Discovery of monoamine oxidase A inhibitory peptides from hairtail (Trichiurus japonicus) using in vitro simulated gastrointestinal digestion and in silico studies.

abstract：:New thiazolylpyrazolyl coumarin derivatives were synthesized and tested for their anticancer potential in vitro against five different human cell lines, including breast MCF-7, lung A549, prostate PC3, liver HepG2 and normal melanocyte HFB4. Breast carcinoma revealed higher sensitivity towards compounds 7a, 8c, 9b, 9c...

journal_title：Bioorganic chemistry

authors： Mohamed TK,Batran RZ,Elseginy SA,Ali MM,Mahmoud AE

更新日期：2019-04-01 00:00:00

abstract：:A new series of derivatives characterized by the presence of the 3,4,5-trimethoxylbenzamide substituted benzofurans were synthesized and evaluated for antiproliferative activity against four cancer cell lines and one normal human cell line. Among them, derivative 6g with greatest cytotoxicity significantly inhibited t...

journal_title：Bioorganic chemistry

authors： Li Q,Jian XE,Chen ZR,Chen L,Huo XS,Li ZH,You WW,Rao JJ,Zhao PL

更新日期：2020-09-01 00:00:00

abstract：:It has been found that alpha-effects in nucleophilic reactions, unexpectedly large nucleophilicity due to adjacent unpaired electrons, are strongly dependent on the structure of substrate. The nucleophilic cleavages of 4-nitrobenzoate esters and 4-methylbenzoate esters by HOO- have been systematically investigated in ...

journal_title：Bioorganic chemistry

authors： Nomura Y,Kubozono T,Hidaka M,Horibe M,Mizushima N,Yamamoto N,Takahashi T,Komiyama M

更新日期：2004-02-01 00:00:00

abstract：:A series of new cytisine derivatives with a unique endocyclic scaffold were synthesized and evaluated for their inhibitory effect on collagen α1 (I) (COL1A1) promotor in human LX2 cells, taking cytisine as the lead. Structure-activity relationship (SAR) revealed that introducing a 12N-benzyl substitution might signifi...

journal_title：Bioorganic chemistry

authors： Tang S,Li Y,Bao Y,Dai Z,Niu T,Wang K,He H,Song D

更新日期：2019-09-01 00:00:00

abstract：:Urease is an important enzyme which breaks urea into ammonia and carbon dioxide during metabolic processes. However, an elevated activity of urease causes various complications of clinical importance. The inhibition of urease activity with small molecules as inhibitors is an effective strategy for therapeutic interven...

journal_title：Bioorganic chemistry

authors： Hameed A,Khan KM,Zehra ST,Ahmed R,Shafiq Z,Bakht SM,Yaqub M,Hussain M,de la Vega de León A,Furtmann N,Bajorath J,Shad HA,Tahir MN,Iqbal J

更新日期：2015-08-01 00:00:00

abstract：:In search of better α-glucosidase inhibitors, a series of bis-indolylmethane sulfonohydrazides derivatives (1-14) were synthesized and evaluated for their α-glucosidase inhibitory potential. All derivatives exhibited outstanding α-glucosidase inhibition with IC50 values ranging between 0.10 ± 0.05 to 5.1 ± 0.05 μM whe...

journal_title：Bioorganic chemistry

authors： Gollapalli M,Taha M,Ullah H,Nawaz M,AlMuqarrabun LMR,Rahim F,Qureshi F,Mosaddik A,Ahmat N,Khan KM

更新日期：2018-10-01 00:00:00

abstract：:Five previously undescribed 4,5-seco-abietane rearrange diterpenoids (1-5, Prionidipene A-E) were isolated from the aerial parts of Salvia prionitis, along with thirteen known seco-abietane diterpenoids (6-18). The structures of 1-5 were elucidated mainly based on analysis of NMR and MS data. The absolute configuratio...

journal_title：Bioorganic chemistry

authors： Li L,Zhou M,Xue G,Wang W,Zhou X,Wang X,Kong L,Luo J

更新日期：2018-12-01 00:00:00

abstract：:YNT-185 is the first known small molecule acting as orexin 2 receptor (OX2R) agonist with implication to narcolepsy treatment, served as a template scaffold in generating a small set of seven compounds with predictive affinity to OX2R. The design of the new small molecules was driven mostly by improving physicochemica...

journal_title：Bioorganic chemistry

authors： Mezeiova E,Janockova J,Konecny J,Kobrlova T,Benkova M,Dolezal R,Prchal L,Karasova-Zdarova J,Soukup O,Korabecny J

更新日期：2020-10-01 00:00:00

abstract：:Three different modified phosphoramidite nucleoside building blocks equipped with additional protected imidazole, masked alcohol and masked carboxylate functionality are synthesized and incorporated into oligonucleotides. Based on the serine-protease active site model, doubly and triply modified duplexes are created a...

journal_title：Bioorganic chemistry

authors： Catry MA,Gheerardijn V,Madder A

更新日期：2010-06-01 00:00:00

abstract：:A series of novel naproxen analogues containing 3-aryl-1,2,4-oxadiazoles moiety (4b-g) and their reaction intermediates aryl carboximidamides moiety (3b-g) was synthesized and evaluated in vitro as dual COXs/15-LOX inhibitors. Compounds 3b-g exhibited superior inhibitory activity than celecoxib as COX-2 inhibitors. Co...

journal_title：Bioorganic chemistry

authors： Youssif BGM,Mohamed MFA,Al-Sanea MM,Moustafa AH,Abdelhamid AA,Gomaa HAM

更新日期：2019-04-01 00:00:00

abstract：:In efforts to develop new antitubercular agents, we report here the synthesis of a series of novel pyrrole hydrazine derivatives. The molecules were evaluated against inhibitors of InhA, which is one of the key enzymes involved in type II fatty acid biosynthetic pathway of the mycobacterial cell wall as well as inhibi...

journal_title：Bioorganic chemistry

authors： Joshi SD,More UA,Dixit SR,Balmi SV,Kulkarni BG,Ullagaddi G,Lherbet C,Aminabhavi TM

更新日期：2017-12-01 00:00:00

abstract：:Tumor hypoxia has been widely explored over the years as a diagnostic and therapeutic marker. Herein, we designed, optimized and synthesized a new multifunctional bioreductive linker (12) containing an alkynyl group (potential click chemistry fragment); the linker is based on 2-nitroimidazole which was expected to sim...

journal_title：Bioorganic chemistry

authors： Huang Y,Jin C,Yu J,Wang L,Lu W

更新日期：2020-08-01 00:00:00

abstract：:Six amino acid derived N-glycoconjugates of d-glucose were synthesized, characterized and tested for antibacterial activity against G(+)ve (Bacillus cereus) as well as G(-)ve (Escherichia coli and Klebsiella pneumoniae) bacterial strains. All the tested compounds exhibited moderate to good antibacterial activity again...

journal_title：Bioorganic chemistry

authors： Baig N,Singh RP,Chander S,Jha PN,Murugesan S,Sah AK

更新日期：2015-12-01 00:00:00

abstract：:In order to develop multitarget-directed ligands as potential treatments for Alzheimer's disease, twenty-eight new tacrine-hydroxamate derivatives were designed, synthesized, and biologically evaluated. As expected, most of the compounds exhibited inhibitory activities against cholinesterases (ChEs) and histone deacet...

journal_title：Bioorganic chemistry

authors： Xu A,He F,Zhang X,Li X,Ran Y,Wei C,James Chou C,Zhang R,Wu J

更新日期：2020-05-01 00:00:00

abstract：:The coenzyme function of ubiquinone was subject of extensive studies in mitochondria since more than 40 years. The catalytic activity of ubiquinone (UQ) in electron transfer and proton translocation in cooperation with mitochondrial dehydrogenases and cytochromes contributes essentially to the bioenergetic activity of...

journal_title：Bioorganic chemistry

authors： Nohl H,Kozlov AV,Staniek K,Gille L

更新日期：2001-02-01 00:00:00

abstract：:Vernicia montana Lour. (tung tree) is an oil-producing plant with multiple uses, especially with its great potential in biodiesel production, which was a small Asian tree of the spurge family (Euphorbiaceae) with big economic values. However, studies on small molecular compositions of V. montana are limited. As a resu...

journal_title：Bioorganic chemistry

authors： Zhou D,Li Y,Chen G,Yang Y,Mi Y,Lin B,Li W,Hou Y,Li N

更新日期：2020-04-01 00:00:00

abstract：:Ring-C of oleanolic acid was chemically modified by treating with NBS under a variety of experimental conditions. The structures of the synthesized compounds were established by spectral analysis ((1)H &(13)C NMR and Mass). All the compounds were evaluated against a panel of five human cancer cell lines by using MTT a...

journal_title：Bioorganic chemistry

authors： Pattnaik B,Lakshma Nayak V,Ramakrishna S,Venkata Mallavadhani U

更新日期：2016-10-01 00:00:00

abstract：:Inhibition of carbonic anhydrases (CAs, EC 4.2.1.1) has clinical importance for the treatment of several diseases. They participate in crucial regulatory mechanisms for balancing intracellular and extracellular pH of the cells. Among CA isoforms, selective inhibition of hCA IX has been linked to decreasing of cell gro...

journal_title：Bioorganic chemistry

authors： Yamali C,Gul HI,Ece A,Bua S,Angeli A,Sakagami H,Sahin E,Supuran CT

更新日期：2019-11-01 00:00:00

abstract：:Mitomycin C (MC), an anti-cancer drug, and its analog, decarbamoylmitomycin C (DMC), are DNA-alkylating agents. MC is currently used in the clinics and its cytotoxicity is mainly due to its ability to form Interstrand Crosslinks (ICLs) which impede DNA replication and, thereby, block cancer cells proliferation. Howeve...

journal_title：Bioorganic chemistry

authors： Zheng M,Hwang S,Snyder T,Aquilina J,Proni G,Paz MM,Pradhan P,Cheng SY,Champeil E

更新日期：2019-11-01 00:00:00

abstract：:A novel 1(2), 2(18)-diseco indole diterpenoid, drechmerin H (1), was isolated from the fermentation broth of Drechmeria sp. together with a new indole diterpenoid, 2'-epi terpendole A (3), and a known analogue, terpendole A (2). Their structures were determined by HRESIMS, 1D and 2D NMR, ECD, and X-ray single crystal ...

journal_title：Bioorganic chemistry

authors： Zhao JC,Luan ZL,Liang JH,Cheng ZB,Sun CP,Wang YL,Zhang MY,Zhang TY,Wang Y,Yang TM,Wu YY,Zhang YX,Zhao XY,Ma XC

更新日期：2018-09-01 00:00:00

abstract：:Lysine specific demethylase 1 (LSD1) is a flavin-dependent amine oxidase that selectively removes one or two methyl groups from H3 at Lys4 and is recognized as a promising therapeutic target for cancer and other diseases. Here, a series of 3-oxoamino-benzenesulfonamides were synthesized and evaluated for their inhibit...

journal_title：Bioorganic chemistry

authors： Xi J,Xu S,Wu L,Ma T,Liu R,Liu YC,Deng D,Gu Y,Zhou J,Lan F,Zha X

更新日期：2017-06-01 00:00:00

abstract：:The ability to custom-make fluorescent sensors for different analytes could have a tremendous impact in a variety of areas. Template-directed polymerization or molecular imprinting seems to be a promising approach for the preparation of high-affinity and specific binding sites for different template molecules. However...

journal_title：Bioorganic chemistry

authors： Gao S,Wang W,Wang B

更新日期：2001-10-01 00:00:00

abstract：:This paper describes a facile protocol, efficient, and environmentally benign for the synthesis a series of barbiturate acid substituted at C5 position 3a-o. The desired compounds subjected in vitro for different set of bioassays including against anti-oxidant (DPPH and super oxide scavenger assays), anti-cancer, α-gl...

journal_title：Bioorganic chemistry

authors： Barakat A,Islam MS,Al-Majid AM,Ghabbour HA,Yousuf S,Ashraf M,Shaikh NN,Iqbal Choudhary M,Khalil R,Ul-Haq Z

更新日期：2016-10-01 00:00:00

abstract：:Though the delivery of siRNA into cells, tissues or organs remains to be a big obstacle for its applications, recently siRNA therapeutics has developed rapidly and already there are clinical trials ongoing or planned. Some non-viral vectors have attracted much more attention and shown the great potential for combating...

journal_title：Bioorganic chemistry

authors： Zhang S,Zhao Y,Zhi D,Zhang S

更新日期：2012-02-01 00:00:00

abstract：:A series of new N-acyl 8,9-dihydro-4-methoxy-7H-2-benzo[de]quinolinalkanamines have been prepared and tested for their ability to activate pigment granule aggregation in Xenopus laevis melanophores and bind to the recombinant human MT(1) and MT(2) melatonin receptor subtypes expressed in NIH 3T3 cells. Compounds with ...

journal_title：Bioorganic chemistry

authors： Tsotinis A,Eleutheriades A,Hough KA,Davidson K,Sugden D

更新日期：2007-04-01 00:00:00

abstract：:With the aim of finding new anti-inflammatory drugs, a series of new Glycyrrhetinic acid derivatives (1-34) have been designed and synthesized by structural modification, and their anti-inflammatory activities in vitro have been evaluated. The anti-inflammatory activities assay demonstrated that compound 5b suppressed...

journal_title：Bioorganic chemistry

authors： Bian M,Zhen D,Shen QK,Du HH,Ma QQ,Quan ZS

更新日期：2020-12-29 00:00:00

abstract：:Inhibition of α-glucosidase is one of the important approaches in designing antidiabetic drugs for its role in decrease of the carbohydrates digestion to avoid post-prandial increase in blood sugar levels in diabetic patients. In the present study we designed a novel series of 2-acetylbenzofuran hydrazones (L1-L7) and...

journal_title：Bioorganic chemistry

authors： Khan S,Tariq M,Ashraf M,Abdullah S,Al-Rashida M,Khalid M,Taslimi P,Fatima M,Zafar R,Shafiq Z

更新日期：2020-09-01 00:00:00

abstract：:Carbamyl is considered a privileged structure in medicinal chemistry. It has a wide range of biological activities such as antimicrobial, anticancer, anti-epilepsy, for which the best evidence is a number of marketed carbamyl-containing drugs. Carbamyl is formed of primary amine and carbonyl moieties that act as hydro...

journal_title：Bioorganic chemistry

authors： Wang K,Zhu H,Zhao H,Zhang K,Tian Y

更新日期：2020-05-01 00:00:00

abstract：:The capping efficiency of glycine on cavitand-based synthetic four-helix bundles was investigated. Glycine, a common C-capping amino acid, has always been included as a C-terminal residue in our de novo peptides, although the exact contribution of the glyince cap to the overall stability and structure of the caviteins...

journal_title：Bioorganic chemistry

authors： Huttunen-Hennelly HE

更新日期：2010-06-01 00:00:00

abstract：:The antimycobacterial investigation of azepanobetulin and its amide derivative was performed. Both compounds showed increased in vitro antibacterial activity on the H37Rv MTB strain in aerobic and anaerobic conditions. Basing on differences between MIC and IC50 values a predominant bactericidal effect for amide in con...

journal_title：Bioorganic chemistry

authors： Kazakova O,Lopatina T,Giniyatullina G,Mioc M,Soica C

更新日期：2020-11-01 00:00:00