A facile route to paclitaxel C-10 carbamates.

abstract：:A nucleopeptide was prepared in a convergent manner via segmental coupling of the protected biopolymers in solution. The resulting nucleopeptide (4b, 72%) containing the binding site of lambda repressor and a peptide containing the consensus sequence of the DNA binding helix of the helix turn-helix-proteins was obtain...

journal_title：Bioorganic & medicinal chemistry letters

authors： McMinn DL,Greenberg MM

更新日期：1999-02-22 00:00:00

abstract：:QSAR models represent the relationship of biological activity with either physicochemical parameters or structural indices. QSAR study was performed on some arylpiperazines as 5-HT(1A)/alpha(1)-adrenergic receptor antagonists using E-state indices to identify the pharmacophoric requirements. It was found that some of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Debnath B,Samanta S,Naskar SK,Roy K,Jha T

更新日期：2003-09-01 00:00:00

abstract：:In the course of screening for a novel anticancer drug candidate, we previously isolated HY251 with the molecular structure of 3-propyl-2-vinyl-1,2,3,3a,3b,6,7,7a,8,8a-decahydrocyclopenta[a]indene-3,3a,7a,8a-tetraol from the roots of Aralia continentalis. The current study was designed to evaluate the detailed mechani...

journal_title：Bioorganic & medicinal chemistry letters

authors： Oh HL,Lee CH

更新日期：2011-03-01 00:00:00

abstract：:A series of pyrrolo[3,2,1-ij]quinoline derivatives was synthesized, evaluated for their activity against the 5-HT2c and 5-HT2a, receptors and found to be agonists at 5-HT2c with selectivity over 5-HT2a. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Isaac M,Slassi A,O'Brien A,Edwards L,MacLean N,Bueschkens D,Lee DK,McCallum K,De Lannoy I,Demchyshyn L,Kamboj R

更新日期：2000-05-01 00:00:00

abstract：:The synthesis of a series of new antitumour agents, the benzothiazole substituted quinol ethers and esters, is reported via the hypervalent iodine mediated oxidation of hydroxylated 2-phenylbenzothiazoles. The products were found to be active in vitro against human colon and breast cancer cell lines with IC50 values i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wells G,Bradshaw TD,Diana P,Seaton A,Shi DF,Westwell AD,Stevens MF

更新日期：2000-03-06 00:00:00

abstract：:In the present study we report the synthesis of halogen-substituted phenanthrene β-diketo acids as new HIV-1 integrase inhibitors. The target phenanthrenes were obtained using both standard thermal- and microwave-assisted synthesis. 4-(6-Chlorophenanthren-2-yl)-2,4-dioxobutanoic acid (18) was the most active compound ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sharma H,Sanchez TW,Neamati N,Detorio M,Schinazi RF,Cheng X,Buolamwini JK

更新日期：2013-11-15 00:00:00

abstract：:The stereoselective synthesis and biological activity of NPS 1407 (4a), (S)-(-)-3-amino-1,1-bis(3-fluorophenyl)butane, a potent, stereoselective antagonist of the NMDA receptor, are described. The racemate (4) was found to be active at the NMDA receptor in an in vitro assay, prompting the synthesis of the individual s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Moe ST,Smith DL,DelMar EG,Shimizu SM,Van Wagenen BC,Balandrin MF,Chien YE,Raszkiewicz JL,Artman LD,White HS,Mueller AL

更新日期：2000-11-06 00:00:00

abstract：:The B(6) vitamers have been shown to display beneficial therapeutic effects in cardiovascular related disorders. The design of novel antiplatelet agents using pyridoxine as a template has led to the discovery of a class of novel cardio- and cerebro-protective agents. The present study describes the synthesis of severa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang W,Yao J,Pham V,Whitney T,Froese D,Friesen A,Stang L,Xu C,Shuaib A,Diakur JM,Haque W

更新日期：2004-09-20 00:00:00

abstract：:The design and synthesis of a series of C28 amine-based betulinic acid derivatives as HIV-1 maturation inhibitors is described. This series represents a continuation of efforts following on from previous studies of C-3 benzoic acid-substituted betulinic acid derivatives as HIV-1 maturation inhibitors (MIs) that were e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen Y,Sit SY,Chen J,Swidorski JJ,Liu Z,Sin N,Venables BL,Parker DD,Nowicka-Sans B,Lin Z,Li Z,Terry BJ,Protack T,Rahematpura S,Hanumegowda U,Jenkins S,Krystal M,Dicker ID,Meanwell NA,Regueiro-Ren A

更新日期：2018-05-15 00:00:00

abstract：:A series of chiral heterocyclic aminopyrrolidine derivatives was synthesized as novel melatoninergic ligands. Binding affinity assays were performed on cloned human MT(1) and MT(2) receptors, stably expressed in NIH3T3 cells. Compound 16 was identified as an orally bioavailable agonist at MT(1) and MT(2) melatonin rec...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sun LQ,Chen J,Mattson RJ,Epperson JR,Deskus JA,Li WS,Takaki K,Hodges DB,Iben L,Mahle CD,Ortiz A,Molstad D,Ryan E,Yeleswaram K,Xu C,Luo G

更新日期：2003-12-15 00:00:00

abstract：:Chaetocin (1), a structurally complex epidithiodiketopiperazine (ETP) alkaloid produced by Chaetomium minutum, is a potent inhibitor of protein lysine methyltransferase G9a, which plays important roles in many biological processes. Here we present our synthetic investigations to identify a simple prototype G9a inhibit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujishiro S,Dodo K,Iwasa E,Teng Y,Sohtome Y,Hamashima Y,Ito A,Yoshida M,Sodeoka M

更新日期：2013-02-01 00:00:00

abstract：:Homology modeling of candida lanosterol C-14 demethylase, synthesis and in vitro antifungal activities of cyclohexyl analogs of restricticin are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tsukuda T,Shiratori Y,Watanabe M,Ontsuka H,Hattori K,Shirai M,Shimma N

更新日期：1998-07-21 00:00:00

abstract：:Selective σ2 ligands continue to be an active target for medications to attenuate the effects of psychostimulants. In the course of our studies to determine the optimal substituents in the σ2-selective phenyl piperazines analogues with reduced activity at other neurotransmitter systems, we discovered that 1-(3-chlorop...

journal_title：Bioorganic & medicinal chemistry letters

authors： Motel WC,Healy JR,Viard E,Pouw B,Martin K,Matsumoto RR,Coop A

更新日期：2013-12-15 00:00:00

abstract：:The inhibition of tyrosinase is an established strategy for treating hyperpigmentation. Our previous findings demonstrated that cinnamic acid and benzoic acid scaffolds can be effective tyrosinase inhibitors with low toxicity. The hydroxyl substituted benzoic and cinnamic acid moieties of these precursors were incorpo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nazir Y,Saeed A,Rafiq M,Afzal S,Ali A,Latif M,Zuegg J,Hussein WM,Fercher C,Barnard RT,Cooper MA,Blaskovich MAT,Ashraf Z,Ziora ZM

更新日期：2020-01-01 00:00:00

abstract：:A series of novel curcumin bisacetamides aiming of enriching their biological activities have been synthesized. The synthesized compounds were screened for their in vitro antioxidant, anti-inflammatory and cytotoxic activities. All the compounds exhibited potent to good anti-inflammatory, antioxidant and noteworthy cy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sribalan R,Kirubavathi M,Banuppriya G,Padmini V

更新日期：2015-10-01 00:00:00

abstract：:In the past few years a significant effort has been devoted by Pharmacia toward the discovery of novel antibiotics. We have recently described the identification of an anthranilic acid lead 1 and the optimization resulting in the advanced lead 2. In this report, we describe the preparation of several selected analogs ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thorarensen A,Li J,Wakefield BD,Romero DL,Marotti KR,Sweeney MT,Zurenko GE,Sarver RW

更新日期：2007-06-01 00:00:00

abstract：:A series of canthin-6-one analogues were designed and synthesized in order to study their antibacterial activity and structure-activity relationships. Compound 22 showed a broad spectrum of antibacterial activity and exhibited better bactericidal effect (8-fold superiority against Staphylococcus aureus and 2-fold supe...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dai J,Dan W,Zhang Y,He M,Wang J

更新日期：2018-10-01 00:00:00

abstract：:The expression of epidermal growth factor receptor (EGFR) across a wide range of tumor cells has attracted attention for use as a tumor marker in drug delivery systems. Therefore, binding molecules with the ability to target EGFR have been developed. Among them, we focused on affibodies that are binding proteins deriv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nishimura Y,Ezawa R,Ishii J,Ogino C,Kondo A

更新日期：2017-01-15 00:00:00

abstract：:The 1,2,3-triazole ring fused with pyridine/pyrimidine was explored as new template for the identification of potential antimicrobial agents. The regioselective synthesis of these pre-designed N-heteroarenes was achieved via exploring the application of Buchwald's strategy (i.e. C-N bond formation/reduction/diazotizat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Marepu N,Yeturu S,Pal M

更新日期：2018-11-01 00:00:00

abstract：:A series of alpha(v)beta(3) antagonists based on a thiophene scaffold were synthesized via two routes and evaluated for in vitro biological activity. We have identified several structurally similar antagonists with different selectivities towards alpha(IIb)beta(3), alpha(v)beta(5) and alpha(5)beta(1) at the cellular l...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bubenik M,Meerovitch K,Bergeron F,Attardo G,Chan L

更新日期：2003-02-10 00:00:00

abstract：:In plant biology, calcium ions are involved in a variety of intriguing biological phenomena as a secondary messenger. However, most conventional calcium indicators are not applicable for plant cells because of the difficulty with their localization control in plant cells. We here introduce a method to monitor spatiote...

journal_title：Bioorganic & medicinal chemistry letters

authors： Takaoka Y,Shigenaga M,Imai M,Nukadzuka Y,Ishimaru Y,Saito K,Yokoyama R,Nishitani K,Ueda M

更新日期：2016-01-01 00:00:00

abstract：:In search for a new antibacterial agent with improved antimicrobial spectrum and potency, we designed and synthesized a series of novel 3-((Z)-2-(4-nitrophenyl)-2-(1H-tetrazol-5-yl) vinyl)-4H-chromen-4-ones 7a-h by convergent synthesis approach. All the synthesized compounds were assayed for their in-vitro antibacteri...

journal_title：Bioorganic & medicinal chemistry letters

authors： Diwakar SD,Bhagwat SS,Shingare MS,Gill CH

更新日期：2008-08-15 00:00:00

abstract：:We report here the synthesis and biological evaluation of a series of 37 compounds as precursors of potent antimalarial bis-thiazolium salts (T3 and T4). These prodrugs were either thioester, thiocarbonate or thiocarbamate type and were synthesized in one step by reaction of an alkaline solution of the parent drug wit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Caldarelli SA,Boisbrun M,Alarcon K,Hamzé A,Ouattara M,Salom-Roig X,Maynadier M,Wein S,Peyrottes S,Pellet A,Calas M,Vial H

更新日期：2010-07-01 00:00:00

abstract：:Beta-hemoglobinopathies such as sickle cell disease represent a major global unmet medical need. De-repression of fetal hemoglobin in erythrocytes is a clinically validated approach for the management of sickle cell disease, but the only FDA-approved medicine for this purpose has limitations to its use. We conducted a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Benowitz AB,Eberl HC,Erickson-Miller CL,Gilmartin AG,Gore ER,Montoute MN,Wu Z

更新日期：2018-12-15 00:00:00

abstract：:Surface enhanced resonance Raman scattering (SERRS) is an alternative to fluorescence for use in bioanalysis however due to the different optical mechanism it requires specifically designed reporters. Recently we have reported the use of 8-hydroxyquinolinyl azo dyes and their ester derivatives as reporters of lipase a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ingram A,Moore BD,Graham D

更新日期：2009-03-15 00:00:00

abstract：:Two series of 1-alkyl-2-aryl-4-(1-naphthoyl)pyrroles were synthesized and their affinities for the cannabinoid CB(1) and CB(2) receptors were determined. In the 2-phenyl series (5) the N-alkyl group was varied from n-propyl to n-heptyl. A second series of 23 1-pentyl-2-aryl-4-(1-naphthoyl)-pyrroles (6) was also prepar...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huffman JW,Padgett LW,Isherwood ML,Wiley JL,Martin BR

更新日期：2006-10-15 00:00:00

abstract：:The synthesis and biological activity of novel CD-ring modified analogues of 22-oxa-1alpha,25-dihydroxyvitamin D(3), lacking the D-ring and featuring a connection between C-12 and C-21 (cis-perhydrindane CE-ring analogues), is described. The synthesis of the CE-ring system follows Meyers' methodology for the preparati...

journal_title：Bioorganic & medicinal chemistry letters

authors： Demin S,Van Haver D,Vandewalle M,De Clercq PJ,Bouillon R,Verstuyf A

更新日期：2004-08-02 00:00:00

abstract：:Makomotindoline (1) was isolated from Makomotake, Zizania latifolia infected with Ustilago esculenta. The structure was determined by the interpretation of spectroscopic data and synthesis. Makomotindoline (1), its l-Glc isomer (2) and its aglycon (3) were synthesized and their effects on rat glioma cells showed adver...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suzuki T,Choi JH,Kawaguchi T,Yamashita K,Morita A,Hirai H,Nagai K,Hirose T,Omura S,Sunazuka T,Kawagishi H

更新日期：2012-07-01 00:00:00

abstract：:A prodrug based on a known antibacterial compound is reported to target Staphylococcus aureus and Escherichia coli under reductive conditions. The prodrug was prepared by masking the N-terminus and side chain amines of a component lysine residue as 4-nitrobenzyl carbamates. Activation to liberate the antibacterial was...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yeoh YQ,Horsley JR,Polyak SW,Abell AD

更新日期：2020-06-01 00:00:00

abstract：:Double-stranded RNA has become a ubiquitous tool for inhibition of gene expression in the laboratory. If similar success could be achieved in vivo, duplex RNA might provide a new class of therapeutics capable of treating a broad spectrum of disease. Chemists and biologists developing duplex RNA as a drug have made pro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Watts JK,Corey DR

更新日期：2010-06-01 00:00:00