Design, synthesis and bioactivities of Celecoxib analogues or derivatives.

abstract：:A novel series of substituted imidazol-5-ones were designed, synthesized and evaluated for in vitro reverse transcriptase (RT) inhibition activity using reverse transcriptase assay kit (Roche, Colorimetric). It has been observed from in vitro screening that newly synthesized compounds possess RT inhibitory activity. D...

journal_title：Bioorganic & medicinal chemistry

authors： Mokale SN,Lokwani D,Shinde DB

更新日期：2012-05-01 00:00:00

abstract：:The effects of Brazilian green propolis ethanol extract on Cry j1-induced cys-leukotrienes and histamine release from peripheral leukocytes of patients with allergic rhinitis were investigated. One of the key mechanisms for the anti-allergic properties of the extract was revealed to be the suppression of cys-LTs relea...

journal_title：Bioorganic & medicinal chemistry

authors： Tani H,Hasumi K,Tatefuji T,Hashimoto K,Koshino H,Takahashi S

更新日期：2010-01-01 00:00:00

abstract：:To characterize the structure-activity relationship between alpha 1-adrenergic receptors and the family of imidazoline/guanidinium receptive sites (IGRS), we synthesized and characterized a series of analogues of cirazoline, an imidazoline with high affinity for alpha 1-adrenergic receptors and IGRS. Analysis of poten...

journal_title：Bioorganic & medicinal chemistry

authors： Brasili L,Pigini M,Marucci G,Quaglia W,Malmusi L,Lanier SM,Lanier B

更新日期：1995-11-01 00:00:00

abstract：:12-O-β-D-glucopyranosyl jasmonic acid (JAG) shows unique biological activities, including leaf-closing of Samanea saman. It is expected that the mode of action for such regulation is distinct from that of other jasmonates. We developed high-performance compact molecular probes (CMPs) based on JAG that can be used for ...

journal_title：Bioorganic & medicinal chemistry

authors： Ueda M,Yang G,Ishimaru Y,Itabashi T,Tamura S,Kiyota H,Kuwahara S,Inomata S,Shoji M,Sugai T

更新日期：2012-10-01 00:00:00

abstract：:Valinol is part of numerous pharmaceuticals and has various other important applications. Optically pure valinol (ee >99%) was prepared employing different ω-transaminases from the corresponding prochiral hydroxy ketone. By the choice of the enzyme the (R)- as well as the (S)-enantiomer were accessible. Reductive amin...

journal_title：Bioorganic & medicinal chemistry

authors： Fuchs CS,Simon RC,Riethorst W,Zepeck F,Kroutil W

更新日期：2014-10-15 00:00:00

abstract：:Competitive antagonists (CAs) of ionotropic GABA receptors (GABARs) reportedly exhibit insecticidal activity and have potential for development as novel insecticides for overcoming emerging resistance to traditional GABAR-targeting insecticides. Our previous studies demonstrated that 4,5-disubstituted 3-isoxazolols or...

journal_title：Bioorganic & medicinal chemistry

authors： Liu G,Li H,Shi J,Wang W,Furuta K,Liu D,Zhao C,Ozoe F,Ju X,Ozoe Y

更新日期：2019-01-15 00:00:00

abstract：:The toxicity of the molecules currently used in the treatment of human cytomegalovirus (HCMV) in immunocompromised hosts often causes interruption of the therapy. Cyclodextrins (Cds), oligosaccharides possessing a hydrophobic cavity, have the property of forming inclusion complexes with a great number of molecules, im...

journal_title：Bioorganic & medicinal chemistry

authors： Nicolazzi C,Abdou S,Collomb J,Marsura A,Finance C

更新日期：2001-02-01 00:00:00

abstract：:A new series of selective PDE4D inhibitors has been designed and synthesized by replacing 3-methoxy group with 3-difluoromethoxy isoster moiety in our previously reported cathecolic structures. All compounds showed a good PDE4D3 inhibitory activity, most of them being inactive toward other PDE4 isoforms (PDE4A4, PDE4B...

journal_title：Bioorganic & medicinal chemistry

authors： Brullo C,Massa M,Villa C,Ricciarelli R,Rivera D,Pronzato MA,Fedele E,Barocelli E,Bertoni S,Flammini L,Bruno O

更新日期：2015-07-01 00:00:00

abstract：:In previous studies, the polycyclic cage amine 8-benzylamino-8,11-oxapentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecane (NGP1-01) and a number of its derivatives showed positive effects in neuroprotection studies with MPTP, in vivo. In view of these findings, we examined these compounds for their effects on [(3)H]dopamin...

journal_title：Bioorganic & medicinal chemistry

authors： Geldenhuys WJ,Malan SF,Murugesan T,Van der Schyf CJ,Bloomquist JR

更新日期：2004-04-01 00:00:00

abstract：:Reverse chemical proteomics using T7 phage display is a powerful technique for identifying cellular receptors of biologically active small molecules. However, to date this method has generally been limited to cDNA libraries constructed from mRNA isolated from eukaryotes. In this paper, we describe the construction of ...

journal_title：Bioorganic & medicinal chemistry

authors： Piggott AM,Kriegel AM,Willows RD,Karuso P

更新日期：2009-10-01 00:00:00

abstract：:Breast cancer resistance protein (BCRP/ABCG2) belongs to the ATP binding cassette family of transport proteins. BCRP has been found to confer multidrug resistance in cancer cells. A strategy to overcome resistance due to BCRP overexpression is the investigation of potent and specific BCRP inhibitors. The aim of the cu...

journal_title：Bioorganic & medicinal chemistry

authors： Juvale K,Pape VF,Wiese M

更新日期：2012-01-01 00:00:00

abstract：:Various 4-analogues of podophyllotoxin and epipodophyllotoxin were obtained via the formation of the corresponding 4-keto derivatives. Methyloximation of podophyllotoxone, followed by subsequent catalytic hydrogenation, gave stereoselective access to 4-alpha-amino-4-deoxypodophyllotoxin and from there, to the correspo...

journal_title：Bioorganic & medicinal chemistry

authors： Roulland E,Magiatis P,Arimondo P,Bertounesque E,Monneret C

更新日期：2002-11-01 00:00:00

abstract：:Tuberculosis is today amongst the worldwide health threats. As resistant strains of Mycobacterium tuberculosis have slowly emerged, treatment failure is too often a fact, especially in countries lacking the necessary health care organisation to provide the long and costly treatment adapted to patients. Because of lack...

journal_title：Bioorganic & medicinal chemistry

authors： Janin YL

更新日期：2007-04-01 00:00:00

abstract：:Fibrosarcoma is one of the fatal cancer types and there is still not satisfactory success in its treatment despite new drugs. Therefore, the search for a new compound has been going on. It is currently known that some palladium-based anti-cancer compounds seem to have powerful apoptosis-inducing effects in cancer cell...

journal_title：Bioorganic & medicinal chemistry

authors： Coskun MD,Ari F,Oral AY,Sarimahmut M,Kutlu HM,Yilmaz VT,Ulukaya E

更新日期：2013-08-01 00:00:00

abstract：:Glucuronide derivatives of CBI-bearing CC-1065 analogues have been synthesized, and their cytotoxicities tested against U937 leukemia cells. The new compounds show potent antitumor activity in vitro. Compounds 1 and 2, and their corresponding glucuronides 3 and 4 have IC(50) values of 0.6, 0.1, 1.4 and 0.6 nM, respect...

journal_title：Bioorganic & medicinal chemistry

authors： Wang Y,Yuan H,Wright SC,Wang H,Larrick JW

更新日期：2003-04-03 00:00:00

abstract：:The AP sites are representative of DNA damage and known as an intermediate in the base excision repair (BER) pathway which is involved in the repair of damaged nucleobases by reactive oxygen species, UVA irradiation, and DNA alkylating agents. Therefore, it is expected that the inhibition or modulation of the AP site ...

journal_title：Bioorganic & medicinal chemistry

authors： Abe YS,Sasaki S

更新日期：2019-12-15 00:00:00

abstract：:5-Lipoxygenase (5-LO) and microsomal prostaglandin E₂ synthase (mPGES)-1 are key enzymes in the biosynthesis of leukotrienes and prostaglandin (PG)E₂, respectively, and are considered as valuable targets for the treatment of inflammatory diseases. Here, we present the identification of 2-mercaptohexanoic acid derivati...

journal_title：Bioorganic & medicinal chemistry

authors： Greiner C,Zettl H,Koeberle A,Pergola C,Northoff H,Schubert-Zsilavecz M,Werz O

更新日期：2011-06-01 00:00:00

abstract：:Three peptide amides, HPRK(Py)(4)HPRK-NH(2) (PyH-12), HPRK(Py)(3)HPRK-NH(2) (PyH-11) and HPRK(Py)(2)HPRK-NH(2) (PyH-10), incorporating two HPRK motifs and various 4-amino-1-methylpyrrole-2-carboxylic acid residues (Py) were synthesized by solid-phase peptide methodology. The binding of these three peptides to a 5'-32P...

journal_title：Bioorganic & medicinal chemistry

authors： Chang JC,Yang CH,Chou PY,Yang WH,Chou IC,Lu CT,Lin PH,Hou RC,Jeng KC,Cheng CC,Sheh L

更新日期：2004-01-02 00:00:00

abstract：:The irreversible inhibition of histidine ammonia lyase by L-cysteine and dioxygen has been reexamined. After denaturation and consecutive digestion of the inhibited enzyme by trypsin and endoproteinase Glu-C, the generated chromophoric system (lambda max = 340 nm) remained intact and was isolated in an octapeptide con...

journal_title：Bioorganic & medicinal chemistry

authors： Weber K,Rétey J

更新日期：1996-07-01 00:00:00

abstract：:A series of new isoxazolyl, triazolyl and phenyl based 3-thiophen-2-yl-quinoline derivatives were synthesized adopting click chemistry approach. In addition, the synthesis of new useful synthon, (2-chloroquinolin-3-yl) (thiophen-2-yl) methanol, is reported. The obtained compounds were characterized by spectral data an...

journal_title：Bioorganic & medicinal chemistry

authors： Othman DIA,Selim KB,El-Sayed MA,Tantawy AS,Amen Y,Shimizu K,Okauchi T,Kitamura M

更新日期：2019-10-01 00:00:00

abstract：:Pyridine-based compounds have been playing a crucial role as agrochemicals or pesticides including fungicides, insecticides/acaricides and herbicides, etc. Since most of the agrochemicals listed in the Pesticide Manual were discovered through screening programs that relied on trial-and-error testing and new agrochemic...

journal_title：Bioorganic & medicinal chemistry

authors： Guan AY,Liu CL,Sun XF,Xie Y,Wang MA

更新日期：2016-02-01 00:00:00

abstract：:The syntheses of new nitroimidazole compounds using silicon-[(18)F]fluorine chemistry for the potential detection of tumor hypoxia are described. [(18)F]silicon-based compounds were synthesized by coupling 2-nitroimidazole with silyldinaphtyl or silylphenyldi-tert-butyl groups and labeled by fluorolysis or isotopic ex...

journal_title：Bioorganic & medicinal chemistry

authors： Joyard Y,Azzouz R,Bischoff L,Papamicaël C,Labar D,Bol A,Bol V,Vera P,Grégoire V,Levacher V,Bohn P

更新日期：2013-07-01 00:00:00

abstract：:1α,25-Dihydroxyvitamin D3 exerts its actions by binding to vitamin D receptor (VDR). We are continuing the study related to the alteration of pocket structure of VDR by 22-alkyl substituent of ligands and the relationships between the alteration and agonistic/antagonistic activity. Previously we reported that compound...

journal_title：Bioorganic & medicinal chemistry

authors： Anami Y,Sakamaki Y,Itoh T,Inaba Y,Nakabayashi M,Ikura T,Ito N,Yamamoto K

更新日期：2015-11-15 00:00:00

abstract：:Synthesized series of cage dimeric 1,4-dihydropyridines have been systematically evaluated as MDR modulators in in vitro assays to investigate structure-dependent selectivity properties of inhibiting most cancer-relevant efflux pump proteins. Structure-activity relationships of each P-glycoprotein (P-gp) and multidrug...

journal_title：Bioorganic & medicinal chemistry

authors： Coburger C,Wollmann J,Krug M,Baumert C,Seifert M,Molnár J,Lage H,Hilgeroth A

更新日期：2010-07-15 00:00:00

abstract：:In this paper, we report the NMR structural study of two quadruplex structures formed by truncations of the human telomeric sequence and containing a modified base, namely d(AprGGGT) and d(TAprGGGT), where Apr indicates 2'-deoxy-8-(propyn-1-yl)adenosines. Both oligonucleotides have been found to form 4-fold symmetric ...

journal_title：Bioorganic & medicinal chemistry

authors： Esposito V,Randazzo A,Galeone A,Varra M,Mayol L

更新日期：2004-03-01 00:00:00

abstract：:A series of non-covalent piperidine-containing peptidyl derivatives with various substituents at side chains of different residues were designed, synthesized and evaluated as proteasome inhibitors. After proteasome inhibitory evaluations of all the synthesized target compounds, selected ones were tested for their anti...

journal_title：Bioorganic & medicinal chemistry

authors： Zhao Y,Xu L,Zhang J,Zhang M,Lu J,He R,Xi J,Zhuang R,Li J,Zhou Y

更新日期：2021-01-01 00:00:00

abstract：:The prokaryotic ATP-dependent ClpP protease, localized in the relict plastid of malaria parasite, represents a potential drug target. In the present study, we utilized in silico structure-based screening and medicinal chemistry approaches to identify a novel pyrimidine series of compounds inhibiting P. falciparum ClpP...

journal_title：Bioorganic & medicinal chemistry

authors： Mundra S,Thakur V,Bello AM,Rathore S,Asad M,Wei L,Yang J,Chakka SK,Mahesh R,Malhotra P,Mohmmed A,Kotra LP

更新日期：2017-10-15 00:00:00

abstract：:The human skin is constantly exposed to external factors that affect its integrity, UV radiation being one of the main stress factors. The repeated exposure to this radiation leads to increased production of Reactive Oxygen Species (ROS) which activate a series of processes involved in photoaging. Excessive UV exposur...

journal_title：Bioorganic & medicinal chemistry

authors： Rosa GP,Palmeira A,Resende DISP,Almeida IF,Kane-Pagès A,Barreto MC,Sousa E,Pinto MMM

更新日期：2021-01-01 00:00:00

abstract：:Aryl diketoacids (ADK) and their bioisosteres are among the most promising HIV-1 integrase (IN) inhibitors. Previously, we designed a series of ADK dimers as a new class of IN inhibitors that were hypothesized to target two divalent metal ions on the active site of IN. Herein we present a further structure-activity re...

journal_title：Bioorganic & medicinal chemistry

authors： Zeng LF,Jiang XH,Sanchez T,Zhang HS,Dayam R,Neamati N,Long YQ

更新日期：2008-08-15 00:00:00

abstract：:We have recently communicated that DNA oligonucleotide d(G(3)T(4)G(4)) forms a dimeric G-quadruplex in the presence of K(+) ions [J. Am. Chem. Soc.2003, 125, 7866-7871]. The high-resolution NMR structure of d(G(3)T(4)G(4))(2) G-quadruplex exhibits G-quadruplex core consisting of three stacked G-quartets. The two overh...

journal_title：Bioorganic & medicinal chemistry

authors： Sket P,Crnugelj M,Plavec J

更新日期：2004-11-15 00:00:00