Active core structure of terfestatin A, a new specific inhibitor of auxin signaling.

abstract：:5-Bromouracil ((Br)U) was incorporated into three types of synthetic RNA and the products of the photoirradiated (Br)U-containing RNAs were investigated using HPLC and MS analysis. The photoirradiation of r(GCA(Br)UGC)(2) and r(CGAA(Br)UUGC)/r(GCAAUUCG) in A-form RNA produced the corresponding 2'-keto adenosine ((keto...

journal_title：Bioorganic & medicinal chemistry

authors： Morinaga H,Kizaki S,Takenaka T,Kanesato S,Sannohe Y,Tashiro R,Sugiyama H

更新日期：2013-01-15 00:00:00

abstract：:Protein geranylgeranylation reactions are dependent on the availability of geranylgeranyl diphosphate (GGDP), which serves as the isoprenoid donor. Inhibition of GGDP synthase (GGDPS) is of interest from a drug development perspective as GGDPS inhibition results in impaired protein geranylgeranylation, which in multip...

journal_title：Bioorganic & medicinal chemistry

authors： Wills VS,Metzger JI,Allen C,Varney ML,Wiemer DF,Holstein SA

更新日期：2017-04-15 00:00:00

abstract：:A novel series of 6-hydroxy-3-morpholinones, in which the functional aldehyde and the hydroxy group of P(2) site form a cyclic hemiacetal, was identified as calpain inhibitors. The placement of isobutyl group at the 2-position of the 3-morpholinone was the most effective modification for inhibiting micro- and m-calpai...

journal_title：Bioorganic & medicinal chemistry

authors： Nakamura M,Miyashita H,Yamaguchi M,Shirasaki Y,Nakamura Y,Inoue J

更新日期：2003-12-01 00:00:00

abstract：:Glyoxalase I (GLO I) is the rate-limiting enzyme for detoxification of methylglyoxal (MG), a side product of glycolysis, which is able to induce apoptosis. Since GLO I is known to be highly expressed in the most tumor cells and little in normal cells, specific inhibitors of this enzyme have been expected as effective ...

journal_title：Bioorganic & medicinal chemistry

authors： Takasawa R,Takahashi S,Saeki K,Sunaga S,Yoshimori A,Tanuma S

更新日期：2008-04-01 00:00:00

abstract：:Reaction of γ-Boc-GABA, prepared by protecting the γ-amino moiety of the amino butyric acid with the tert-butyloxycarbonyl (Boc) protecting group, with 4-methyl/ethyl benzenesulfonamide, followed by removal of the Boc protecting group in 3 M HCl afforded the corresponding hydrochlorides, which were further derivatized...

journal_title：Bioorganic & medicinal chemistry

authors： Ceruso M,Antel S,Vullo D,Scozzafava A,Supuran CT

更新日期：2014-12-15 00:00:00

abstract：:Many therapeutically-relevant protein-protein interactions (PPIs) have been reported that feature a helix and helix-binding cleft at the interface. Given this, different approaches to disrupting such PPIs have been developed. While short peptides (<15 amino acids) typically do not fold into a stable helix, researchers...

journal_title：Bioorganic & medicinal chemistry

authors： Tennyson RL,Walker SN,Ikeda T,Harris RS,McNaughton BR

更新日期：2018-03-15 00:00:00

abstract：:Our present report deals with the preparation of hitherto unreported 7-([carbonyl-14C]-acetyl)paclitaxel 4 and two new bioactive 7-substituted fluorescent taxoids (FITC 9 and rhodamine 11), as well as evaluation towards their applications as biological probes. The results in this report demonstrate that (a) the new pa...

journal_title：Bioorganic & medicinal chemistry

authors： Rao CS,Chu JJ,Liu RS,Lai YK

更新日期：1998-11-01 00:00:00

abstract：:The design, synthesis, and biological evaluation of new phosphodiesterase type 4 inhibitors, which possess new templates instead of a cyclohexane ring, are described. The mode of interaction with the enzyme is discussed based on the structure-activity relationship (SAR) data obtained for the synthesized inhibitors. Fu...

journal_title：Bioorganic & medicinal chemistry

authors： Ochiai H,Odagaki Y,Ohtani T,Ishida A,Kusumi K,Kishikawa K,Yamamoto S,Takeda H,Obata T,Kobayashi K,Nakai H,Toda M

更新日期：2004-10-01 00:00:00

abstract：:An analogue 2 of coenzyme A (CoA) has been prepared in which the geminal methyl groups are replaced with hydrogens. An NMR titration study was conducted and shifts in frequency of protons in the pantetheine portion of the molecule upon titration of the adenine base were observed as has been previously reported with Co...

journal_title：Bioorganic & medicinal chemistry

authors： Vogel KW,Stark LM,Mishra PK,Yang W,Drueckhammer DG

更新日期：2000-10-01 00:00:00

abstract：:To elucidate the receptor-bound conformation of glucagon-like peptide-1 (GLP-1), a series of conformationally constrained GLP-1 analogues were synthesized by introducing lactam bridges between Lys(i) and Glu(i)(+4) to form alpha-helices at various positions. The activity and affinity of these analogues to GLP-1 recept...

journal_title：Bioorganic & medicinal chemistry

authors： Murage EN,Schroeder JC,Beinborn M,Ahn JM

更新日期：2008-12-01 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：:Cancer is a major cause of death, and the development of new anticancer drugs is urgently needed. Invasion and metastasis are the primary causes of death due to cancer rather than growth of the primary tumor. In the current study, we examined the anti-invasive effects of p-dodecylaminophenol (1), which was developed b...

journal_title：Bioorganic & medicinal chemistry

authors： Takahashi N,Takeda K,Imai M

更新日期：2013-10-01 00:00:00

abstract：:The 3-D QSAR analysis with new imidazo- and pyrrolo-quinolinedione derivatives was conducted by Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices Analysis (CoMSIA). When crossvalidation value (q(2)) is 0.844 at four components, the Pearson correlation coefficient (r(2)) of the C...

journal_title：Bioorganic & medicinal chemistry

authors： Suh ME,Kang MJ,Park SY

更新日期：2001-11-01 00:00:00

abstract：:The purpose of this study was to synthesize two new positron emission tomography (PET) probes, N-(4-(2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl)phenyl)-9,10-dihydro-5-[¹⁸F]fluoroethoxy-9-oxo-4-acridine carboxamide ([¹⁸F]3) and quinoline-3-carboxylic acid [2-(4-{2-[7-(2-[¹⁸F]fluoroethoxy)-6-methoxy-3,4-d...

journal_title：Bioorganic & medicinal chemistry

authors： Kawamura K,Yamasaki T,Konno F,Yui J,Hatori A,Yanamoto K,Wakizaka H,Ogawa M,Yoshida Y,Nengaki N,Fukumura T,Zhang MR

更新日期：2011-01-15 00:00:00

abstract：:We have previously reported the discovery and initial SAR of the [1,7]naphthyridine-3-carbonitriles and quinoline-3-carbonitriles as Tumor Progression Loci-2 (Tpl2) kinase inhibitors. In this paper, we report new SAR efforts which have led to the identification of 4-alkylamino-[1,7]naphthyridine-3-carbonitriles. These...

journal_title：Bioorganic & medicinal chemistry

authors： Kaila N,Green N,Li HQ,Hu Y,Janz K,Gavrin LK,Thomason J,Tam S,Powell D,Cuozzo J,Hall JP,Telliez JB,Hsu S,Nickerson-Nutter C,Wang Q,Lin LL

更新日期：2007-10-01 00:00:00

abstract：:The β-lactam antibiotic resistance of Gram-negative bacteria has shown to be a critical global health problem. One of the primary reasons for the drug resistance is the existence of β-lactamases especially metallo-β-lactamases such as New Delhi metallo-β-lactamase (NDM-1) and Verona Integron-encoded metallo-β-lactamas...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang J,Wang S,Wei Q,Guo Q,Bai Y,Yang S,Song F,Zhang L,Lei X

更新日期：2017-10-01 00:00:00

abstract：:Here we describe the design, synthesis, and pharmacological evaluation of a set of compounds structurally related to the high affinity serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide (6, LP-211). Specific structural modifications were performed in order to maintain affini...

journal_title：Bioorganic & medicinal chemistry

authors： Lacivita E,Niso M,Hansen HD,Di Pilato P,Herth MM,Lehel S,Ettrup A,Montenegro L,Perrone R,Berardi F,Colabufo NA,Leopoldo M,Knudsen GM

更新日期：2014-03-01 00:00:00

abstract：:As part of a continuing effort aimed at the development of selective, efficacious, and centrally active m1 muscarinic agonists for the treatment of Alzheimer's disease, a series of amide and hydrazide amidine derivatives (2a-e and 3b-d) was synthesized and examined for muscarinic agonist activity. Preliminary biochemi...

journal_title：Bioorganic & medicinal chemistry

authors： Ojo B,Dunbar PG,Durant GJ,Nagy PI,Huzl JJ 3rd,Periyasamy S,Ngur DO,el-Assadi AA,Hoss WP,Messer WS Jr

更新日期：1996-10-01 00:00:00

abstract：:The beta-amino acid, (S)-ethyl-3-amino-4-pentynoate, is a chiral synthon used in the synthesis of xemilofiban hydrochloride, an anti-platelet agent. A biocatalytic approach was developed to resolve (R)- and (S)-enantiomers of ethyl 3-amino-4-pentynoate in enantiomerically pure form employing the enzyme Penicillin acyl...

journal_title：Bioorganic & medicinal chemistry

authors： Topgi RS,Ng JS,Landis B,Wang P,Behling JR

更新日期：1999-10-01 00:00:00

abstract：:A tetracyclic, conformationally constrained analogue of delta8-THC (2) has been synthesized in which a two carbon bridge exists between C2 and C2'. Two conceptually related syntheses of 2 are described, both of which employ 5,7-dimethoxy-4-oxo-1,2,3,4-tetrahydronaphthoic acid (11) as starting material. This substrate ...

journal_title：Bioorganic & medicinal chemistry

authors： Huffman JW,Yu S

更新日期：1998-12-01 00:00:00

abstract：:Seven new triterpenoid saponins (1-7), have been isolated and elucidated from the roots of Gypsophila oldhamiana together with five known triterpenoid saponins (8-12). These saponins which could be classified into three series: 3-O-monoglucosides (1, 8, 9), 28-O-monoglucosides (2-4, 12) and 3, 28-O-bidesmosides (5-7, ...

journal_title：Bioorganic & medicinal chemistry

authors： Luo JG,Ma L,Kong LY

更新日期：2008-03-15 00:00:00

abstract：:Peptide-semicarbazones derived from Z-Trp-Trp-Phe-aldehyde inhibit the chymotryptic activity of the human proteasome at nanomolar concentrations, but are less active in a NFkappaB reporter gene assay. Cyclic semicarbazones, in contrast, combine a strong inhibitory effect on the enzyme with an inhibition of NFkappaB si...

journal_title：Bioorganic & medicinal chemistry

authors： Leban J,Blisse M,Krauss B,Rath S,Baumgartner R,Seifert MH

更新日期：2008-04-15 00:00:00

abstract：:Cannabinoid receptors have been studied extensively in view of their potential functional role in several physiological and pathological processes. For this reason, the search for new potent, selective ligands for subtype CB receptors, CB(1) and CB(2), is still of great importance, in order to investigate their role i...

journal_title：Bioorganic & medicinal chemistry

authors： Ferrarini PL,Calderone V,Cavallini T,Manera C,Saccomanni G,Pani L,Ruiu S,Gessa GL

更新日期：2004-04-15 00:00:00

abstract：:Sphingolipids are ubiquitous and abundant components of all eukaryotic and some prokaryotic organisms. Sphingolipids show a large structural variety not only between the different species, but also within an individual cell. This variety is not limited to alterations in the polar headgroups of e.g. glycosphingolipids,...

journal_title：Bioorganic & medicinal chemistry

authors： Saied EM,Le TL,Hornemann T,Arenz C

更新日期：2018-08-07 00:00:00

abstract：:Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring. Of the four oxadiazoles known, 1,3,4-oxadiazole has become an important structural motif for the development of new drugs and the compounds containing 1,3,4-oxadiazole cores have a broad spectrum of biologic...

journal_title：Bioorganic & medicinal chemistry

authors： Pidugu VR,Yarla NS,Pedada SR,Kalle AM,Satya AK

更新日期：2016-11-01 00:00:00

abstract：:High specificity has been an important feature in affinity labeling for target profiling. Especially, to label targets via rapidly progressing reactions with consumption of ligand (probe), high specificity of reaction with common functional groups of target protein should be achieved without reactions with similar gro...

journal_title：Bioorganic & medicinal chemistry

authors： Tomohiro T,Nakabayashi M,Sugita Y,Morimoto S

更新日期：2016-08-01 00:00:00

abstract：:A series of novel sulfonamides incorporating phenylacrylamido functionalities were synthesized and investigated for the inhibition of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). The physiologically and pharmacologically relevant human (h) isoforms hCA I and II (cytosolic isozymes), as well as the transmembr...

journal_title：Bioorganic & medicinal chemistry

authors： Angapelly S,Ramya PVS,Angeli A,Del Prete S,Capasso C,Arifuddin M,Supuran CT

更新日期：2017-10-15 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：:Parkinson's disease (PD) is a common chronic degenerative disease of the central nervous system. Due to a rapidly aging society worldwide, PD morbidity is on the rise; however, the treatment of PD with conventional drugs carries serious adverse reactions and cannot fix the root cause of PD, the degeneration of dopamin...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang H,Tong R,Bai L,Shi J,Ouyang L

更新日期：2016-04-01 00:00:00

abstract：:High-throughput screening of a small-molecule library identified a 5-triazolo-2-arylpyridazinone as a novel inhibitor of the important glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). Such inhibitors are of interest due to PFKFB3's control of the important glycolytic pathway used by cancer cel...

journal_title：Bioorganic & medicinal chemistry

authors： Brooke DG,van Dam EM,Watts CK,Khoury A,Dziadek MA,Brooks H,Graham LJ,Flanagan JU,Denny WA

更新日期：2014-02-01 00:00:00