Further insights on the structural aspects of PLA(2) inhibition by gamma-hydroxybutenolide-containing natural products: a comparative study on petrosaspongiolides M-R.

abstract：:RNA stem-loop microhelices with helix sequences based on tRNA acceptor stems can be charged with specific amino acids. Experiments were designed to test the possibility that microhelices could laterally associate through complementary loop sequences and thereby bring their attached aminoacyl groups close enough togeth...

journal_title：Bioorganic & medicinal chemistry

authors： Henderson BS,Schimmel P

更新日期：1997-06-01 00:00:00

abstract：:The molecular design and chemical synthesis of novel enediyne molecules related to the neocarzinostatin chromophore (1), and their chemical and DNA cleaving properties are described. The 10-membered enediyne triols 16-18 were effectively synthesized from xylitol (10) in a short step, and found to be quite stable when ...

journal_title：Bioorganic & medicinal chemistry

authors： Toshima K,Ohta K,Kano T,Nakamura T,Nakata M,Kinoshita M,Matsumura S

更新日期：1996-01-01 00:00:00

abstract：:A series of fifteen N4-benzyl substituted 5-nitroisatin-3-thiosemicarbazones 5a-o was synthesized and evaluated for urease inhibitory, phytotoxic and cytotoxic influences. All the compounds proved to be highly potent inhibitors of the enzyme, showing inhibitory activity (IC50=0.87±0.25-8.09±0.23μM) much better than th...

journal_title：Bioorganic & medicinal chemistry

authors： Pervez H,Khan N,Zaib S,Yaqub M,Naseer MM,Tahir MN,Iqbal J

更新日期：2017-02-01 00:00:00

abstract：:Sustained activation of the Janus kinase-signal transducers and activators of transcription (JAK-STAT) pathway contributed to the progression of cancer and liver diseases. STAT3 signaling inhibitor has been extensively investigated for pharmacological use. We synthesized a series of andrographolide derivatives, and ch...

journal_title：Bioorganic & medicinal chemistry

authors： Chen SR,Li F,Ding MY,Wang D,Zhao Q,Wang Y,Zhou GC,Wang Y

更新日期：2018-10-01 00:00:00

abstract：:Novel benzimidazole derivatives were synthesized and their pharmacological activities were examined. These compounds showed a good suppressive action on histamine release from rat peritoneal mast cells produced by antigen-antibody reaction, an antagonistic action on guinea pig ileum contraction caused by histamine, an...

journal_title：Bioorganic & medicinal chemistry

authors： Nakano H,Inoue T,Kawasaki N,Miyataka H,Matsumoto H,Taguchi T,Inagaki N,Nagai H,Satoh T

更新日期：2000-02-01 00:00:00

abstract：:We have recently reported that a series of (E)-8-styrylcaffeines and (E)-2-styrylbenzimidazoles are moderate to very potent competitive inhibitors of monoamine oxidase B (MAO-B). The most potent member of the series was found to be (E)-8-(3-chlorostyryl)caffeine (CSC) with an enzyme-inhibitor dissociation constant (K(...

journal_title：Bioorganic & medicinal chemistry

authors： van den Berg D,Zoellner KR,Ogunrombi MO,Malan SF,Terre'Blanche G,Castagnoli N Jr,Bergh JJ,Petzer JP

更新日期：2007-06-01 00:00:00

abstract：:Biological assay guided fractionation of a dichloromethane extract of Synaptolepis kirkii led to the isolation of four new and five known daphnane-type diterpene orthoesters, whose structure was established by spectroscopic data. Full spectroscopic data of the new and known natural products are reported here for the f...

journal_title：Bioorganic & medicinal chemistry

authors： He W,Cik M,Van Puyvelde L,Van Dun J,Appendino G,Lesage A,Van der Lindin I,Leysen JE,Wouters W,Mathenge SG,Mudida FP,De Kimpe N

更新日期：2002-10-01 00:00:00

abstract：:Novel reversed isoniazid (RINH) agents were synthesized by covalently linking isoniazid with various efflux pump inhibitor (EPI) cores and their structural motifs. These RINH agents were then evaluated for anti-mycobacterial activity against sensitive, isoniazid mono-resistant and MDR clinical isolates of M. tuberculo...

journal_title：Bioorganic & medicinal chemistry

authors： Kumar M,Singh K,Ngwane AH,Hamzabegovic F,Abate G,Baker B,Wiid I,Hoft DF,Ruminski P,Chibale K

更新日期：2018-02-15 00:00:00

abstract：:There is strong evidence to indicate that a positively charged nitrogen of endogenous and exogenous opioid ligands forms a salt bridge with the Asp residue in the third transmembrane helix of opioid receptors. To further examine the role of this electrostatic interaction in opioid receptor binding and activation, we s...

journal_title：Bioorganic & medicinal chemistry

authors： Weltrowska G,Lemieux C,Chung NN,Guo JJ,Wilkes BC,Schiller PW

更新日期：2014-09-01 00:00:00

abstract：:A series of new scopoletin derivatives were designed and synthesized. Their anti-proliferative effect was initially evaluated against various human cancer cell lines. Among the tested compounds, A1, A2, and D6 showed significant anti-proliferative activities. Angiogenesis was detected by endothelial cell migration ass...

journal_title：Bioorganic & medicinal chemistry

authors： Cai X,Yang J,Zhou J,Lu W,Hu C,Gu Z,Huo J,Wang X,Cao P

更新日期：2013-01-01 00:00:00

abstract：:Use of herbal plant remedies to treat infectious diseases is a common practice in many countries in traditional and alternative medicine. However to date there are only few antimicrobial agents derived from botanics. Based on microbiological screening tests of crude plant extracts we identified four compounds derived ...

journal_title：Bioorganic & medicinal chemistry

authors： Artini M,Papa R,Barbato G,Scoarughi GL,Cellini A,Morazzoni P,Bombardelli E,Selan L

更新日期：2012-01-15 00:00:00

abstract：:A number of isosteres (oxadiazoles, thiadiazoles, tetrazoles and diazines) of benzocaine were prepared and evaluated for their capacity to induce methemoglobinemia-with a view to their possible application as humane pest control agents. It was found that an optimal lipophilicity for the formation of methemoglobin (met...

journal_title：Bioorganic & medicinal chemistry

authors： Conole D,Beck TM,Jay-Smith M,Tingle MD,Eason CT,Brimble MA,Rennison D

更新日期：2014-04-01 00:00:00

abstract：:Allergic diseases are hypersensitivity disorders associated with the production of specific immunoglobulin E (IgE) to environmental allergens. Interleukin (IL)-4, produced primarily by CD4(+) T cells, is an important stimulus for the switch of the antibody isotype to IgE in both mice and humans. In this study we inves...

journal_title：Bioorganic & medicinal chemistry

authors： Park J,Li Q,Chang YT,Kim TS

更新日期：2005-04-01 00:00:00

abstract：:Acute myeloid leukemia (AML) is characterized by fast progression and low survival rates, in which Fms-like tyrosine kinase 3 (FLT3) receptor mutations have been identified as a driver mutation in cancer progression in a subgroup of AML patients. Clinical trials have shown emergence of drug resistant mutants, emphasiz...

journal_title：Bioorganic & medicinal chemistry

authors： Grimm SH,Gagestein B,Keijzer JF,Liu N,Wijdeven RH,Lenselink EB,Tuin AW,van den Nieuwendijk AMCH,van Westen GJP,van Boeckel CAA,Overkleeft HS,Neefjes J,van der Stelt M

更新日期：2019-03-01 00:00:00

abstract：:Based on 2-(4-phenoxybenzoyl)-5-hydroxyindole (2), a novel structural class of CaMKII inhibitors were synthesized and further optimized. The strong acidity of the hydroxyl group and the lipophilic group at the 4 and 6-positions were found to be necessary for strong CaMKII inhibition. Compound 25 was identified as a pr...

journal_title：Bioorganic & medicinal chemistry

authors： Komiya M,Asano S,Koike N,Koga E,Igarashi J,Nakatani S,Isobe Y

更新日期：2012-12-01 00:00:00

abstract：:The design, synthesis, and evaluation of a series of novel inhibitors of aspartate transcarbamoylase (ATCase) are reported. Several submicromolar phosphorus-containing inhibitors are described, but all-carboxylate compounds are inactive. Compounds were synthesized to probe the postulated cyclic transition-state of the...

journal_title：Bioorganic & medicinal chemistry

authors： Coudray L,Pennebaker AF,Montchamp JL

更新日期：2009-11-15 00:00:00

abstract：:A series of novel twenty-eight rigid 2-phenyl- or hydroxylated 2-phenyl-4-aryl-5H-indeno[1,2-b]pyridines were synthesized and evaluated for their topoisomerase inhibitory activity as well as their cytotoxicity against several human cancer cell lines. Generally, hydroxylated compounds (16-18, 22-25, and 29-31) containi...

journal_title：Bioorganic & medicinal chemistry

authors： Kadayat TM,Song C,Shin S,Magar TB,Bist G,Shrestha A,Thapa P,Na Y,Kwon Y,Lee ES

更新日期：2015-07-01 00:00:00

abstract：:The preparation of novel 5-aryl-2-thio-1,3,4-oxadiazoles 4a-41 and the computer-aided study of their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) are reported. The average accuracy of the electronic-topological method and neural network methods applied to the activity predict...

journal_title：Bioorganic & medicinal chemistry

authors： Macaev F,Rusu G,Pogrebnoi S,Gudima A,Stingaci E,Vlad L,Shvets N,Kandemirli F,Dimoglo A,Reynolds R

更新日期：2005-08-15 00:00:00

abstract：:In the amyloid cascade hypothesis, β-amyloid (Aβ) plaques is one of the major pathological biomarkers in the Alzheimer's disease (AD) brain. We report the synthesis and evaluation of novel radiofluorinated chalcones, [18F]4-dimethylamino-4'-fluoro-chalcone ([18F]DMFC) and [18F]4'-fluoro-4-methylamino-chalcone ([18F]FM...

journal_title：Bioorganic & medicinal chemistry

authors： Kaide S,Ono M,Watanabe H,Shimizu Y,Nakamoto Y,Togashi K,Yamaguchi A,Hanaoka H,Saji H

更新日期：2018-07-23 00:00:00

abstract：:Aminoglycoside antibiotics have recently emerged as an intriguing family of RNA binding molecules and they became leading structures for the design of novel RNA ligands. The demystification of the aminoglycoside-RNA recognition phenomenon is required for the development of superior binders. To explore the existence of...

journal_title：Bioorganic & medicinal chemistry

authors： Michael K,Wang H,Tor Y

更新日期：1999-07-01 00:00:00

abstract：:Matrix metalloproteinases are implicated in a wide range of pathophysiological processes and potent selective inhibitors for these enzymes continue to be eagerly sought. 5,5-Disubstituted barbiturates hold promise as inhibitor types being stable in vivo and relatively selective for the gelatinases (MMP-2 and MMP-9). I...

journal_title：Bioorganic & medicinal chemistry

authors： Wang J,Medina C,Radomski MW,Gilmer JF

更新日期：2011-08-15 00:00:00

abstract：:The synthesis of novel melatonin analogues 3a and 4a-c designed as melatonin receptor ligands is described. Among the newly synthesized ligands, 2-((S)-2-hydroxymethylindolin-1-ylmethyl)-melatonin 4b displayed the highest affinity for MT(1) receptors (K(i)=9.8 nM) and for MT(2) subtype (K(i)=7.8 nM), whereas the rigid...

journal_title：Bioorganic & medicinal chemistry

authors： Attia MI,Witt-Enderby PA,Julius J

更新日期：2008-08-15 00:00:00

abstract：:A series of 33 quinoline derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H(37)Rv using the Alamar Blue susceptibility test and the activity expressed as the minimum inhibitory concentration (MIC) in microg/mL. Compounds 5e and 5f exhibited a ...

journal_title：Bioorganic & medicinal chemistry

authors： de Souza MV,Pais KC,Kaiser CR,Peralta MA,de L Ferreira M,Lourenço MC

更新日期：2009-02-15 00:00:00

abstract：:Concise total syntheses of (R)- and (S)-argentilactone have been developed via enantioselective catalytic allylation (ECA) and ring-closing metathesis pathways (four steps, 39% overall yield and 82-84% ee) from 2-octynal and their in vitro activity against cancer cells is described. ...

journal_title：Bioorganic & medicinal chemistry

authors： de Fatima A,Kohn LK,Antônio MA,de Carvalho JE,Pilli RA

更新日期：2004-10-15 00:00:00

abstract：:The proteasome, a validated cellular target for cancer, is central for maintaining cellular homeostasis, while fatty acid synthase (FAS), a novel target for numerous cancers, is responsible for palmitic acid biosynthesis. Perturbation of either enzymatic machine results in decreased proliferation and ultimately cellul...

journal_title：Bioorganic & medicinal chemistry

authors： Zhu M,Harshbarger WD,Robles O,Krysiak J,Hull KG,Cho SW,Richardson RD,Yang Y,Garcia A,Spiegelman L,Ramirez B,Wilson CT,Yau JA,Moore JT,Walker CB,Sacchettini JC,Liu WR,Sieber SA,Smith JW,Romo D

更新日期：2017-06-01 00:00:00

abstract：:The most common lysosomal storage disorder, Gaucher disease, is caused by inefficient folding and trafficking of certain variants of lysosomal beta-glucosidase (beta-Glu, also known as beta-glucocerebrosidase). Recently, Sawker et al. reported that the addition of subinhibitory concentrations (10 microM) of the pharma...

journal_title：Bioorganic & medicinal chemistry

authors： Yu L,Ikeda K,Kato A,Adachi I,Godin G,Compain P,Martin O,Asano N

更新日期：2006-12-01 00:00:00

abstract：:New compounds able to counteract staphylococcal biofilm formation are needed. In this study we investigate the mechanism of action of pyrrolomycins, whose potential as antimicrobial agents has been demonstrated. We performed a new efficient and easy method to use microwave organic synthesis suitable for obtaining pyrr...

journal_title：Bioorganic & medicinal chemistry

authors： Raimondi MV,Listro R,Cusimano MG,La Franca M,Faddetta T,Gallo G,Schillaci D,Collina S,Leonchiks A,Barone G

更新日期：2019-03-01 00:00:00

abstract：:Compounds from a wide variety of structural classes inhibit HIV-1 integrase. However, a single unified understanding of the relationship between the structures and activities of these compounds still eludes researchers. We report herein the development of QSAR models for integrase inhibition. The genetic function appr...

journal_title：Bioorganic & medicinal chemistry

authors： Yuan H,Parrill AL

更新日期：2002-12-01 00:00:00

abstract：:Because the activation of matrix metalloproteinases (MMP) is a key factor in the metastatic process, compounds with the ability to inhibit MMP activity have a potential in the treatment of tumor. From the examination of 2000 plant extracts, obovatal isolated from the extract of the leaves of Magnolia obovata THUNB was...

journal_title：Bioorganic & medicinal chemistry

authors： Lee SK,Chun HK,Yang JY,Han DC,Son KH,Kwon BM

更新日期：2007-06-15 00:00:00

abstract：:Analogs of the antibiotic fosmidomycin, an inhibitor of the methylerythritol phosphate pathway to isoprenoids, were synthesized and evaluated against the recombinant Synechocystis sp. PCC6803 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR). Fosfoxacin, the phosphate analog of fosmidomycin, and its acetyl congene...

journal_title：Bioorganic & medicinal chemistry

authors： Woo YH,Fernandes RP,Proteau PJ

更新日期：2006-04-01 00:00:00