当前位置： SCI文献检索 > BIOORGANIC CHEMISTRY期刊下所有文献 > Recent advancement in the discovery and development of COX-2 inhibitors: Insight into biological activities and SAR studies (2008-2019).

Recent advancement in the discovery and development of COX-2 inhibitors: Insight into biological activities and SAR studies (2008-2019).

Abstract：

:Cyclooxygenase-2 is a very important physiological enzyme playing key roles in various biological functions especially in the mechanism of pain and inflammation, among other roles, making it a molecule of high interest to the pharmaceutical community as a target. COX 2 enzyme is induced only during inflammatory processes or cancer and reflects no role in the guarding stomach lining. Thus, selective COX-2 inhibition can significantly reduce the adverse effects including GI tract damage and hepatotoxic effects of traditional NSAIDs like aspirin, ibuprofen, etc. Recent developments on COX-2 inhibitors is primarily focused on improving the selectivity index of the drug towards COX-2 along with enhancing the potency of the drug by modifying the scaffolds of Coxibs currently in the market like Celecoxib, Indomethacin, Oxaprozin, etc. We have reported the progress on new COX-2 inhibitors in the last decade (2008-2019) focussing on five heterocyclic rings- Pyrazole, Indole, Oxazole, Pyridine and Pyrrole. The addition of various moieties to these core rings and their structure-activity relationship along with their molecular modelling data have been explored in the article. This review aims to aid medicinal chemists in the design and discovery of better COX-2 inhibitors constructed on these five heterocyclic pharmacophores.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Sharma V,Bhatia P,Alam O,Javed Naim M,Nawaz F,Ahmad Sheikh A,Jha M

doi

10.1016/j.bioorg.2019.103007

subject

Has Abstract

pub_date

2019-08-01 00:00:00

pages

103007

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)30322-0

journal_volume

89

pub_type

杂志文章,评审

相关文献

BIOORGANIC CHEMISTRY文献大全
  • Suntamide A, a neuroprotective cyclic peptide from Cicadidae Periostracum.

    abstract：:Suntamide A (1), a new cyclic peptide, was isolated from Cicadidae Periostracum. The gross structure of 1 was elucidated by detailed analysis of HRMS and 1D/2D NMR spectra, and the absolute configuration was established by C3 Marfey's method. We extended our study to examine biological activity of 1, and found that 1 ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104493

    authors： Thapa P,Katila N,Choi DY,Choi H,Nam JW

    更新日期：2021-01-01 00:00:00

  • The management of diabetes mellitus-imperative role of natural products against dipeptidyl peptidase-4, α-glucosidase and sodium-dependent glucose co-transporter 2 (SGLT2).

    abstract：:Diabetes mellitus is a chronic metabolic disorder which is rapidly spreading worldwide. It is characterized by persistent elevated blood glucose level above normal values (hyperglycemia) due to defect in either insulin secretion or in insulin action or both of them. Currently approved oral synthetic antidiabetic drugs...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.bioorg.2019.02.009

    authors： Abbas G,Al Harrasi A,Hussain H,Hamaed A,Supuran CT

    更新日期：2019-05-01 00:00:00

  • Synthesis of Mitomycin C and decarbamoylmitomycin C N6 deoxyadenosine-adducts.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103280

    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

  • 8-Chrysoeriol, as a potential BCL-2 inhibitor triggers apoptosis of SW1990 pancreatic cancer cells.

    abstract：:8-Chrysoeriol, a bioactive flavanoid, was firstly identified to bind directly to BCL-2 as BH3 mimetics by structure-based virtual ligand screening. And 3D docking model revealed the molecular basis of 8-Chrysoeriol targeting to BCL-2. The interaction between 8-Chrysoeriol and BCL-2 was further confirmed using Microsca...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.01.042

    authors： Zhang Y,Li Z,Min Q,Palida A,Zhang Y,Tang R,Chen L,Li H

    更新日期：2018-04-01 00:00:00

  • Discovery of a series of selective and cell permeable beta-secretase (BACE1) inhibitors by fragment linking with the assistance of STD-NMR.

    abstract：:Two β-secreatase (BACE1) inhibitors from natural products (cinnamic acid and flavone) were linked to furnish potent, cell permeable BACE1 inhibitors with noncompetitive mode of inhibition, with the assistance of saturated transfer difference (STD)-NMR technique. Some of these conjugates also exhibited selective BACE1 ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103253

    authors： Fang WS,Sun DY,Yang S,Cheng C,Moschke K,Li T,Sun S,Lichtenthaler SF,Huang J,Wang Y

    更新日期：2019-11-01 00:00:00

  • Novel carbazole-stilbene hybrids as multifunctional anti-Alzheimer agents.

    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

    authors： Patel DV,Patel NR,Kanhed AM,Teli DM,Patel KB,Joshi PD,Patel SP,Gandhi PM,Chaudhary BN,Prajapati NK,Patel KV,Yadav MR

    更新日期：2020-08-01 00:00:00

  • Bioactive flavonoid dimers from Chinese dragon's blood, the red resin of Dracaena cochinchinensis.

    abstract：:Seven flavonoid dimers, biflavocochins A-G, together with six known compounds were isolated from the red resins of Dracaena cochinchinensis (Chinese dragon's blood). Their structures were elucidated based on extensive spectroscopic analysis. The absolute configurations of 1-7 was assigned by experimental and quantum c...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.103659

    authors： Lang GZ,Li CJ,Gaohu TY,Li C,Ma J,Yang JZ,Zhou TT,Yuan YH,Ye F,Wei JH,Zhang DM

    更新日期：2020-04-01 00:00:00

  • Structure-activity relationships of rationally designed AMACR 1A inhibitors.

    abstract：:α-Methylacyl-CoA racemase (AMACR; P504S) is a promising novel drug target for prostate and other cancers. Assaying enzyme activity is difficult due to the reversibility of the 'racemisation' reaction and the difficulties in the separation of epimeric products; consequently few inhibitors have been described and no str...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.04.024

    authors： Yevglevskis M,Lee GL,Nathubhai A,Petrova YD,James TD,Threadgill MD,Woodman TJ,Lloyd MD

    更新日期：2018-09-01 00:00:00

  • Synthesis of some N-aroyl-2-oxindole benzenesulfonamide conjugates with carbonic anhydrase inhibitory activity.

    abstract：:Implication of carbonic anhydrases (CAs) in many physiological functions made them attractive therapeutic targets. Herein, we report the synthesis of three series of benzenesulfonamide-based compounds (5a-e, 9a-e and 10a-e) as potential ligands to four of the human CA isoforms (hCA I, hCA II, hCA IX and hCA XII). All ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.103635

    authors： George RF,Bua S,Supuran CT,Awadallah FM

    更新日期：2020-03-01 00:00:00

  • Design, synthesis and pharmacological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.

    abstract：:Two series of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 2,4-imidazolinedione/pyrazolone scaffold were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against HT-29, H460, A549, MKN-45, and U87MG cancer cell lines in vitro. The pharmacological data indicated that mo...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2014.07.011

    authors： Zhou S,Ren J,Liu M,Ren L,Liu Y,Gong P

    更新日期：2014-12-01 00:00:00

  • Building fluorescent sensors for carbohydrates using template-directed polymerizations.

    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

    pub_type： 杂志文章

    doi：10.1006/bioo.2001.1219

    authors： Gao S,Wang W,Wang B

    更新日期：2001-10-01 00:00:00

  • Synthesis and biological evaluation of benzimidazole-oxindole conjugates as microtubule-targeting agents.

    abstract：:A series of benzimidazole-oxindole conjugates were synthesized and evaluated for their cytotoxic activity. The cytotoxicity assay results suggest that conjugates 5c and 5p exhibit promising cytotoxicity against human breast cancer cell line (MCF-7). The Cell cycle analysis revealed that these conjugates induced cell c...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2015.09.003

    authors： Kamal A,Nagaseshadri B,Nayak VL,Srinivasulu V,Sathish M,Kapure JS,Suresh Reddy C

    更新日期：2015-12-01 00:00:00

  • Antimalarial activity of HIV-1 protease inhibitor in chromone series.

    abstract：:Increasing parasite resistance to nearly all available antimalarial drugs becomes a serious problem to human health and necessitates the need to continue the search for new effective drugs. Recent studies have shown that clinically utilized HIV-1 protease (HIV-1 PR) inhibitors can inhibit the in vitro and in vivo grow...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2014.10.006

    authors： Lerdsirisuk P,Maicheen C,Ungwitayatorn J

    更新日期：2014-12-01 00:00:00

  • Non-viral vectors for the mediation of RNAi.

    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

    pub_type： 杂志文章,评审

    doi：10.1016/j.bioorg.2011.07.005

    authors： Zhang S,Zhao Y,Zhi D,Zhang S

    更新日期：2012-02-01 00:00:00

  • The effective molarity (EM) puzzle in proton transfer reactions.

    abstract：:The DFT and HF calculation results for the proton transfer reactions of three different systems reveal that the reaction mechanism (transfer of a proton to a nucleophile) is largely determined by the distance between the two reactive centers (r). Systems with relatively large r values tend to abstract a proton from a ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2009.04.003

    authors： Karaman R

    更新日期：2009-08-01 00:00:00

  • Bioactive constituents from Thunbergia erecta as potential anticholinesterase and anti-ageing agents: Experimental and in silico studies.

    abstract：:Acetylcholinesterase (AChE) inhibitor and telomerase reverse transcriptase (TERT) potentiator phytochemicals are highly targeted as anti-Alzheimerꞌs disease and as an anti-ageing process. A phytochemical study of Thunbergia erecta aerial parts resulted in the isolation of ten compounds (1-10). Their structures were id...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2021.104643

    authors： Refaey MS,Abdelhamid RA,Elimam H,Elshaier YAMM,Ali AA,Orabi MAA

    更新日期：2021-01-11 00:00:00

  • Discovery of novel N-substituted thiazolidinediones (TZDs) as HDAC8 inhibitors: in-silico studies, synthesis, and biological evaluation.

    abstract：:Epigenetics plays a fundamental role in cancer progression, and developing agents that regulate epigenetics is crucial for cancer management. Among Class I and Class II HDACs, HDAC8 is one of the essential epigenetic players in cancer progression. Therefore, we designed, synthesized, purified, and structurally charact...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.103934

    authors： Upadhyay N,Tilekar K,Jänsch N,Schweipert M,Hess JD,Henze Macias L,Mrowka P,Aguilera RJ,Choe JY,Meyer-Almes FJ,Ramaa CS

    更新日期：2020-07-01 00:00:00

  • Synthesis of novel 1,2-bis-quinolinyl-1,4-naphthoquinones: ERK2 inhibition, cytotoxicity and molecular docking studies.

    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

    authors： Aly AA,El-Sheref EM,Bakheet MEM,Mourad MAE,Brown AB,Bräse S,Nieger M,Ibrahim MAA

    更新日期：2018-12-01 00:00:00

  • Steering the antitumor drug discovery campaign towards structurally diverse indolines.

    abstract：:Indoline framework is often perpended as a privileged heterocycle present in medicinally valuable compounds of natural and synthetic origin. This review article presents the rational approaches/strategies employed for the design of anticancer indolines along with the structure activity relationship and mechanistic ins...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.bioorg.2019.103436

    authors： Thakur A,Singh A,Kaur N,Ojha R,Nepali K

    更新日期：2020-01-01 00:00:00

  • Synthesis and evaluation of antioxidant and antiproliferative activity of 2-arylbenzimidazoles.

    abstract：:Three series of arylbenzimidazole derivatives 3-40, 45 have been simply synthesized and tested for their antioxidant capacity. The 2-arylbenzimidazoles were tested against various radicals by the DPPH, FRAP and ORAC tests and showed different activity profiles. It has been observed that the number and position of the ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103396

    authors： Baldisserotto A,Demurtas M,Lampronti I,Tacchini M,Moi D,Balboni G,Pacifico S,Vertuani S,Manfredini S,Onnis V

    更新日期：2020-01-01 00:00:00

  • Quinoxalines as potent selective CRFRs ligands for monitoring and brain diagnostic.

    abstract：:The paper highlighted quinoxalines as potent ligands to corticotropin-releasing factor receptor types 1 and 2. The content includes design and structure-activity relationship of 50 model substances to CRFR1, CRFR2α and CRF2β, respectively. It is important to bear in mind, that our concept has based on challenging rese...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2014.10.008

    authors： Ivanova B,Spiteller M

    更新日期：2015-02-01 00:00:00

  • Caffeine-hydrazones as anticancer agents with pronounced selectivity toward T-lymphoblastic leukaemia cells.

    abstract：:We report design and synthesis of set of novel anticancer agents based on caffeine-hydrazones bearing 2-hydroxyaryl- or 2-N-heteroaryl moiety. Anticancer activity evaluation using seven cancer cell lines and two non-malignant cell lines demonstrated that several derivatives display significant anticancer activity and ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2015.03.003

    authors： Kaplánek R,Jakubek M,Rak J,Kejík Z,Havlík M,Dolenský B,Frydrych I,Hajdúch M,Kolář M,Bogdanová K,Králová J,Džubák P,Král V

    更新日期：2015-06-01 00:00:00

  • Novel 1,2,4-triazole derivatives as apoptotic inducers targeting p53: Synthesis and antiproliferative activity.

    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

    authors： Gomaa HAM,El-Sherief HAM,Hussein S,Gouda AM,Salem OIA,Alharbi KS,Hayallah AM,Youssif BGM

    更新日期：2020-12-01 00:00:00

  • Quinazoline-4(3H)-one derivatives as novel and potent inhibitors of soluble epoxide hydrolase: Design, synthesis and biological evaluation.

    abstract：:Inhibition of soluble epoxide hydrolase (sEH) is considered as a promising target to reduce blood pressure, improve insulin sensitivity, and decrease inflammation. In this study, a series of some novel quinazoline-4(3H)-one derivatives (3a-t) with varying steric and electronic properties was designed, synthesized and ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.103736

    authors： Hejazi L,Rezaee E,Tabatabai SA

    更新日期：2020-06-01 00:00:00

  • A novel bi-functional chalcone inhibits multi-drug resistant Staphylococcus aureus and potentiates the activity of fluoroquinolones.

    abstract：:Staphylococcus aureus is the leading cause of bacteraemia and the dwindling supply of effective antibacterials has exacerbated the problem of managing infections caused by this bacterium. Isoliquiritigenin (ISL) is a plant flavonoid that displays therapeutic potential against S. aureus. The present study identified a ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.10.024

    authors： Gupta VK,Gaur R,Sharma A,Akther J,Saini M,Bhakuni RS,Pathania R

    更新日期：2019-03-01 00:00:00

  • Current development of 5-nitrofuran-2-yl derivatives as antitubercular agents.

    abstract：:Pulmonary tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis (MTB) and still remains one of the foremost fatal infectious diseases, infecting nearly a third of the worldwide population. The emergencies of multidrug-resistant and extensively drug-resistant tuberculosis (MDR and XDR-TB) prom...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.bioorg.2019.102969

    authors： Elsaman T,Mohamed MS,Mohamed MA

    更新日期：2019-07-01 00:00:00

  • Novel pyrimidine-pyridine hybrids: Synthesis, cyclooxygenase inhibition, anti-inflammatory activity and ulcerogenic liability.

    abstract：:Some derivatives containing pyrido[2,3-d:6,5d']dipyrimidine-4,5-diones (9a-f), tetrahydropyrido[2,3-d]pyrimidine-6-carbonitriles (11a-c) and 6-(4-acetylphenyl)-2-thioxo-2,3,5,6,7,8-hexahydro-1H-pyrimido[4,5-d]pyrimidin-4-one (12) were synthesized from 6-amino-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one (8). The anti-infla...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.01.028

    authors： Abdelgawad MA,Bakr RB,Azouz AA

    更新日期：2018-04-01 00:00:00

  • Novel aryl carboximidamide and 3-aryl-1,2,4-oxadiazole analogues of naproxen as dual selective COX-2/15-LOX inhibitors: Design, synthesis and docking studies.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.02.043

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

    更新日期：2019-04-01 00:00:00

  • Discovery of 7H-pyrrolo[2,3-d]pyridine derivatives as potent FAK inhibitors: Design, synthesis, biological evaluation and molecular docking study.

    abstract：:Focal adhesion kinase (FAK) is an intracellular non-receptor tyrosine kinase responsible for development of various tumor types. Aiming to explore new potent inhibitors, two series of 2,4-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives were designed and synthesized on the base of structure-based design strategy....

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104092

    authors： Wang R,Zhao X,Yu S,Chen Y,Cui H,Wu T,Hao C,Zhao D,Cheng M

    更新日期：2020-09-01 00:00:00

  • Chemical characterization of cytotoxic indole acetic acid derivative from mulberry fruit (Morus alba L.) against human cervical cancer.

    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

    authors： Yu JS,Lee D,Lee SR,Lee JW,Choi CI,Jang TS,Kang KS,Kim KH

    更新日期：2018-02-01 00:00:00