Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.

abstract：:The synthesis of novel C6-aryl substituted derivatives of 3-(dimethylamino)chroman is described. The novel derivatives display 5-HT(7) receptor affinities that varies from nM to muM, indicating that this small set of derivatives constitute a novel and interesting starting point for further structure-serotonin 5-HT(7) ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Holmberg P,Tedenborg L,Rosqvist S,Johansson AM

更新日期：2005-02-01 00:00:00

abstract：:Several chemically modified analogues to a tightly binding ligand for the second PDZ domain of MAGI-3 were synthesized and evaluated for their ability to compete with native peptide ligands. N-methyl scanning of the ligand backbone amides revealed the energetically important hydrogen bonds between the ligand backbone ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Novak KA,Fujii N,Guy RK

更新日期：2002-09-02 00:00:00

abstract：:N-substituted chitosan and quaternized chitosan were synthesized and their antioxidant activity against hydroxyl radicals was assessed, respectively. Compared with the antioxidant activity of chitosan, the results indicated that the two kinds of chitosan derivatives had different scavenging ability on hydroxyl radical...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guo Z,Liu H,Chen X,Ji X,Li P

更新日期：2006-12-15 00:00:00

abstract：:Amyloid-β (Aβ) deposition and oxidative stress observed in the brains of patients with Alzheimer's disease (AD) are important targets for therapeutic intervention. In this study, we conjugated the antioxidants caffeic acid (CA) and dihydrocaffeic acid (DHCA) to Aβ1-42 C-terminal motifs (Aβx-42: x=38, 40) to synthesize...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arai T,Ohno A,Mori K,Kuwata H,Mizuno M,Imai K,Hara S,Shibanuma M,Kurihara M,Miyata N,Nakagawa H,Fukuhara K

更新日期：2016-11-15 00:00:00

abstract：:The discovery and SAR of a series of potent renin inhibitors possessing a novel biaryl scaffold are described herein. Molecular modeling revealed that the cyclopropylamide spacer present in 1 can be replaced by a simple, substituted aromatic ring such as a toluene in 2. The resulting compounds exhibit subnanomolar ren...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lacombe P,Aspiotis R,Bayly C,Chen A,Dubé D,Fortin R,Gallant M,Juteau H,Liu S,McKay D,Roy P,Wu T

更新日期：2010-10-01 00:00:00

abstract：:In order to obtain information regarding the design of selective DPP4 inhibitors, a 3D-QSAR study was conducted using DPP4, DPP8, and DPP9 inhibitors including newly synthesized six- and seven-membered cyclic hydrazine derivatives (KR64300, KR64301), which were evaluated in vitro for their inhibition of DPP4, DPP8, an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kang NS,Ahn JH,Kim SS,Chae CH,Yoo SE

更新日期：2007-07-01 00:00:00

abstract：:To improve the DNA hydrolytic activity of the zinc finger nuclease, we have created a new artificial zinc finger nuclease (ZWH4) by connecting two distinct zinc finger domains possessing different types of Zn(II) binding sites (Cys(2)His(2)- and His(4)-types). The overall fold of ZWH4 is similar to that of the wild-ty...

journal_title：Bioorganic & medicinal chemistry letters

authors： Negi S,Umeda Y,Masuyama S,Kano K,Sugiura Y

更新日期：2009-05-15 00:00:00

abstract：:A new series of 1,2,4-triazole-linked urea and thiourea conjugates have been synthesized and evaluated for their in vitro cytotoxicity against selected human cancer cell lines namely, breast (MCF-7, MDA-MB-231), lung (A549) prostate (DU145) and one mouse melanoma (B16-F10) cell line and compared with reference drug. T...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tokala R,Bale S,Janrao IP,Vennela A,Kumar NP,Senwar KR,Godugu C,Shankaraiah N

更新日期：2018-06-01 00:00:00

abstract：:A new cytotoxic oxysterol, 16beta-hydroxy-5alpha-cholestane-3,6-dione was isolated from the red alga Jania rubens. Its structure was established by spectroscopic method. The ID50 value was 0.5 microg/mL. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ktari L,Blond A,Guyot M

更新日期：2000-11-20 00:00:00

abstract：:A series of amino-pyrimidines was developed based upon an initial kinase cross-screening hit from a CDK2 program. Kinase profiling and structure-based drug design guided the optimization from the initial 1,2,3-benzotriazole hit to a potent and selective JNK inhibitor, compound 24f (JNK1 and 2 IC(50)=16 and 66 nM, resp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Palmer WS,Alam M,Arzeno HB,Chang KC,Dunn JP,Goldstein DM,Gong L,Goyal B,Hermann JC,Hogg JH,Hsieh G,Jahangir A,Janson C,Jin S,Ursula Kammlott R,Kuglstatter A,Lukacs C,Michoud C,Niu L,Reuter DC,Shao A,Silva T,Tr

更新日期：2013-03-01 00:00:00

abstract：:The synthesis and biological activity of sordarin oxazepine derivatives are described. The key step features a regioselective oxidation of an unprotected triol followed by double reductive amination to afford the ring-closed products. The spectrum of antifungal activity for these novel derivatives includes coverage of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Serrano-Wu MH,St Laurent DR,Chen Y,Huang S,Lam KR,Matson JA,Mazzucco CE,Stickle TM,Tully TP,Wong HS,Vyas DM,Balasubramanian BN

更新日期：2002-10-07 00:00:00

abstract：:In the search of new antihyperglycemic agents and following rational approach of drug designing here new 2-hydrazolyl-4-thiazolidinone-5-carboxylic acids (4a-g) with pyrazolyl pharmacophore have been synthesized via thia Michael addition reaction of 1-((3-(4-substituted phenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)thios...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bhosle MR,Mali JR,Pal S,Srivastava AK,Mane RA

更新日期：2014-06-15 00:00:00

abstract：:This manuscript concludes the Structure Activity Relationship (SAR) on the pyridazinone scaffold and identifies a compound with subnanomolar p38α activity and 24h coverage in the rat arthritis efficacy model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tynebor RM,Chen MH,Natarajan SR,O'Neill EA,Thompson JE,Fitzgerald CE,O'Keefe SJ,Doherty JB

更新日期：2012-09-15 00:00:00

abstract：:Regioselective synthesis, biological evaluation and 3D-molecular modeling for a series of novel diastereomeric 2-thioxo-5H-dispiro[imidazolidine-4,3-pyrrolidine-2,3-indole]-2,5(1H)-diones are described. The studied compounds have been tentatively identified as potent small molecule MDM2/p53 PPI inhibitors and can ther...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ivanenkov YA,Vasilevski SV,Beloglazkina EK,Kukushkin ME,Machulkin AE,Veselov MS,Chufarova NV,Chernyaginab ES,Vanzcool AS,Zyk NV,Skvortsov DA,Khutornenko AA,Rusanov AL,Tonevitsky AG,Dontsova OA,Majouga AG

更新日期：2015-01-15 00:00:00

abstract：:We have synthesized a series of 4H,6H-[1,2,5]oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide nucleoside and their anti-vesicular stomatitis virus (VSV) activities in Wish cell were also investigated in vitro. It was found that most compounds showed obvious anti-VSV activities and compound 9 with ribofuranoside improved ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu X,Wang J,Yao Q

更新日期：2015-01-15 00:00:00

abstract：:Based on the structure of 4-hydroxy-3-methyl-6-phenylbenzofuran-2-carboxylic acid ethyl ester (1), which exhibits selective cytotoxicity against a tumorigenic cell line, (2,4-dimethoxyphenyl)-(4-hydroxy-3-methyl-6-phenylbenzofuran-2-yl)-methanone (18m) was designed and synthesized as a biologically stable derivative c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hayakawa I,Shioya R,Agatsuma T,Furukawa H,Naruto S,Sugano Y

更新日期：2004-01-19 00:00:00

abstract：:Chemical modifications are essential to improve metabolic stability and pharmacokinetic properties of siRNA to enable their systemic delivery. We investigated the effect of combing the phosphorothioate (PS) modification with metabolically stable phosphate analog (E)-5'-vinylphosphonate and GalNAc cluster conjugation o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Prakash TP,Kinberger GA,Murray HM,Chappell A,Riney S,Graham MJ,Lima WF,Swayze EE,Seth PP

更新日期：2016-06-15 00:00:00

abstract：:Two new merosesquiterpenes, verruculides A (1) and B (2), were isolated from a culture broth of the Indonesian ascidian-derived Penicillium verruculosum TPU1311, together with three known congeners, chrodrimanins A (3), B (4), and H (5). The structures of 1 and 2 were assigned on the basis of their spectroscopic data ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yamazaki H,Nakayama W,Takahashi O,Kirikoshi R,Izumikawa Y,Iwasaki K,Toraiwa K,Ukai K,Rotinsulu H,Wewengkang DS,Sumilat DA,Mangindaan RE,Namikoshi M

更新日期：2015-08-15 00:00:00

abstract：:Nicotinic acid (niacin) has been used for decades as an antidyslipidemic drug in man. Its main target is the hydroxy-carboxylic acid receptor HCA2 (GPR109A), a G protein-coupled receptor. Other acids and esters such as methyl fumarate also interact with the receptor, which constituted the basis for the current study. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： van Veldhoven JP,Blad CC,Artsen CM,Klopman C,Wolfram DR,Abdelkadir MJ,Lane JR,Brussee J,Ijzerman AP

更新日期：2011-05-01 00:00:00

abstract：:Selective inhibitors of protein tyrosine phosphatases (PTPases) are of great interest as therapeutic agents and research tools. Several phenylalanine derivatives (1, 2) designed as phosphotyrosine mimetics or irreversible active site inhibitors were successfully synthesized, then incorporated into a combinatorial libr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yan Z,Kahn M,Qabar M,Urban J,Kim HO,Blaskovich MA

更新日期：2003-06-16 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：:By means of functional interconversions in ring D of the tetracyclic diterpene isosteviol (ent-16-ketobeyeran-19-oic acid 1), various 15- and 16-substituted isosteviol derivatives were stereoselectively prepared. The cytotoxic activities in vitro of these new isosteviol derivatives were investigated, and some of them ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wu Y,Dai GF,Yang JH,Zhang YX,Zhu Y,Tao JC

更新日期：2009-03-15 00:00:00

abstract：:A new class of NO-donor phenol derivatives is described. The products were obtained by joining appropriate phenols with either nitrooxy or 3-phenylsulfonylfuroxan-4-yloxy moieties. All the compounds proved to inhibit the ferrous salt/ascorbate induced lipidic peroxidation of membrane lipids of rat hepatocytes. They we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cena C,Boschi D,Tron GC,Chegaev K,Lazzarato L,Di Stilo A,Aragno M,Fruttero R,Gasco A

更新日期：2004-12-20 00:00:00

abstract：:Structure-activity relationship studies directed toward improving the metabolic stability of compound 1 resulted in the identification of 3-[5-(3,5-difluorophenyl)-3-({[(1S,3R)-3-fluorocyclopentyl]amino}methyl)-4-methyl-1H-pyrazol-1-yl]propanenitrile 39 (MK-1925) as a selective, orally available and brain-penetrable o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kobayashi K,Tsujita T,Ito H,Ozaki S,Tani T,Ishii Y,Okuda S,Tadano K,Fukuroda T,Ohta H,Okamoto O

更新日期：2009-08-15 00:00:00

abstract：:Reaction of TBDMS-protected bile acids (cholic, chenodeoxycholic, deoxycholic, lithocholic, ursodeoxycholic acids) or dehydrocholic acid with aromatic/heterocyclic sulfonamides possessing free amino/hydroxy moieties, in the presence of carbodiimides, afforded after deprotection of the OTBDMS ethers, a series of sulfon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Scozzafava A,Supuran CT

更新日期：2002-06-17 00:00:00

abstract：:Novel phenothiazine derivatives bearing an amino acid residue were synthesized via peptide chemistry, and evaluated for their inhibitory potential on human farnesyltransferase. The phenothiazine unit proved to be an important bulky unit in the structure of the synthesized inhibitors. Propargyl ester 20 bearing a tyros...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dumitriu GM,Ghinet A,Bîcu E,Rigo B,Dubois J,Farce A,Belei D

更新日期：2014-07-15 00:00:00

abstract：:Synthesis of 13'[(cholest-5-en)-3beta-yloxyethoxycarbamoyl]-chlorin e6 starting from methylpheophorbide and 3beta(2-hydroxy)-ethoxycholest-5-ene is presented, as well as the preparation of related copper complex. Both conjugates obtained may be simply incorporated in phosphatidyl choline vesicles. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nikolaeva IA,Misharin AY,Ponomarev GV,Timofeev VP,Tkachev YV

更新日期：2010-05-01 00:00:00

abstract：:N-Substituted cyclam-amino acid conjugates have been synthesised both in solution and on the solid phase. The DNA binding affinity of these species has been studied: the nature of the amino acid strongly influences the change in melting temperature suggesting that simple cyclam-peptide conjugates could interact with D...

journal_title：Bioorganic & medicinal chemistry letters

authors： Venkata Ramana A,Watkinson M,Todd MH

更新日期：2008-05-01 00:00:00

abstract：:The synthesis of 1- and 2-substituted aza-benzothiopyranoindazoles has been accomplished. The comparisons of the in vitro antitumor activities of the 2-substituted analogues with the benzothiopyranoindazole chemotypes indicate that the positioning of the nitrogen atom at C-9 (9-aza analogue 4d) leads to a substrate wi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Krapcho AP,Haydar SN,Truong-Chiott S,Hacker MP,Menta E,Beggiolin G

更新日期：2000-02-07 00:00:00

abstract：:EZH2 is the core subunit of Polycomb repressive complex 2 catalyzing the methylation of histone H3 lysine-27 and closely involved in tumorigenesis. To discover small molecule inhibitors for EZH2 methyltransferase activity, we performed an inhibitor screen with catalytically active EZH2 protein complex and identified t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Woo J,Kim HY,Byun BJ,Chae CH,Lee JY,Ryu SY,Park WK,Cho H,Choi G

更新日期：2014-06-01 00:00:00