Abstract：
:Five new maleimide derivatives, (+)- and (-)- farinomalein F (1), (+)- and (-)- farinomalein G (2), farinomalein H (3) and one new linearly fused prenylated indole alkaloid phomoamide (8), along with five known compounds 4-7 and 9 were isolated from the mangrove endophytic fungus Phomopsis sp. SYSUQYP-23. Their structures and absolute configurations were determined by HRESIMS, spectroscopic and electronic circular dichroism (ECD) calculations. Bioassay results showed that compounds 3-9 exhibited significant inhibitory activities against nitric oxide (NO) production in lipopolysaccharides (LPS) induced RAW 264.7 cells, with IC50 values ranging from 4.5 to 25 μM. Moreover, the molecular docking study implied the probable binding interaction of compounds 4 and 5 with nitric oxide synthase.
journal_name
Bioorg Chemjournal_title
Bioorganic chemistryauthors
Chen Y,Zhang L,Zou G,Li C,Yang W,Liu H,She Zdoi
10.1016/j.bioorg.2020.103712subject
Has Abstractpub_date
2020-04-01 00:00:00pages
103712eissn
0045-2068issn
1090-2120pii
S0045-2068(20)30077-8journal_volume
97pub_type
杂志文章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
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103222
更新日期：2019-11-01 00:00:00
abstract：:Acute lymphoblastic leukemia (ALL) or white blood cell cancer is one of the major causes that kills many children worldwide. Although various therapeutic agents are available for ALL treatment, the new drug discovery and drug delivery system are needed to improve their effectiveness, to reduce the toxicity and side-ef...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104601
更新日期：2021-01-01 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
pub_type： 杂志文章
doi：10.1016/j.bioorg.2017.09.008
更新日期：2017-12-01 00:00:00
abstract：:One new eudesmane sesquiterpenoid, 11β-hydroxy-13-chloro-eudesm-5-en-12, 8-olide (1), was isolated from the roots of Inula helenium together with nine eudesmanolides (2-10) and one germacranolide (11). Their structures were elucidated on the basis of detailed spectroscopic analyses. All isolates were evaluated for the...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.01.055
更新日期：2019-05-01 00:00:00
abstract：:Lambertellin (1) and ergosta-5,7,22-trien-3-ol (2) were isolated from the solid rice fermentation of the plant pathogenic fungus Pycnoporus sanguineus MUCL 51321. Their structures were elucidated using comprehensive spectroscopic methods. The isolated compounds were tested on lipopolysaccharide (LPS)-stimulated RAW 26...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.06.021
更新日期：2018-10-01 00:00:00
abstract：:Molecules capable of engaging with multiple targets associated with pathological condition of Alzheimer's disease have proved to be potential anti-Alzheimer's agents. In our goal to develop multitarget-directed ligands for the treatment of Alzheimer's disease, a novel series of carbazole-based stilbene derivatives wer...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.103977
更新日期：2020-08-01 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
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104209
更新日期：2020-11-01 00:00:00
abstract：:In the present work, a novel series of B-RAF kinase inhibitors having imidazo[2,1-b]oxazole scaffold was designed and synthesized based on the structures of the well-known B-RAF inhibitors. The twenty two final compounds were tested over A375 and SKMEL28 cell lines to determine the primary cytotoxic activity of these ...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103349
更新日期：2019-12-01 00:00:00
abstract：:Two novel series of N-2,3-bis(6-substituted-4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)naphthalene-1,4-diones 3a-d and substituted N-(methyl/ethyl)bisquinolinone triethyl-ammonium salts 4e,f were successfully synthesized. The synthesized compounds were targeted as new candidates to extracellular signal-regulated kinases...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.09.017
更新日期：2018-12-01 00:00:00
abstract：:The stereoselective synthesis and anti- Hymenolepis nana activity of six Linezolid-type compounds, obtained by chemical modification of l-Alanine, are reported in this work. The synthetic strategy was to prepare diasteromeric N,N-dibenzylamino oxazolidinones 1 and 2, and coupling with 4-(4-bromophenyl)morpholine (3) t...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104359
更新日期：2020-12-01 00:00:00
abstract：:A series of novel thiazolo[3,2-b][1,2,4]-triazoles 3a-n has been synthesized and evaluated in vitro as potential antiproliferative. Compounds 3b-d exhibited significant antiproliferative activity. Compound 3b was the most potent with Mean GI50 1.37 µM comparing to doxorubicin (GI50 1.13 µM). The transcription effects ...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104369
更新日期：2020-12-01 00:00:00
abstract：:This article describes discovery of a novel and new class of cholinesterase inhibitors as potential therapeutics for Alzheimer's disease. A series of novel isoalloxazine derivatives were synthesized and biologically evaluated for their potential inhibitory outcome for both acetylcholinesterase (AChE) and butyrylcholin...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2015.05.005
更新日期：2015-08-01 00:00:00
abstract：:P-glycoprotein (P-gp) is one of the cell membrane pumps which mediate the efflux of molecules such as anticancer drugs to the extracellular matrix of tumor cells. P_gp is a member of the ATP-binding cassette (ABC) transporter family that is implicated in cancer multidrug resistance (MDR). Since MDR is a contributor to...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103156
更新日期：2019-10-01 00:00:00
abstract：:Several new 5,6-dihydropyrimidine-2(1H)-thione derivatives have been prepared and investigated for their potencies for anticonvulsant activity against maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) test in mice. The acute neurotoxicity was measured by rotarod test. Compounds 3c and 3l were foun...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2017.07.017
更新日期：2017-10-01 00:00:00
abstract：:Advanced glycation end products (AGEs) are implicated to be the key players in most of the diabetic complications. The AGE's interfere with the proteins heterogeneously, thereby rendering denaturation and the consequent loss of function and accumulation. Thus, a novel natural product inspired indeno[2,1-c]pyridinone (...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104375
更新日期：2020-12-01 00:00:00
abstract：:Alkyl ester prodrugs are well known to be bioconverted by carboxylesterases, particularly in rodents' by first-pass metabolism in the systemic circulation and liver. However, the bioconversion of structurally more complex esters with polar functional groups is less well understood, especially in humans. Therefore, it ...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.09.018
更新日期：2018-12-01 00:00:00
abstract：:Colchicine site antimitotic agents typically suffer from low aqueous solubilities and are formulated as phosphate prodrugs of phenolic groups. These hydroxyl groups are the aim of metabolic transformations leading to resistance. There is an urgent need for more intrinsically soluble analogues lacking these hydroxyl gr...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.103755
更新日期：2020-05-01 00:00:00
abstract：:In the present study, we have reported synthesis and biological evaluation of a series of fifteen 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole derivatives against both promastigotes and amastigotes of Leishmania parasites responsible for visceral (L. donovani) and cutaneous (L. amazonensis) leishmaniasis. Among these repo...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2016.11.013
更新日期：2017-02-01 00:00:00
abstract：:Glycyrrhetinic acid has been usually studied for their anti-tumor activities. However, the low bioavailability and poor aqueous solubility as well as limited intracellular accumulation have limited their utility. In this present study, a series of new glycyrrhetinic acid conjugates with a triphenylphosphonium cation (...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.12.036
更新日期：2019-04-01 00:00:00
abstract：:Synthesis of C-5-substituted 1,3-dioxoisoindoline-4-aminoquinolines having amide group as a spacer was developed with an intent to evaluate their antiplasmodial activities. The synthesized dioxoisoindoline-aminoquinolines tethered with β-alanine as a spacer and secondary amine as substituent displayed good anti-plasmo...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.04.006
更新日期：2019-07-01 00:00:00
abstract：:The structurally related tetrapyrrolic pigments are a group of natural products that participate in many of the fundamental biosynthetic and catabolic processes of living organisms. Hydroxymethylbilane synthase catalyzes a rate-limiting step for the biosyntheses of tetrapyrrolic natural products. We carried out extens...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2008.07.001
更新日期：2008-10-01 00:00:00
abstract：:A new series of 2-(4-aminobenzosulfonyl)-5H-benzo[b]carbazole-6,11-dione derivatives, which has not been reported yet, has been synthesized from 1,4-naphthoquinone and 4-aminophenylsulfone involving an Michael addition, benzoylation and Pd catalyzed coupling. This set of compounds has been evaluated for in vitro cytot...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2014.01.002
更新日期：2014-04-01 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
pub_type： 杂志文章
doi：10.1016/j.bioorg.2015.10.002
更新日期：2015-12-01 00:00:00
abstract：:Activated carbon's porous structure allows it to adsorb a substrates, products and catalysts from the environment thus modificated the biocatalysis processes in digestive tract. Active carbons are currently used to remove solvents from gas streams and for water purification; however, few studies have examined the mech...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.02.029
更新日期：2019-12-01 00:00:00
abstract：:The fruit of the white mulberry tree (Morus alba L.) is a multiple fruit with a sweet flavor commonly consumed around the world. Chemical investigation of the fruits led to the isolation of two indole acetic acid derivatives (1 -2) including a new compound, which turned out to be an isolation artifact, 3S-(β-D-glucopy...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2017.10.015
更新日期：2018-02-01 00:00:00
abstract：:Three new compounds, including a prenylated tryptophan derivative, luteoride E (1), a butenolide derivative, versicolactone G (2), and a linear aliphatic alcohol, (3E,7E)-4,8-dimethyl-undecane-3,7-diene-1,11-diol (3), together with nine known compounds (4-12), were isolated and identified from a coral-associated fungu...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.06.029
更新日期：2018-10-01 00:00:00
abstract：:In previous work, the target of asperphenamate as a natural product was successfully determined as cathepsin by the natural product consensus pharmacophore strategy. In order to develop accurate SAR (structure-activity relationship) of asperphenamate-type cathepsin inhibitor, we chose several novel analogs with hetero...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103417
更新日期：2020-01-01 00:00:00
abstract：:The synthesis of the unsaturated 4,6-dideoxy-3-fluoro-2-keto-beta-d-glucopyranosyl nucleosides of 5-fluorouracil (6a), N(6)-benzoyl adenine (6b), uracil (6c), thymine (6d) and N(4)-benzoyl cytosine (6e), is described. Monoiodination of compounds 1a,b, followed by acetylation, catalytic hydrogenation and finally regios...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2009.11.001
更新日期：2010-04-01 00:00:00
abstract：:Euphoroids A-C (1-3), three new ent-abietane-type diterpenoids, together with ten known analogues (4-13) were obtained from the roots of Euphorbia ebracteolata. The structures of these compounds were determined by extensive spectroscopic data analysis, including UV, HRESIMS, 1D-, and 2D-NMR data. The inhibitory effect...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.07.032
更新日期：2018-12-01 00:00:00
abstract：:Convenient structures such as 2,4-diketo esters have been widely used as an effective pattern in medicinal chemistry and pharmacology for drug discovery. 2,4-Diketonate is a common scaffold that can be found in many biologically active and naturally occurring compounds. Also, many 2,4-diketo ester derivatives have bee...
journal_title：Bioorganic chemistry
pub_type： 杂志文章,评审
doi：10.1016/j.bioorg.2020.104343
更新日期：2020-12-01 00:00:00
