Synthesis of cynaropicrin-d(4).

abstract：:Two new austalide meroterpenoids, named austalides V and W (1 and 2), were isolated from the fungus Aspergillus ustus VKM F-4692. Their structures were elucidated by extensive spectroscopic analysis and by comparison with related known compounds. The main structural feature of both compounds is a tetrahydrofuranyl rin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Antipova TV,Zaitsev KV,Oprunenko YF,Ya Zherebker A,Rystsov GK,Zemskova MY,Zhelifonova VP,Ivanushkina NE,Kozlovsky AG

更新日期：2019-11-15 00:00:00

abstract：:The multiple-step, one-pot procedure for a series of 2-substituted-3-phosphono-1-thia-4-aza-2-cyclohexene-5-carboxylates, analogues of the natural, sulfur amino acid metabolite lanthionine ketimine (LK), its 5-ethyl ester (LKE) and 2-substituted LKEs is described. Initiating the synthesis with the Michaelis-Arbuzov pr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shen D,Hensley K,Denton TT

更新日期：2018-02-15 00:00:00

abstract：:Pinostrobin (5-hydroxy-7-methoxyflavanone) obtained in relatively large amounts from fingerroot (Boesenbergia pandurata) was converted to its C-6 and C-8 prenylated derivatives. The Mitsunobu reaction, europium(III)-catalyzed Claisen-Cope rearrangement, and Claisen reaction coupled with cross-metathesis were used as t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Poerwono H,Sasaki S,Hattori Y,Higashiyama K

更新日期：2010-04-01 00:00:00

abstract：:Two reactive metabolites were identified in vivo for the dual A(2A)/A(1) receptor antagonist 1. Two strategies were implemented to successfully mitigate the metabolic liabilities associated with 1. Optimization of the arylindenopyrimidines led to a number of amide, ether, and amino analogs having comparable in vitro a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shook BC,Rassnick S,Chakravarty D,Wallace N,Ault M,Crooke J,Barbay JK,Wang A,Leonard K,Powell MT,Alford V,Hall D,Rupert KC,Heintzelman GR,Hansen K,Bullington JL,Scannevin RH,Carroll K,Lampron L,Westover L,Russell

更新日期：2010-05-01 00:00:00

abstract：:The structure activity relationship on a series of ester and hydroxamate analogues of methionyl and isoleucyl adenylate has been investigated through introducing linkers between the 1'-position of ribose and adenine surrogates as methionyl-tRNA, and isoleucyl-tRNA synthetase inhibitors, respectively. The results indic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee J,Kang SU,Kim SY,Kim SE,Kang MK,Jo YJ,Kim S

更新日期：2001-04-23 00:00:00

abstract：:New analogues of the venerable antimalarial drug primaquine have been synthesized and bioassayed in vivo against Pneumocystis carinii, a life-threatening infection common among immunosuppressed patients. Two of these new compounds are significantly more active than primaquine itself, and provide new information for fu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Goodwin TE,Boylan CJ,Current WL,Byrd JC,Edwards CB,Fuller DA,Green JL,Larocca CD,Raney KD,Ross AS,Tucker WA

更新日期：2000-10-02 00:00:00

abstract：:The Hedgehog (Hh-) signalling pathway is a key developmental pathway and there is a growing body of evidence showing that this pathway is aberrantly reactivated in a number of human tumors. Novel agents capable of inhibiting this pathway are sought, and an entirely novel series of smoothened (Smo) antagonists capable ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ontoria JM,Bufi LL,Torrisi C,Bresciani A,Giomini C,Rowley M,Serafini S,Bin H,Hao W,Steinkühler C,Jones P

更新日期：2011-09-15 00:00:00

abstract：:6-Nitroquipazine has been known as one of the most potent and selective inhibitors of serotonin transporter in vitro and in vivo. Nine derivatives of 6-nitroquipazine were synthesized and tested for their potential abilities to displace [3H]citalopram binding to the rat cortical membranes. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee BS,Chu S,Lee BC,Chi DY,Choe YS,Jeong KJ,Jin C

更新日期：2000-07-17 00:00:00

abstract：:A new cyclic depsipeptide, designated neamphamide B (1), was isolated from a marine sponge of Neamphius sp. collected at Okinawa, Japan in 1993 as an anti-mycobacterial substance against active and dormant bacilli. The planar structure of neamphamide B (1) was determined on the basis of spectroscopic analysis, and ste...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yamano Y,Arai M,Kobayashi M

更新日期：2012-07-15 00:00:00

abstract：:3-Arylpyrrolidines are synthesized through the coupling of N-benzyl-3-(methanesulfonyloxy)pyrrolidine with diarylcuprates. Pharmacological evaluation of a series of N-substituted-3-arylpyrrolidines toward several neurotransmitter receptors indicated that some of them are good ligands for serotonin 1A receptor. Particu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ahn KH,Lee SJ,Lee CH,Hong CY,Park TK

更新日期：1999-05-17 00:00:00

abstract：:A small library of 1-aminoalkyl 2-naphthols has been synthesized through the direct Mannich reaction of 2-naphthols with (hetero)aromatic aldehydes and secondary amines. All of the Mannich bases having a thiophen-2-yl ring in their structure had good activity against Gram-positive bacteria, irrespective of the nature ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Roman G,Năstasă V,Bostănaru AC,Mareş M

更新日期：2016-05-15 00:00:00

abstract：:A 1,8-naphthalimide-Cu(II) ensemble was rationally designed and synthesized as a new turn-on fluorescent probe utilizing the 'chemosensing ensemble' method for detections of thiols (Cys, Hcy and GSH) with high selectivity over other α-amino acids at pH 7.4 in organic aqueous media (EtOH/HEPES, v/v=9:1). The recognitio...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shi YG,Yao JH,Duan YL,Mi QL,Chen JH,Xu QQ,Gou GZ,Zhou Y,Zhang JF

更新日期：2013-05-01 00:00:00

abstract：:A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives were synthesized via converting the readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and then reacting with different substituted amines. The molecular struct...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rambabu D,Mulakayala N,Ismail,Kumar KR,Kumar GP,Mulakayala C,Kumar CS,Kalle AM,Rao MV,Oruganti S,Pal M

更新日期：2012-11-01 00:00:00

abstract：:Starting from a weak omeprazole screening hit, replacement of the pyridine with a 1,3-benzodioxole moiety, modification of the thioether linkage, and substitution of the benzimidazole pharmacophore led to the discovery of nanomolar BRS-3 agonists. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Carlton DL,Collin-Smith LJ,Daniels AJ,Deaton DN,Goetz AS,Laudeman CP,Littleton TR,Musso DL,Morgan RJ,Szewczyk JR,Zhang C

更新日期：2008-10-15 00:00:00

abstract：:Bioconjugate formats provide alternative strategies for antigen targeting with bispecific antibodies. Here, PSMA-targeted Fab conjugates were generated using different bispecific formats. Interchain disulfide bridging of an αCD3 Fab enabled installation of either the PSMA-targeting small molecule DUPA (SynFab) or the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patterson JT,Isaacson J,Kerwin L,Atassi G,Duggal R,Bresson D,Zhu T,Zhou H,Fu Y,Kaufmann GF

更新日期：2017-12-15 00:00:00

abstract：:We report the discovery and structure-activity relationship of 2,6-disubstituted pyrazines, which are potent and selective CK2 inhibitors. Lead compound 1 was identified, and derivatives were prepared to develop potent inhibitory activity. As a result, we obtained compound 7, which was the smallest unit that retained ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fuchi N,Iura Y,Kaneko H,Nitta A,Suyama K,Ueda H,Yamaguchi S,Nishimura K,Fujii S,Sekiya Y,Yamada M,Takahashi T

更新日期：2012-07-01 00:00:00

abstract：:Based on the X-ray crystallography of our lead compound 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-cyanopyrazin-2-yl)urea in the checkpoint kinase 1 (Chk1) enzyme, we modified R4, and to a lesser extent, R2, and R5 of the phenyl ring, and made a variety of N-aryl-N'-pyrazinylurea Chk1 inhibitors. Enzymatic activity less th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li G,Hasvold LA,Tao ZF,Wang GT,Gwaltney SL 2nd,Patel J,Kovar P,Credo RB,Chen Z,Zhang H,Park C,Sham HL,Sowin T,Rosenberg SH,Lin NH

更新日期：2006-04-15 00:00:00

abstract：:In this work we present the synthesis, aqueous solubility and stability, hydrolysis by alkaline phosphatase, and in vivo fasciolicidal activity in sheep of a highly water soluble phosphate salt prodrug of triclabendazole (MFR-5). The aqueous solubility of MFR-5 at pH 7 was 88,000-fold that of triclabendazole. MFR-5 sh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Flores-Ramos M,Ibarra-Velarde F,Jung-Cook H,Hernández-Campos A,Vera-Montenegro Y,Castillo R

更新日期：2017-02-01 00:00:00

abstract：:The 5-HT3 receptor antagonist tropisetron (ICS 205-930) was found to be a potent and selective partial agonist at alpha7 nicotinic receptors. Two other 5-HT3 receptor antagonists, ondansetron and LY-278,584, were found to lack high affinity at the alpha7 nicotinic receptor. Quinuclidine analogues (1 and 2) of tropiset...

journal_title：Bioorganic & medicinal chemistry letters

authors： Macor JE,Gurley D,Lanthorn T,Loch J,Mack RA,Mullen G,Tran O,Wright N,Gordon JC

更新日期：2001-02-12 00:00:00

abstract：:Early studies led to the identification of 11β-aryl-4',5'-dihydrospiro[estra-4,9-diene-17β,4'-oxazole] analogs with potent and more selective antiprogestational activity compared to antiglucocorticoid activity than mifepristone. In the present study, we replaced the 4'-dimethylaminophenyl group of mifepristone with th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jin C,Fix SE,Kepler JA,Cook CE

更新日期：2012-02-15 00:00:00

abstract：:Inhibition of Rho kinase (ROCK) is an attractive strategy for the treatment of diseases such as hypertension, glaucoma, and cancer. Here we report chroman-3-amides as highly potent ROCK inhibitors with sufficient kinase selectivity, excellent cell activity, good microsomal stability, and desirable pharmacokinetic prop...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen YT,Bannister TD,Weiser A,Griffin E,Lin L,Ruiz C,Cameron MD,Schürer S,Duckett D,Schröter T,LoGrasso P,Feng Y

更新日期：2008-12-15 00:00:00

abstract：:Type-2 diabetes (T2D) is a complex metabolic disease characterized by insulin resistance in the liver and peripheral tissues accompanied by a defect in pancreatic beta-cell. Since their discovery three subtypes of Peroxisomes Proliferators Activated Receptors were identified namely PPARalpha, PPARgamma and PPARbeta/(d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Parmenon C,Guillard J,Caignard DH,Hennuyer N,Staels B,Audinot-Bouchez V,Boutin JA,Dacquet C,Ktorza A,Viaud-Massuard MC

更新日期：2008-03-01 00:00:00

abstract：:The Kemp elimination reaction is a well-known chemical reaction that is facilitated on a protein surface microenvironment, and in particular is highly accelerated in a unique binding pocket of serum albumin. We have designed and synthesized a fluorescently activatable coumarin derivative with a benzisoxazole scaffold ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sakamoto S,Komatsu T,Ueno T,Hanaoka K,Urano Y

更新日期：2017-08-01 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：:In the search for plants, containing compounds with α-glucosidase inhibitory activity, we found that a methanolic extract from the leaves and twigs of Archidendron clypearia (Jack.) Nielsen significantly inhibited rat intestinal sucrase in vitro. A phytochemical investigation of the aqueous layer of an A. clypearia ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thao NP,Luyen BT,Vinh le B,Lee JY,Kwon YI,Kim YH

更新日期：2016-09-01 00:00:00

abstract：:The synthesis of two separable isomeric testosterone dimers is reported. The dimers are made from testosterone in a 5 step sequence and with 36% overall yield. The key dimerization step was performed using Hoveyda-Grubb's metathesis catalysts on 7alpha-allyltestosterone with 75% yield. The synthesis led to separable i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bastien D,Leblanc V,Asselin E,Bérubé G

更新日期：2010-04-01 00:00:00

abstract：:Guided by co-crystal structural information obtained from a different series we were exploring, a scaffold morphing and SBDD approach led to the discovery of the 1,4-disubstituted indazole series as a novel class of GKAs that potently activate GK in enzyme and cell assays. anti-diabetic OGTT efficacy was demonstrated ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cheruvallath ZS,Gwaltney SL 2nd,Sabat M,Tang M,Wang H,Jennings A,Hosfield D,Lee B,Wu Y,Halkowycz P,Grimshaw CE

更新日期：2017-06-15 00:00:00

abstract：:Cu(II) complexes of Alzheimer's disease-related β-amyloid (Aβ) peptides exhibit metal-centered oxidation chemistry. The metallo-Aβ complexes are the hallmark of the disease and have been attributed to the generation of reactive oxygen species (ROS), causing oxidative stress. In this communication, the inhibitions of t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hashim A,Wang L,Juneja K,Ye Y,Zhao Y,Ming LJ

更新日期：2011-11-01 00:00:00

abstract：:Methanolic extract of Miliusa balansae Finet et Gagnep exerts an anti-inflammatory effect via inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated murine RAW 264.7 macrophage cells. Three new megastigmane glycosides, milbasides A-C (1-3), together with fifteen known compounds (4-18), were ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thao NP,Luyen BT,Tai BH,Cuong NM,Kim YC,Minh CV,Kim YH

更新日期：2015-09-15 00:00:00

abstract：:Symmetrically and asymmetrically substituted 1,2,4,5-tetraoxanes were synthesized by the oxidative system H(2)O(2)/TFE in presence of MeReO(3) as a catalyst. All of the synthesized compounds were characterized spectroscopically, and evaluated for cytotoxicity, and antimalarial activity. Several of these tetraoxanes ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Atheaya H,Khan SI,Mamgain R,Rawat DS

更新日期：2008-02-15 00:00:00