abstract：:Proanthocyanidins are oligomers of catechins that exhibit potent antioxidative activity and inhibit binding of oxidized low-density lipoprotein (OxLDL) to the lectin-like oxidized LDL receptor (LOX-1), which is involved in the onset and development of arteriosclerosis. Previous attempts aimed at developing proanthocya...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mizuno M,Nakanishi I,Matsumoto KI,Fukuhara K

更新日期：2017-11-15 00:00:00

abstract：:From a readily available 5-C-Me ribofuranoside, we have realized a reliable route to valuable 5'-deoxy-5'-amino-5'-C-methyl adenosine derivatives at gram scale with confirmed stereochemistry. These adenosine derivatives are useful starting materials for the preparation of 5'-deoxy-5'-amino-5'-C-methyl adenosine deriva...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu T,Xie W,Li C,Ren H,Mao Y,Chen G,Cheng M,Zhao D,Shen J,Li J,Zhou Y,Xiong B,Chen YL

更新日期：2017-11-15 00:00:00

abstract：:Lysine specific demethylase 1 (LSD1), the first identified histone demethylase, plays an important role in epigenetic regulation of gene activation and repression, has been reported to be up-regulated and involved in numbers of solid malignant tumors. In this study, we identified a series of phenylalanyl hydrazones ba...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sun K,Peng JD,Suo FZ,Zhang T,Fu YD,Zheng YC,Liu HM

更新日期：2017-11-15 00:00:00

abstract：:Novel thienopyrimidine compounds 2 and 3 were discovered from high-throughput screening as Natriuretic Peptide Receptor A (NPR-A) agonists. Scaffold hopping of a thienopyrimidine ring to a quinazoline ring, introduction of the basic functional group and optimization of the substituent on the 6-position of the benzene ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Iwaki T,Nakamura Y,Tanaka T,Ogawa Y,Iwamoto O,Okamura Y,Kawase Y,Furuya M,Oyama Y,Nagayama T

更新日期：2017-11-01 00:00:00

abstract：:Pseudomonas aeruginosa is a Gram-negative pathogenic bacterium responsible for severe infections, and it is naturally resistant to many clinically approved antibiotic families. Oxazolidinone antibiotics are active against many Gram-positive bacteria, but are inactive against P. aeruginosa. Increasing the uptake of oxa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Paulen A,Hoegy F,Roche B,Schalk IJ,Mislin GLA

更新日期：2017-11-01 00:00:00

abstract：:A novel series of variously substituted N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-arylsulfonamides has been synthesized and assayed for β-Secretase (BACE1) inhibitory activity. BACE1 is a widely recognized drug target for the prevention and treatment of Alzheimer's Disease (AD). The introduction of benzyl substituents ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bertini S,Ghilardi E,Asso V,Minutolo F,Rapposelli S,Digiacomo M,Saccomanni G,Salmaso V,Sturlese M,Moro S,Macchia M,Manera C

更新日期：2017-11-01 00:00:00

abstract：:Twenty-five novel pregnenolone/2-cyanoacryloyl conjugates (6-30) were designed and prepared, with the aim of developing novel anticancer drugs with dual NF-κB inhibitory and anti-proliferative activities. Compounds 22 and 27-30 showed inhibition against TNF-α-induced NF-κB activation in luciferase assay, which was con...

journal_title：Bioorganic & medicinal chemistry letters

authors： Song JL,Zhang J,Liu CL,Liu C,Zhu KK,Yang FF,Liu XG,Figueiró Longo JP,Alexandre Muehlmann L,Azevedo RB,Zhang YY,Guo YW,Jiang CS,Zhang H

更新日期：2017-10-15 00:00:00

abstract：:Modulation of gastrointestinal nutrient sensing pathways provides a promising a new approach for the treatment of metabolic diseases including diabetes and obesity. The calcium-sensing receptor has been identified as a key receptor involved in mineral and amino acid nutrient sensing and thus is an attractive target fo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sparks SM,Spearing PK,Diaz CJ,Cowan DJ,Jayawickreme C,Chen G,Rimele TJ,Generaux C,Harston LT,Roller SG

更新日期：2017-10-15 00:00:00

abstract：:Primaquine (PQ) is the only commercially available drug that clears dormant liver stages of malaria and blocks transmission to mosquito vectors. Although an old drug, much remains to be known about the mechanism(s) of action. Herein we develop a fluorescent tagged PQ to discover cellular localization in the human mala...

journal_title：Bioorganic & medicinal chemistry letters

authors： McQueen A,Blake LD,Azhari A,Kemp MT,McGaha TW Jr,Namelikonda N,Larsen RW,Manetsch R,Kyle DE

更新日期：2017-10-15 00:00:00

abstract：:A range of amphiphilic sorbitan ethers has been synthesized in two steps from sorbitan following an acetalization/hydrogenolysis sequence. These sorbitan ethers and the acetal intermediates have been evaluated as antimicrobials against Gram-negative and Gram-positive bacteria. No antimicrobial activity was observed fo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Belmessieri D,Gozlan C,Duclos MC,Dumitrescu O,Lina G,Redl A,Duguet N,Lemaire M

更新日期：2017-10-15 00:00:00

abstract：:Fluorination is a well-known strategy for improving the bioavailability of bioactive molecules in the lead optimization phase of drug discovery projects. In an attempt to improve the antitumor activity of camptothecins (CPTs), novel 10-fluoro-CPT derivatives were designed, synthesized and evaluated for cytotoxicity ag...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang CJ,Song ZL,Goto M,Hsu PL,Zhang XS,Yang QR,Liu YQ,Wang MJ,Morris-Natschke SL,Shang XF,Lee KH

更新日期：2017-10-15 00:00:00

abstract：:Compounds belonging to a carbazole series have been identified as potent fungal plasma membrane proton adenosine triphophatase (H+-ATPase) inhibitors with a broad spectrum of antifungal activity. The carbazole compounds inhibit the adenosine triphosphate (ATP) hydrolysis activity of the essential fungal H+-ATPase, the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Clausen JD,Kjellerup L,Cohrt KO,Hansen JB,Dalby-Brown W,Winther AL

更新日期：2017-10-01 00:00:00

abstract：:A series of 2-phenylpyrimidine coumarin derivatives with potential telomerase-inhibiting activity was designed and synthesized. All of the compounds were screened for antiproliferative activity against CNE2, KB, and Cal27 cell lines in vitro. The results showed that most of the derivatives had a favorable effect on re...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lv N,Sun M,Liu C,Li J

更新日期：2017-10-01 00:00:00

abstract：:A series of novel 1,3,4-oxadiazole/thiadiazole-chalcone conjugates were synthesized and their in vitro and in vivo antiviral activities were evaluated via microscale thermophoresis method and half-leaf method, respectively. The in vitro results indicated that compounds 7g, 7l, 8h, and 8l displayed good antiviral activ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gan X,Hu D,Chen Z,Wang Y,Song B

更新日期：2017-09-15 00:00:00

abstract：:A novel 6-aminopurine scaffold bearing an N9-cis-cyclobutyl moiety was designed using structure-based molecular design based on two known CDK inhibitors, dinaciclib and Cmpd-27. A series of novel 6-aminopurine compounds was prepared for structure-activity relationship (SAR) studies of CDK2 and CDK5 inhibitors. Among t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park SJ,Kim E,Yoo M,Lee JY,Park CH,Hwang JY,Ha JD

更新日期：2017-09-15 00:00:00

abstract：:Knoevenagel condensation was employed to generate a set of molecules potentially capable of inhibiting the RNA polymerase-σ70/σA interaction in bacteria. Synthesis was achieved via reactions between a variety of indole-7-carbaldehydes and rhodanine, N-allylrhodanine, barbituric acid or thiobarbituric acid. A library o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wenholz DS,Zeng M,Ma C,Mielczarek M,Yang X,Bhadbhade M,Black DSC,Lewis PJ,Griffith R,Kumar N

更新日期：2017-09-15 00:00:00

abstract：:The worldwide increase in antibiotic resistance has led to search of alternatives anti-microbial therapies such as photodynamic inactivation. The aim of this paper was to evaluate the photodynamic activity in vitro of a neutral and two cationic Zn phthalocyanines. Their photokilling activity was tested on Escherichia ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Miretti M,Clementi R,Tempesti TC,Baumgartner MT

更新日期：2017-09-15 00:00:00

abstract：:Novel 3-[4-(dimethylamino)phenyl]alkyl-2-oxindole analogs were synthesized by either of the following two pathways: (1) a sequence of Knoevenagel condensation of oxindole with (4-dimethylamino)cinnamaldehyde-hydrogenation, or (2) alkylation of oxindole dianion with [(4-dimethylamino)phenyl]alkyl halides. Subsequent al...

journal_title：Bioorganic & medicinal chemistry letters

authors： Furuta K,Kawai Y,Mizuno Y,Hattori Y,Koyama H,Hirata Y

更新日期：2017-09-15 00:00:00

abstract：:The selectivity and the binding affinity of previously reported carborane-containing ligands 2 and 3 toward ERβ remains to be optimized. To improve their biological profiles, a series of iodinated carboranyl phenol derivatives (4-6) were designed and synthesized as prospective ERβ-selective ligands with high affinity....

journal_title：Bioorganic & medicinal chemistry letters

authors： Ohta K,Ogawa T,Endo Y

更新日期：2017-09-01 00:00:00

abstract：:A series of macrocyclic factor XIa (FXIa) inhibitors was designed based on an analysis of the crystal structures of the acyclic phenylimidazole compounds. Further optimization using structure-based design led to inhibitors with pM affinity for FXIa, excellent selectivity against a panel of relevant serine proteases, a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang C,Corte JR,Rossi KA,Bozarth JM,Wu Y,Sheriff S,Myers JE Jr,Luettgen JM,Seiffert DA,Wexler RR,Quan ML

更新日期：2017-09-01 00:00:00

abstract：:A series of newer 1,2,4-triazole-3-thiol derivatives 5(a-m) and 6(a-i) containing a triazole fused with pyrazine moiety of pharmacological significance have been synthesized. All the synthesized compounds were screened for their in vitro antileishmanial and antioxidant activities. Compounds 5f (IC50=79.0µM) and 6f (IC...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patil SR,Asrondkar A,Patil V,Sangshetti JN,Kalam Khan FA,Damale MG,Patil RH,Bobade AS,Shinde DB

更新日期：2017-08-15 00:00:00

abstract：:A series of thirty-seven 1,3,5-triazine analogues have been synthesized, characterized and evaluated for their antiproliferative activity against a panel of four different human cancer cell lines such as HeLa, HepG2, A549 and MCF-7. Most of the 1,3,5-triazine analogues exhibited promising antiproliferative activity ag...

journal_title：Bioorganic & medicinal chemistry letters

authors： Narva S,Chitti S,Amaroju S,Bhattacharjee D,Rao BB,Jain N,Alvala M,Sekhar KVGC

更新日期：2017-08-15 00:00:00

abstract：:Oxidative-stress induces inflammatory diseases. Further, infections caused by drug-resistant microbial strains are on the rise. This necessitates the discovery of novel small-molecules for intervention therapy. A series of 3-(2,3-dichlorophenyl)-1-(aryl)prop-2-en-1-ones are synthesized as intermediates via Claisen-Sch...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lokeshwari DM,Achutha DK,Srinivasan B,Shivalingegowda N,Krishnappagowda LN,Kariyappa AK

更新日期：2017-08-15 00:00:00

abstract：:Inhibitors of CYP1 enzymes may play vital roles in the prevention of cancer and overcoming chemo-resistance to anticancer drugs. In this letter, we report synthesis of twenty-three pyrrole based heterocyclic chalcones which were screened for inhibition of CYP1 isoforms. Compound 3n potently inhibited CYP1B1 with an IC...

journal_title：Bioorganic & medicinal chemistry letters

authors： Williams IS,Joshi P,Gatchie L,Sharma M,Satti NK,Vishwakarma RA,Chaudhuri B,Bharate SB

更新日期：2017-08-15 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：:Resveratrol (Rsv) is widely reported to possess anticarcinogenic properties in a plethora of cellular and animal models having limited toxicity toward normal cells. In the molecular level, Rsv can act as a suppressive agent for several impaired signaling pathways on cancer cells. However, Fukuhara and Miyata have show...

journal_title：Bioorganic & medicinal chemistry letters

authors： Andrade Volkart P,Benedetti Gassen R,Mühlen Nogueira B,Nery Porto B,Eduardo Vargas J,Arigony Souto A

更新日期：2017-08-01 00:00:00

abstract：:We designed and synthesized novel δ opioid receptor (DOR) agonists 3a-i with an azatricyclodecane skeleton, which was a novel structural class of DOR agonists. Among them, 3b exhibited high values of binding affinity and potent agonistic activity for the DOR that were approximately equivalent to those of 2 which bore ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Watanabe Y,Hayashida K,Saito D,Takahashi T,Sakai J,Nakata E,Kanda T,Iwai T,Hirayama S,Fujii H,Yamakawa T,Nagase H

更新日期：2017-08-01 00:00:00

abstract：:Pradimicins are a group of antiviral and antifungal natural products from Actinomadura hibisca. Two putative O-methyltransferase genes, pdmF and pdmT, are present in the pradimicin biosynthetic gene cluster. However, there is only one methoxy group (11-OCH3) in pradimicins. Through heterologous expression and in vitro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu F,Napan K,Zhang S,Gladwin T,Takemoto J,Zhan J

更新日期：2017-08-01 00:00:00

abstract：:Continuing study of the ethyl acetate (EtOAc) extract of the cultured soft coral Sinularia brassica afforded five new withanolides, sinubrasolides H-L (1-5). The structures of the new compounds were elucidated on the basis of spectroscopic analysis. The cytotoxicities of new compounds 1-5 and a known compound sinubras...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang CY,Ahmed AF,Su JH,Sung PJ,Hwang TL,Chiang PL,Dai CF,Liaw CC,Sheu JH

更新日期：2017-08-01 00:00:00

abstract：:The vertebrate Cys-loop family of ligand-gated ion channels (LGICs) are comprised of nicotinic acetylcholine (nAChR), serotonin type 3 (5-HT3R), γ-aminobutyric acid (GABAAR), and glycine (GlyR) receptors. Here, we review efforts to discover selective small molecules targeting one or more Cys-loop receptors, with a foc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sparling BA,DiMauro EF

更新日期：2017-08-01 00:00:00

abstract：:Docking studies of 4-phenylthiazolinethione on human IDO1 suggest complexation of the heme iron by the exocyclic sulfur atom further reinforced by hydrophobic interactions of the phenyl ring within pocket A of the enzyme. On this basis, chemical modifications were proposed to increase inhibition activity. Synthetic ro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Balti M,Plas A,Meinguet C,Haufroid M,Thémans Q,Efrit ML,Wouters J,Lanners S

更新日期：2017-08-01 00:00:00

abstract：:A naphthyridine carbamate tetramer (NCT8) is a synthetic compound, which selectively binds to nucleic acids containing CGG/CGG sequence. Although NCT8 is a promising compound for a wide range of DNA and RNA based biotechnology such as modulation of specific gene expression, little is known about its behavior in human ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Matsumoto S,Iida K,Murata A,Denawa M,Hagiwara M,Nakatani K

更新日期：2017-08-01 00:00:00

abstract：:Sialidases are key virulence factors that remove sialic acid from host cell surface glycans, thus unmasking receptors to facilitate bacterial adherence and colonization. In this study, we report the isolation and characterization of novel inhibitors of the Streptococcus pneumoniae sialidases NanA, NanB, and NanC from ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park JY,Hwan Lim S,Ram Kim B,Jae Jeong H,Kwon HJ,Song GY,Bae Ryu Y,Song Lee W

更新日期：2017-07-15 00:00:00

abstract：:A series of potent dual JAK1/3 inhibitors have been developed from a moderately selective JAK3 inhibitor. Substitution at the C6 position of the pyrrolopyridazine core with aryl groups provided exceptional biochemical potency against JAK1 and JAK3 while maintaining good selectivity against JAK2 and Tyk2. Translation t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hynes J Jr,Wu H,Kempson J,Duan JJ,Lu Z,Jiang B,Stachura S,Tokarski JS,Sack JS,Khan JA,Lippy JS,Zhang RF,Pitt S,Shen G,Gillooly K,McIntyre K,Carter PH,Barrish JC,Nadler SG,Salter-Cid LM,Fura A,Schieven GL,Pitts

更新日期：2017-07-15 00:00:00

abstract：:In this study, we investigated the anti-inflammatory effects and mechanisms of cirsimaritin isolated from an ethanol extract of the aerial parts of Cirsium japonicum var. maackii Maxim. using RAW264.7 cells. The extract and its flavonoid cirsimaritin inhibited nitric oxide (NO) production and inducible nitric oxide sy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shin MS,Park JY,Lee J,Yoo HH,Hahm DH,Lee SC,Lee S,Hwang GS,Jung K,Kang KS

更新日期：2017-07-15 00:00:00

abstract：:We synthesized prodrug-type phosphotriester (PTE) oligonucleotides containing the six-membered cyclic disulfide moiety by using phosphoramidite chemistry. Prodrug-type oligonucleotides named "Reducing-Environment-Dependent Uncatalyzed Chemical Transforming (REDUCT) PTE oligonucleotides" were converted into natural oli...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hayashi J,Samezawa Y,Ochi Y,Wada SI,Urata H

更新日期：2017-07-15 00:00:00

abstract：:The investigation of the Vietnamese marine sponge Spongia sp. led to the isolation of three new sesquiterpene phenols, langconols A-C (1-3), and one new sesquiterpene hydroxyquinone, langcoquinone C (4), together with two known meroterpenoids (5 and 6). Their structures were determined on the basis of spectroscopic an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nguyen HM,Ito T,Kurimoto SI,Ogawa M,Win NN,Hung VQ,Nguyen HT,Kubota T,Kobayashi J,Morita H

更新日期：2017-07-15 00:00:00

abstract：:We designed and synthesized strobilurin analogues as hypoxia-inducible factor (HIF) inhibitors based on the molecular structure of kresoxim-methyl. Biological evaluation in human colorectal cancer HCT116 cells showed that most of the synthesized kresoxim-methyl analogues possessed moderate to potent inhibitory activit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee S,Kwon OS,Lee CS,Won M,Ban HS,Ra CS

更新日期：2017-07-01 00:00:00

abstract：:A phytochemical investigation into the bark of Erythrophleum fordii yielded four new compounds, two new cassaine diterpenoids (erythrofordin T and U, 1 and 2) and two new cassaine diterpenoid amines (erythroformine A and B, 6 and 7), as well as nine known compounds. We report for the first time the isolation of erythr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ha MT,Tran MH,Phuong TT,Kim JA,Woo MH,Choi JS,Lee S,Lee JH,Lee HK,Min BS

更新日期：2017-07-01 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