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Combined active pocket and hinge region engineering to develop an NADPH-dependent phenylglycine dehydrogenase.

Xinjian Yin, Yujing Zeng, Jun Chen, Lan Liu, Zhizeng Gao,

NADPH-dependent amino acid dehydrogenases (AADHs) are favorable enzymes to construct artificial biosynthetic pathways in whole-cell for high-value noncanonical amino acids (NcAAs) production. Glutamate dehydrogenases (GluDHs) represent attractive candidates for the development of novel NADPH-dependent AADHs. Here, we report the development of a novel NADPH-dependent phenylglycine dehydrogenase by combining active pocket ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2022, 120:105601]

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Enzyme engineering improves catalytic efficiency and enantioselectivity of hydroxynitrile lyase for promiscuous retro-nitroaldolase activity.

Badipatla Vishnu Priya, D H Sreenivasa Rao, Rubina Gilani, Surabhi Lata, Nivedita Rai, Mohd Akif, Santosh Kumar Padhi,

Protein engineering to improve promiscuous catalytic activity is important for biocatalytic application of enzymes in green synthesis. We uncovered the significance of binding site residues in Arabidopsis thaliana hydroxynitrile lyase (AtHNL) for promiscuous retro-nitroaldolase activity. Engineering of AtHNL has improved enantioselective retro-nitroaldolase activity, a synthetically important biotransformation, for the production ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2022, 120:105594]

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Rates of competing fluoride elimination and iodination from a thiamin-derived Breslow intermediate.

Nathan Wu, Ronald Kluger,

Rates of fluoride elimination and iodination of the Breslow intermediate (BI) derived from 2-(1-hydroxy-2,2,2-trifluoroethyl)-thiamin provide a quantitative assessment of competing reactions at C2α of the BI. The competition probes the intrinsic reactivity of this important class of intermediates. Fluoride elimination, which occurs upon formation of the BI, produces 2-(2',2'-difluoroacetyl)-thiamin, while ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2022, 120:105579]

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Corrigendum to "Design and synthesis of novel isatin-based derivatives targeting cell cycle checkpoint pathways as potential anticancer agents" [Bioorg. Chem. 105 (2020) 104366].

Mohamed A Yousef, Ahmed M Ali, Wael M El-Sayed, Wesam S Qayed, Hassan H A Farag, Tarek Aboul-Fadl,

Bioorg Chem (Bioorganic chemistry)
[2022, 120:105598]

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Structural modification and strategies for the enhanced doxorubicin drug delivery.

Shah Alam Khan, Md Jawaid Akhtar,

Doxorubicin belongs to the anthracycline chemical class of the drug and is one of the widely used anticancer drugs. The common side effects of doxorubicin include vomiting, hair loss, rashes to serious side-effects such as irreversible cardiotoxicity, and drug-induced leukemia. This led many researchers around the globe to develop methods ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2022, 120:105599]

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Anti-leukemic effect and molecular mechanism of 11-methoxytabersonine from Melodinus cochinchinensis via network pharmacology, ROS-mediated mitochondrial dysfunction and PI3K/Akt signaling pathway.

Yong-Peng Wang, Fei Pan, Yu-Dan Wang, Afsar Khan, Ya-Ping Liu, Mei-Lian Yang, Jian-Xin Cao, Tian-Rui Zhao, Gui-Guang Cheng,

Melodinus cochinchinensis (Lour.) Merr. is a Yunnan endemic folk medicine. Our previous study showed that 11-methoxytabersonine (11-MT) isolated from M. cochinchinensis has strong cytotoxicity on human T-ALL cells, but its molecular mechanism has not been studied. In current study, the cytotoxicity and possible mechanism of 11-MT on T-cell acute lymphoblastic ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2022, 120:105607]

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Characterization of novel heterocyclic compounds based on 4-aryl-4H-chromene scaffold as anticancer agents: Design, synthesis, antiprofilerative activity against resistant cancer cells, dual β-tubulin/c-Src inhibition, cell cycle arrest and apoptosis induction.

Eman K A Abdelall, Heba A H Elshemy, Madlen B Labib, Fatma E A Mohamed,

In this study, three novel sets of 4-aryl-4H-chromene derivatives 4a-c, 6a-d and 7a-c were synthesized and evaluated for anticancer activity. Characterization of new compounds was established on basis of elemental analyses and spectral data. All new compounds were investigated for their antiproliferative activity against HCT-116, HepG-2 and MCF-7 cell lines ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 120:105591]

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Recent advances in B-RAF inhibitors as anticancer agents.

Pathan Shahebaaz Khan, Patil Rajesh, Patil Rajendra, Manohar G Chaskar, Arote Rohidas, Sangshetti Jaiprakash,

The significance of B-RAF in the promotion of cell proliferation and motility was explored by the researchers in the past. However, in 2002, several researchers found that mutation in B-RAF leads to cancer. Extensive research on B-RAF mutations suggested B-RAF V600E mutation as a critical predictive, prognostic and diagnostic biomarker ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2022, 120:105597]

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Corrigendum to "Daphnegiravone D from Daphne giraldii induces cell death by targeting ATR in Hep3B cells" [Bioorg. Chem. 110 (2021) 104802].

Xin-Yue Shang, Xiao-Qi Yu, Guo-Dong Yao, Shao-Jiang Song,

Bioorg Chem (Bioorganic chemistry)
[2022, 119:105584]

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Design, synthesis and structure-activity relationship optimization of phenanthridine derivatives as new anti-vitiligo compounds.

Bi-Juan Yang, Shi-Rui Fan, Xin-Fang Zhang, Jie-Yun Cai, Ting Ruan, Zheng-Rui Xiang, Juan Ren, Xiao-Jiang Hao, Duo-Zhi Chen,

Humans have been suffering from vitiligo for a long time. Target vitiligo drugs have yet been approved. Activation of Wnt/β-catenin signalling has potential in the therapeutic use of vitiligo, so exploring new drugs that specifically directly activate Wnt is worthwhile to obtain new anti-vitiligo agents. In this work, two portions ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 119:105582]

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New aniline derivatives from the volva of Phallus rubrovolvatus and their anti-inflammatory activity.

Jianhua Lv, Lan Yao, Shiyu Li, Jing Dong, Mingyu Ye, Dongyu Fan, Changtian Li, Fenghua Tian, Yu Li,

Phallus rubrovolvatus is an important commercially cultivated mushroom species in China. However, the volva of P. rubrovolvatus usually discarded as a by-product due to the unpleasant flavor and difficulty in processing. In this study, we investigated the chemical constituents and bioactivities of the volva of P. rubrovolvatus. As a result, ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 119:105577]

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In vitro potential antiviral SARS-CoV-19- activity of natural product thymohydroquinone and dithymoquinone from Nigella sativa.

Eman R Esharkawy, Faisal Almalki, Taibi Ben Hadda,

Inflammation, oxidation, and compromised immunity all increase the dangers of COVID-19, whereas many pharmaceutical protocols may lead to increased immunity such as ingesting from sources containing vitamin E and zinc. A global search for natural remedies to fight COVID-19 has emerged, to assist in the treatment of this infamous coronavirus. ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2022, 120:105587]

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Structures and antitumor activities of ten new and twenty known surfactins from the deep-sea bacterium Limimaricola sp. SCSIO 53532.

Wenping Ding, Yanqun Li, Min Chen, Rouwen Chen, Xinpeng Tian, Hao Yin, Si Zhang,

Surfactins are natural biosurfactants with myriad potential applications in the areas of healthcare and environment. However, surfactins were almost exclusively produced by the bacterium Bacillus species in previous reported literatures, together with difficulty in isolating pure monomer, which resulted in making extensive effort to remove duplication and little discovery of ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 120:105589]

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Novel imidazo[1,2-a]pyridine derivatives as potent ATX allosteric inhibitors: Design, synthesis and promising in vivo anti-fibrotic efficacy in mice lung model.

Hongrui Lei, Zhen Li, Tong Li, Huinan Wu, Jing Yang, Xinlian Yang, Yu Yang, Nan Jiang, Xin Zhai,

Aiming to develop novel allosteric autotaxin (ATX) inhibitors, hybrid strategy was utilized by assembling the benzyl carbamate fragment in PF-8380 onto the imidazo[1,2-a]pyridine skeleton of GLPG-1690. The piperazine moiety in GLPG-1690 was replaced with phenyl ring to enhance the π-π interactions with adjacent residues. In the light of FS-3 based ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 120:105590]

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Design, synthesis and SAR study of Fluorine-containing 3rd-generation taxoids.

Changwei Wang, Lei Chen, Yi Sun, Wanrong Guo, Adam K Taouil, Iwao Ojima,

It has been shown that the incorporation of fluorine or organofluorine groups into pharmaceutical and agricultural drugs often induces desirable pharmacological properties through unique protein-drug interactions involving fluorine. We have reported separately remarkable effects of the 2,2-difluorovinyl (DFV) group at the C3' position, as well as those of the CF<sub>3</sub>O ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 119:105578]

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Discovery of novel cholic acid derivatives as highly potent agonists for G protein-coupled bile acid receptor.

Mingcheng Qian, Zhijie Luo, Wenwen Hou, Jingjing Sun, Xin Lu, Qianxi Zhang, Yi Wu, Caile Xue, Shuai Zhao, Xin Chen,

In this study, fourteen new cholic acid (CA) derivatives were designed and synthesized, and the GloSensor cAMP accumulation assay indicated that all derivatives could activate the Takeda G protein-coupled receptor 5 (TGR5). Methylation of 7- and 12-hydroxyl groups in CA significantly increased TGR5 agonism for the new derivatives. For example, ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 120:105588]

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Discovery of linear unnatural peptides as potent mutant isocitrate dehydrogenase 1 inhibitors by Ugi reaction.

Xuechen Zhou, Mengzhu Zheng, Na Zhao, Yixin Hu, Kaiyin Yang, Junfeng Huo, Guangyuan Liu, Jiangeng Huang, Lixia Chen, Yirong Zhou, Hua Li,

Isocitrate dehydrogenases 1 (IDH1) catalyzes the oxidative decarboxylation of isocitrate to ɑ-ketoglutaric acid (α-KG). It is the most frequently mutated metabolic gene in human cancer and its mutations interfere with cell metabolism and epigenetic regulation, thus promoting tumorigenesis. In order to discover potent new mutant IDH1 inhibitors, based on the ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 119:105569]

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Caffeine improves the cytotoxic effect of dacarbazine on B16F10 murine melanoma cells.

Tatiane Renata Fagundes, Tiago Bervelieri Madeira, Gabriella Pasqual Melo, Heloíza Paranzini Bordini, Poliana Camila Marinello, Suzana Lucy Nixdorf, Alessandra Lourenço Cecchini, Rodrigo Cabral Luiz,

<h4>Objective</h4>Caffeine has been studied as a potentiating agent in chemotherapy against some types of cancer, but there are few reports on its effects on melanoma. This study aimed to investigate caffeine's ability to enhance the effects of dacarbazine in vitro.<h4>Materials and methods</h4>Murine melanoma B16F10 cells were treated 24 h with 1-40 µM ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 120:105576]

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Design, synthesis, and evaluation of novel pyridone derivatives as potent BRD4 inhibitors for the potential treatment of prostate cancer.

Wenhua Jiang, Xiaohui Wang, Chengxia Shu, Qiangqiang Hou, Kexin Yang, Xiaoxing Wu,

Since androgen receptor (AR) can bind to BRD4 protein and this binding can be blocked by BRD4 inhibitors, targeting BRD4 has emerged as a promising approach for the treatment of prostate cancer (PC). Herein, we designed and synthesized a series of 5-(1-benzyl-1H-indazol-6-yl)-4-ethoxy-1-methylpyridin-2(1H)-one derivatives as novel BRD4 inhibitors for prostate cancer. ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 119:105575]

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Development of novel indolin-2-one derivative incorporating thiazole moiety as DHFR and quorum sensing inhibitors: Synthesis, antimicrobial, and antibiofilm activities with molecular modelling study.

Abdullah Y Alzahrani, Yousry A Ammar, Mohammed Abu-Elghait, Mohamed A Salem, Mohammed A Assiri, Tarik E Ali, Ahmed Ragab,

Nowadays, it's imperative to develop novel antimicrobial agents active against both drug-sensitive and drug-resistant bacterial infections with favorable profiles as high efficacy, low toxicity, and short therapy duration. Accordingly, a series of new thiazolo-indolin-2-one derivatives were synthesized based on acid and base catalyzed condensation or reaction of thiosemicarbazone 8 with ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 119:105571]

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Structure elucidation, biogenesis, and bioactivities of acylphloroglucinol-derived meroterpenoid enantiomers from Dryopteris crassirhizoma.

Ping Hai, Kairui Rao, Na Jiang, Dan Liu, Ruirui Wang, Yuan Gao, Xiaocong Liu, Sihao Deng, Yu Zhou, Xuanqin Chen, Xiaonian Li, Rongtao Li,

Twenty-four racemic acylphloroglucinol meroterpenoids including eighteen unusual stuctures (3 ∼ 10, 13, 14, and 17 ∼ 24), and a major component filixic acid ABA (25), were isolated from Dryopteris crassirhizoma. Structurally, the dimeric acylphloroglucinol derivatives possess unprecedented skeletons of mixed acylphloroglucinol and sesquiterpene biosynthetic origin. The stereochemistries of six reported meroterpenoids with undefined chiral ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 119:105567]

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Novel thiophene Chalcones-Coumarin as acetylcholinesterase inhibitors: Design, synthesis, biological evaluation, molecular docking, ADMET prediction and molecular dynamics simulation.

Aso Hameed Hasan, Sankaranarayanan Murugesan, Syazwani Itri Amran, Subhash Chander, Mohammed M Alanazi, Taibi Ben Hadda, Sonam Shakya, Mohammad Rizki Fadhil Pratama, Basundhara Das, Subhrajit Biswas, Joazaizulfazli Jamalis,

A series of around eight novel chalcone based coumarin derivatives (23a-h) was designed, subjected to in-silico ADMET prediction, synthesized, characterized by IR, NMR, Mass analytical techniques and evaluated as acetylcholinesterase (AChE) inhibitor for the treatment of Alzheimer's disease (AD). The results of predicted ADMET study demonstrated the drug-likeness properties of ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 119:105572]

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Indoles and 1-(3-(benzyloxy)benzyl)piperazines: Reversible and selective monoamine oxidase B inhibitors identified by screening an in-house compound library.

Damijan Knez, Martina Hrast, Rok Frlan, Anja Pišlar, Simon Žakelj, Janko Kos, Stanislav Gobec,

The therapeutic indications for monoamine oxidases A and B (MAO-A and MAO-B) inhibitors that have emerged from biological studies on animal and cellular models of neurological and oncological diseases have focused drug discovery projects upon identifying reversible MAO inhibitors. Screening of our in-house academic compound library identified two hit compounds ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 119:105581]

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H2O2-Responsive amphiphilic polymer with aggregation-induced emission (AIE) for DOX delivery and tumor therapy.

Ya-Xuan Liang, Xue-Yi Sun, De-Zhong Xu, Jun-Ru Huang, Quan Tang, Zhong-Lin Lu, Rui Liu,

Stimuli-responsive drug delivery systems (DDSs) based on amphiphilic polymers have attracted much attention. In this study, we reported an innovative H<sub>2</sub>O<sub>2</sub>-responsive amphiphilic polymer (TBP), bearing a H<sub>2</sub>O<sub>2</sub>-sensitive phenylboronic ester, AIE fluorophore tetraphenylethene (TPE) hydrophobic, and polyethylene glycol hydrophilic (PEG) moieties. TBP could self-assemble into micelles with an encapsulation efficiency as ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 119:105559]

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The role of remote flavin adenine dinucleotide pieces in the oxidative decarboxylation catalyzed by salicylate hydroxylase.

Mozart S Pereira, Simara S de Araújo, Ronaldo A P Nagem, John P Richard, Tiago A S Brandão,

Salicylate hydroxylase (NahG) has a single redox site in which FAD is reduced by NADH, the O<sub>2</sub> is activated by the reduced flavin, and salicylate undergoes an oxidative decarboxylation by a C(4a)-hydroperoxyflavin intermediate to give catechol. We report experimental results that show the contribution of individual pieces of the FAD ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 119:105561]

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