Degradation of target protein in living cells by small-molecule proteolysis inducer.

abstract：:A series of pyridine-linked indanone derivatives were designed and synthesized to discover new small molecules for the treatment of inflammatory bowel disease (IBD). Compounds 5b and 5d exhibited strongest inhibitory activity against TNF-α-induced monocyte adhesion to colon epithelial cells (an in vitro model of colit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kadayat TM,Banskota S,Bist G,Gurung P,Magar TBT,Shrestha A,Kim JA,Lee ES

更新日期：2018-08-01 00:00:00

abstract：:SAR studies for the exploration a novel class of anti-human immunodeficiency virus type 1 (HIV-1) agents based on the hematoxylin structure (1) are described. The systematic deoxygenations of 1 including asymmetric synthesis were conducted to obtain a compound showing high potencies for inhibiting the nuclear import a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ishii H,Koyama H,Hagiwara K,Miura T,Xue G,Hashimoto Y,Kitahara G,Aida Y,Suzuki M

更新日期：2012-02-01 00:00:00

abstract：:The discovery of potent benzimidazole stearoyl-CoA desaturase (SCD1) inhibitors by ligand-based virtual screening is described. ROCS 3D-searching gave a favorable chemical motif that was subsequently optimized to arrive at a chemical series of potent and promising SCD1 inhibitors. In particular, compound SAR224 was se...

journal_title：Bioorganic & medicinal chemistry letters

authors： Matter H,Zoller G,Herling AW,Sanchez-Arias JA,Philippo C,Namane C,Kohlmann M,Pfenninger A,Voss MD

更新日期：2013-03-15 00:00:00

abstract：:Strigolactones (SLs) are new plant hormones with varies important bio-functions. This Letter deals with germination of seeds of parasitic weeds. Natural SLs have a too complex structure for synthesis. Therefore, there is an active search for SL analogues and mimics with a simpler structure with retention of activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zwanenburg B,Nayak SK,Charnikhova TV,Bouwmeester HJ

更新日期：2013-09-15 00:00:00

abstract：:A series of 4beta-arylamino-4'-O-demethylepipodophyllotoxins and 4beta-arylaminoepipodophyllotoxins have been synthesized with significant stereoselectivity and improved yields by employing the methanesulphonic acid/sodium iodide reagent system. Compounds NPF. W-68 and other DNA topoisomerase II inhibitors are prepare...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kamal A,Laxman N,Ramesh G

更新日期：2000-09-18 00:00:00

abstract：:A series of substituted biphenyl ethylene ether compounds has been designed to target the gp41N-trimer in order to inhibit formation of the six-helical bundle that represents the end state of gp41-mediated viral fusion. A size exclusion HPLC based helical bundle formation (HBF) assay was developed to evaluate in vitro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu B,Joseph RW,Dorsey BD,Schiksnis RA,Northrop K,Bukhtiyarova M,Springman EB

更新日期：2009-10-01 00:00:00

abstract：:The enzyme ATP citrate lyase (ACL) catalyzes the formation of cytosolic acetyl CoA, the starting material for de novo lipid and cholesterol biosynthesis. The dysfunction and upregulation of ACL in numerous cancers makes it an attractive target for developing anticancer therapies. ACL inhibition by shRNA knockdown limi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jernigan FE,Hanai JI,Sukhatme VP,Sun L

更新日期：2017-02-15 00:00:00

abstract：:A new abietane, namely, 20-hydroxyferruginol (1), together with known ferruginol (2), 18-hydroxyferruginol (3), sugiol (4), and 6alpha-hydroxysugiol (5), were isolated from the cones of Sequoia sempervirens. Their structures were elucidated through spectral data. Compounds 1 and 5 strongly inhibited colon, lung, and b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Son KH,Oh HM,Choi SK,Han DC,Kwon BM

更新日期：2005-04-15 00:00:00

abstract：:Screening of a metalloprotease library led to the identification of a thiol-based dual ACE/NEP inhibitor as a potent ACE2 inhibitor. Modifications of the P(1) benzyl moiety led to improvements in ACE2 potency as well as to increased selectivity versus ACE and NEP. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deaton DN,Gao EN,Graham KP,Gross JW,Miller AB,Strelow JM

更新日期：2008-01-15 00:00:00

abstract：:The syntheses and anti-tuberculosis activity of quinolone-cephalosporin conjugates (1 and 2) are described. Both showed broad-spectrum antibacterial activity and significant anti-TB activity. The carbamate-linked quinolone-cephem 2 showed better antimycobacterial activity, including anti-TB activity, than the direct a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao G,Miller MJ,Franzblau S,Wan B,Möllmann U

更新日期：2006-11-01 00:00:00

abstract：:A series of tertiary amine analogs derived from lead azaaromatic quaternary ammonium salts has been designed and synthesized. The preliminary structure-activity relationships of these new analogs suggest that such tertiary amine analogs, which potently inhibit nicotine-evoked dopamine release from rat striatum, repres...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang Z,Zheng G,Pivavarchyk M,Deaciuc AG,Dwoskin LP,Crooks PA

更新日期：2011-01-01 00:00:00

abstract：:A major challenge in the application of cytotoxic anti-cancer drugs is their general lack of selectivity, which often leads to systematic toxicity due to their inability to discriminate between malignant and healthy cells. A particularly promising target for selective targeting are the folate receptors (FR) that are o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Geersing A,de Vries RH,Jansen G,Rots MG,Roelfes G

更新日期：2019-08-01 00:00:00

abstract：:VanX, a Zn(II)-dependent D-ala-D-ala dipeptidase, is essential for vancomycin resistance in Enterococcus faecium. The enzymatic activity of VanX was previously found to be inhibited competitively by 2-{[(1-aminoethyl) (hydroxy) phosphoryl]oxy} propanoic acid (1B). Here we report the synthesis and characterization of s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jia C,Yang KW,Liu CC,Feng L,Xiao JM,Zhou LS,Zhang YL

更新日期：2012-01-01 00:00:00

abstract：:A series of 1-aminotetralin scaffolds was synthesized via metal-catalyzed ring-opening reactions of heterobicyclic alkenes. Small libraries of amides and amines were made using the amino group of each scaffold as a handle. Screening of these libraries against human opioid receptors led to the identification of (S)-(S)...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dockendorff C,Jin S,Olsen M,Lautens M,Coupal M,Hodzic L,Spear N,Payza K,Walpole C,Tomaszewski MJ

更新日期：2009-02-15 00:00:00

abstract：:Two cyclopropanecarbonyl derivatives were independently found to be 15 and 14 times more potent than the corresponding isopropylcarbonyl analogues as inhibitors of 4-hydroxyphenylpyruvate dioxygenase and dihydroorotate dehydrogenase, respectively. A thorough examination of the co-crystal structures of available enzyme...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kuo PY,Shie TL,Chen YS,Lai JT,Yang DY

更新日期：2006-12-01 00:00:00

abstract：:Model reactions offer a chemical mechanism by which formation of a sulfenyl amide residue at the active site of the redox-regulated protein tyrosine phosphatase PTP1B protects the cysteine redox switch in this enzyme against irreversible oxidative destruction. The results suggest that 'overoxidation' of the sulfenyl a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sivaramakrishnan S,Cummings AH,Gates KS

更新日期：2010-01-15 00:00:00

abstract：:A series of (S)-N-(1,4-naphthoquinon-2-yl)-alpha-amino acid methyl esters 3-9, 2-N,N-dialkylamino-1,4-naphthoquinones 10-11 and 2-hydroxy-3-(2'-mercaptoimidazolyl)-1,4-naphthoquinones and their cyclic analogs 12-15 were synthesized and evaluated for antifungal and antibacterial activities. The structure-activity relat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tandon VK,Yadav DB,Singh RV,Chaturvedi AK,Shukla PK

更新日期：2005-12-01 00:00:00

abstract：:Triple-negative breast cancer (TNBC) has been reported to be correlated with high expression of proliferation markers as well as constitutive activation of metastasis-relevant signaling pathways. For many years, breast cancer researchers have been investigating specific and effective methods to treat or to control the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen L,Long C,Nguyen J,Kumar D,Lee J

更新日期：2018-02-01 00:00:00

abstract：:A number of novel 1-(3-arylprop-2-ynyl) substituted 1,2-dihydroquinoline derivatives related to nimesulide and their 2-oxo analogues have been designed as potential inhibitors of PDE4. All these compounds were synthesized by using Sonogashira coupling as a key step. In vitro PDE4B inhibitory properties and molecular m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pal S,Durgadas S,Nallapati SB,Mukkanti K,Kapavarapu R,Meda CL,Parsa KV,Pal M

更新日期：2011-11-01 00:00:00

abstract：:Bioassay-guided fractionation of the EtOAc extract of the stem bark of Erythrina abyssinica (Leguminosae) resulted in the isolation of three new (1-3), along with 12 known (4-15) pterocarpan derivatives. Their chemical structures were determined by physicochemical and spectroscopic data analysis (IR, UV, [alpha](D), C...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nguyen PH,Le TV,Thuong PT,Dao TT,Ndinteh DT,Mbafor JT,Kang KW,Oh WK

更新日期：2009-12-01 00:00:00

abstract：:A stereoselective synthesis of dinucleoside boranophosphates by using nucleoside 3'-oxazaphospholidine derivatives is described. The diastereoselectivity of the internucleotidic bond formation reactions varied with the nucleobase used. (Rp)- and (Sp)-dithymidine boranophosphates were synthesized with excellent diaster...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wada T,Maizuru Y,Shimizu M,Oka N,Saigo K

更新日期：2006-06-15 00:00:00

abstract：:A series of novel 1-acetyl-3-(3,4-dimethoxypheny)-5-(4-(3-(arylureido/arylthioureido/arylsulfonamido) phenyl)-4,5-dihydropyrazole derivatives of biological interest have been prepared by sequential cyclization of 1-(4-nitrophenyl)-3-(3,4-dimethoxyphenyl)-pro-2-ene-1 with hydrazine hydrate, reduction followed by reacti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Keche AP,Hatnapure GD,Tale RH,Rodge AH,Kamble VM

更新日期：2012-11-01 00:00:00

abstract：:A protocol applicable for the synthesis of an oseltamivir positron emission tomography (PET) tracer was developed. Acetylation of amine 3 with CH(3)COCl, followed by deprotection and aqueous workup, produced oseltamivir 4 from 3 within 10 min. The obtained 4 was sufficiently pure for PET studies. This method can be ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Morita M,Sone T,Yamatsugu K,Sohtome Y,Matsunaga S,Kanai M,Watanabe Y,Shibasaki M

更新日期：2008-01-15 00:00:00

abstract：:In continuation of our efforts to find new antimicrobial compounds, series of fatty N-acyldiamines were prepared from fatty methyl esters and 1,2-ethylenediamine, 1,3-propanediamine or 1,4-butanediamine. The synthesized compounds were screened for their antibacterial activity against Gram-positive bacteria (Staphyloco...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ferreira BDS,de Almeida AM,Nascimento TC,de Castro PP,Silva VL,Diniz CG,Le Hyaric M

更新日期：2014-10-01 00:00:00

abstract：:A series of pyrazoline derivatives were prepared for evaluating their acyl-CoA:cholesterol acyltransferase activities. 3-(3,5-Di-tert-butyl-4-hydroxyphenyl)-5-(multi-substituted 4-hydroxyphenyl)-2-pyrazolines 4a-i were shown in vitro inhibitory activity on hACAT-1 and -2. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jeong TS,Kim KS,An S,Cho KH,Lee S,Lee WS

更新日期：2004-06-07 00:00:00

abstract：:Current biosynthetic methods for producing proteins containing site-specifically incorporated unnatural amino acids are inefficient because the majority of the amino acid goes unused. Here we present a universal approach to improve the efficiency of such processes using condensed Escherichia coli cultures. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu J,Castañeda CA,Wilkins BJ,Fushman D,Cropp TA

更新日期：2010-10-01 00:00:00

abstract：:A series of novel pyrimido[1,2-b]indazoles 5, 7 have been prepared from 3-trifluoromethyl-5-phenyl-2,6-dicyano anilines 1 via novel indazole regioisomers 3 and 4 through a facile strategy. Specific examples were evaluated for anticancer activity in vitro and found to exhibit promising activity against A-549 cell lines...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yakaiah T,Lingaiah BP,Narsaiah B,Shireesha B,Ashok Kumar B,Gururaj S,Parthasarathy T,Sridhar B

更新日期：2007-06-15 00:00:00

abstract：:The design of potent Pin1 inhibitors has been challenging because its active site specifically recognizes a phospho-protein epitope. The de novo design of phosphate-based Pin1 inhibitors focusing on the phosphate recognition pocket and the successful replacement of the phosphate group with a carboxylate have been prev...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guo C,Hou X,Dong L,Marakovits J,Greasley S,Dagostino E,Ferre R,Johnson MC,Humphries PS,Li H,Paderes GD,Piraino J,Kraynov E,Murray BW

更新日期：2014-09-01 00:00:00

abstract：:A novel class of MurF inhibitors was discovered and structure-activity relationship studies have led to several potent compounds with IC(50)=22 approximately 70 nM. Unfortunately, none of these potent MurF inhibitors exhibited significant antibacterial activity even in the presence of bacterial cell permeabilizers. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gu YG,Florjancic AS,Clark RF,Zhang T,Cooper CS,Anderson DD,Lerner CG,McCall JO,Cai Y,Black-Schaefer CL,Stamper GF,Hajduk PJ,Beutel BA

更新日期：2004-01-05 00:00:00

abstract：:A series of novel amide functionalized 2H-chromene derivatives 3 were prepared starting from ethyl-2-hydroxy-2-(trifluoromethyl)-2H-chromene-3-carboxylate 1 via sodium borohydride reduction followed by Ritter amidation using HBF4·OEt2 as a mild and versatile reagent. All the products 3 were screened for antimicrobial ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ratnakar Reddy K,Poornachandra Y,Jitender Dev G,Mallareddy G,Nanubolu JB,Kumar CG,Narsaiah B

更新日期：2015-08-01 00:00:00