(2-(substituted) hydrazinyl)-4-(1-methyl-1H-benzo[d]imidazol-2-yl) thiazoles 4a-q were designed as epidermal growth factor receptor (EGFR) inhibitors and synthesized using concise synthetic methods. The new target ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(18):115657]

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Identification of the first noncompetitive SARM1 inhibitors.

Heather S Loring, Sangram S Parelkar, Santanu Mondal, Paul R Thompson,

Sterile Alpha and Toll Interleukin Receptor Motif-containing protein 1 (SARM1) is a key therapeutic target for diseases that exhibit Wallerian-like degeneration; Wallerian degeneration is characterized by degeneration of the axon distal to the site of injury. These diseases include traumatic brain injury, peripheral neuropathy, and neurodegenerative diseases. SARM1 promotes neurodegeneration ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2020, 28(18):115644]

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