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你正在浏览BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献
  • Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).

    abstract：:Sustained proliferative capacity and gene dysregulation are hallmarks of cancer. In mammalian cells, cyclin-dependent kinases (CDKs) control critical cell cycle checkpoints and key transcriptional events in response to extracellular and intracellular signals leading to proliferation. Significant clinical activity for ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章,评审

    doi：10.1016/j.bmcl.2019.126637

    authors： Sánchez-Martínez C,Lallena MJ,Sanfeliciano SG,de Dios A

    更新日期：2019-10-15 00:00:00

  • Synthesis of new triazole fused imidazo[2,1-b]thiazole hybrids with emphasis on Staphylococcus aureus virulence factors.

    abstract：:A series of new triazole fused imidazo[2,1-b]thiazole hybrids (9a-u) were designed, synthesized and evaluated as antimicrobial agents. Compounds 9c, 9d, 9e, 9j and 9l showed promising broad spectrum antimicrobial activity. Further, compound 9c exhibited significant anti-biofilm activity with single and mixed biofilm d...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.08.025

    authors： Shareef MA,Sirisha K,Sayeed IB,Khan I,Ganapathi T,Akbar S,Ganesh Kumar C,Kamal A,Nagendra Babu B

    更新日期：2019-10-01 00:00:00

  • 19-Hydroxyeicosatetraenoic acid analogs: Antagonism of 20-hydroxyeicosatetraenoic acid-induced vascular sensitization and hypertension.

    abstract：:19-Hydroxyeicosatetraenoic acid (19-HETE, 1), a metabolically and chemically labile cytochrome P450 eicosanoid, has diverse biological activities including antagonism of the vasoconstrictor 20-hydroxyeicosatetraenoic acid (20-HETE, 2). A SAR study was conducted to develop robust analogs of 1 with improved in vitro and...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.08.020

    authors： Dakarapu R,Errabelli R,Manthati VL,Michael Adebesin A,Barma DK,Barma D,Garcia V,Zhang F,Laniado Schwartzman M,Falck JR

    更新日期：2019-10-01 00:00:00

  • Recent advances in natural antifungal flavonoids and their derivatives.

    abstract：:The resistance of pathogenic fungi and failure of drug therapy increased dramatically. Numerous studies have reported the individual or synergistic antifungal potency of natural and synthesized flavonoids, especially against drug-resistant fungi. This brief review summarizes the structure and individual or synergistic...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章,评审

    doi：10.1016/j.bmcl.2019.07.048

    authors： Jin YS

    更新日期：2019-10-01 00:00:00

  • Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker.

    abstract：:Two series of novel gemcitabine-nucleoside analogue dimers were synthesized using the 'click' chemistry approach. In the first series of dimers (21-30), the nucleoside units were connected with a stable methyltriazole 4N-3'(or 5')C linker whereas in the second series (31-40) with a cleavable ester-methyltriazole 4N-3'...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.08.003

    authors： Trznadel R,Singh A,Kleczewska N,Liberska J,Ruszkowski P,Celewicz L

    更新日期：2019-09-15 00:00:00

  • An investigation of targeted inhibition of transcription factor activity with pyrrole imidazole polyamide (PA) in chronic myeloid leukemia (CML) blast crisis cells.

    abstract：:Tyrosine kinase inhibitor (TKI) therapy is the standard treatment for chronic phase (CP)-chronic myeloid leukemia (CML), yet patients in blast crisis (BC) phase of CML are unlikely to respond to TKI therapy. The transcription factor E2F1 is a down-stream target of the tyrosine kinase BCR-ABL1 and is up-regulated in TK...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.07.049

    authors： Hayatigolkhatmi K,Padroni G,Su W,Fang L,Gómez-Castañeda E,Hsieh YC,Jackson L,Pellicano F,Burley GA,Jørgensen HG

    更新日期：2019-09-15 00:00:00

  • Targeting TRAIL.

    abstract：:Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL), also known as Apo2L, has been investigated in the past decade for its promising anticancer activity due to its ability to selectively induce apoptosis in tumoral cells by binding to TRAIL receptors (TRAIL-R). Macromolecules such as agonistic monoclonal a...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章,评审

    doi：10.1016/j.bmcl.2019.07.053

    authors： Ion GND,Nitulescu GM,Popescu CI

    更新日期：2019-09-15 00:00:00

  • Synthesis and evaluation of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives as Mnk inhibitors.

    abstract：:Post-translational modulation of eIF4E through phosphorylation by Mnks is highly integral to the pathogenesis of different cancers. Therefore, inhibition of Mnks offers a strategy for cancer treatment. Herein, a series of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives is presented as Mnk in...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.07.043

    authors： Abdelaziz AM,Basnet SKC,Islam S,Li M,Tadesse S,Albrecht H,Gerber C,Yu M,Wang S

    更新日期：2019-09-15 00:00:00

  • Synthesis of N-arylindazole-3-carboxamide and N-benzoylindazole derivatives and their evaluation against α-MSH-stimulated melanogenesis.

    abstract：:We have designed and synthesized twenty-six N-arylindazole-3-carboxamide (3a-p) and N-benzoylindazole (6a-j) derivatives to discover with excellent inhibition activities of α-MSH-stimulated melanogenesis. In the bio evaluation studies of these compounds, we discovered eighteen compounds, out of twenty-six exhibited mo...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.07.055

    authors： Arepalli SK,Lee C,Jung JK,Kim Y,Lee K,Lee H

    更新日期：2019-09-15 00:00:00

  • Essential structure of orexin 1 receptor antagonist YNT-707, Part IV: The role of D-ring in 4,5-epoxymorphinan on the orexin 1 receptor antagonistic activity.

    abstract：:The orexin 1 receptor (OX1R) antagonists carrying a morphinan skeleton such as YNT-707 (2) and YNT-1310 (3) showed potent and extremely high selective antagonistic activity against OX1R. In the course of our study of the essential structure of YNT-707 for high binding affinity against OX1R, we prepared derivatives of ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.07.039

    authors： Saitoh T,Seki K,Nakajima R,Yamamoto N,Kutsumura N,Nagumo Y,Irukayama-Tomobe Y,Ogawa Y,Ishikawa Y,Tanimura R,Yanagisawa M,Nagase H

    更新日期：2019-09-15 00:00:00

  • Synthesis of novel benzothiazole amides: Evaluation of PPAR activity and anti-proliferative effects in paraganglioma, pancreatic and colorectal cancer cell lines.

    abstract：:The reduced activation of PPARs has a positive impact on cancer cell growth and viability in multiple preclinical tumor models, suggesting a new therapeutic potential for PPAR antagonists. In the present study, the benzothiazole amides 2a-g were synthesized and their activities on PPARs were investigated. Transactivat...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.06.020

    authors： Ammazzalorso A,De Lellis L,Florio R,Laghezza A,De Filippis B,Fantacuzzi M,Giampietro L,Maccallini C,Tortorella P,Veschi S,Loiodice F,Cama A,Amoroso R

    更新日期：2019-08-15 00:00:00

  • Inhibition of neutral lipid synthesis by avarols from a marine sponge.

    abstract：:The effects of 14 sesquiterpene hydroquinones, including 8 marine sponge-derived avarols (1-8) and 6 semisynthetic derivatives (9-14), on lipid droplet accumulation and neutral lipid synthesis in Chinese hamster ovary (CHO) K1 cells were investigated. In intact CHO-K1 cell assays, avarol (1) markedly decreased the num...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.06.026

    authors： Ohshiro T,Kobayashi K,Suzuki A,Yamazaki H,Uchida R,Namikoshi M,Tomoda H

    更新日期：2019-08-15 00:00:00

  • In vitro selection of a 3' terminal short protector that stabilizes transcripts to improve the translation efficiency in a wheat germ extract.

    abstract：:Wheat cell-free expression systems based on wheat germ extract (WGE) enable us to briefly synthesize various types of proteins in vitro merely by exogenously adding their mRNA templates. Moreover, it is possible to produce larger amounts of protein by thoroughly removing the endosperm, which contains many translation ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 信件

    doi：10.1016/j.bmcl.2019.06.058

    authors： Ogawa A,Kutsuna A,Takamatsu M,Okuzono T

    更新日期：2019-08-15 00:00:00

  • Bioactive triterpene glycosides from the fruit of Stauntonia hexaphylla and insights into the molecular mechanism of its inflammatory effects.

    abstract：:Chromatography of the ethanol extract of the medicinal fruit Stauntonia hexaphylla resulted in the purification of 26 compounds (1-26), including two undescribed triterpene saponins 1 and 2 (hexaphylosides A and B). Their structures were confirmed by spectroscopic data, including IR, HR QTOF MS, 1H, 13C NMR, COSY, HMQ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.07.010

    authors： Ba Vinh L,Jang HJ,Viet Phong N,Dan G,Won Cho K,Ho Kim Y,Young Yang S

    更新日期：2019-08-15 00:00:00

  • 2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.

    abstract：:Imidazoline-based small molecule inhibitors of p53-MDM2 interaction intended for the treatment of p53 wild-type tumors are the promising structures for design of anticancer drugs. Based on fragment approach we have investigated a key role of substituents in cis-imidazoline core for biological activity of nutlin family...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.06.007

    authors： Bazanov DR,Pervushin NV,Savitskaya VY,Anikina LV,Proskurnina MV,Lozinskaya NA,Kopeina GS

    更新日期：2019-08-15 00:00:00

  • Dual functional cholinesterase and PDE4D inhibitors for the treatment of Alzheimer's disease: Design, synthesis and evaluation of tacrine-pyrazolo[3,4-b]pyridine hybrids.

    abstract：:A series of tacrine-pyrazolo[3,4-b]pyridine hybrids were synthesised and evaluated as dual cholinesterase (ChE) and phosphodiesterase 4D (PDE4D) inhibitors for the treatment of Alzheimer's disease (AD). Compound 10j, which is tacrine linked with pyrazolo[3,4-b]pyridine moiety by a six-carbon spacer, was the most poten...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 信件

    doi：10.1016/j.bmcl.2019.06.056

    authors： Pan T,Xie S,Zhou Y,Hu J,Luo H,Li X,Huang L

    更新日期：2019-08-15 00:00:00

  • Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.

    abstract：:Bromodomain-containing protein 4 (BRD4) is a new therapeutic target for the treatment of diseases including cardiovascular diseases, cancer, inflammation and central nervous system (CNS) disorders. In this study, we introduced the pharmacophore of fibrates to a BRD4 inhibitor, RVX-208, to design dual-active hypolipide...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 信件

    doi：10.1016/j.bmcl.2019.06.028

    authors： Yu P,Liu W,Ren J,Wang Y,Ning Y,Huang M,Hu X,Wei L,Ji M,Cai J

    更新日期：2019-08-15 00:00:00

  • Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.

    abstract：:The TAIRE family of kinases are an understudied branch of the CDK kinase family, that have been implicated in a number of cancers. This manuscript describes the design, synthesis and SAR of covalent CDK14 inhibitors, culminating in identification of FMF-04-159-2, a potent, covalent CDK14 inhibitor with a TAIRE kinase ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.05.024

    authors： Ferguson FM,Doctor ZM,Ficarro SB,Marto JA,Kim ND,Sim T,Gray NS

    更新日期：2019-08-01 00:00:00

  • Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.

    abstract：:A low level of high density lipoprotein (HDL) is an independent risk factor for cardiovascular disease. HDL reduces inflammation and plays a central role in reverse cholesterol transport, where cholesterol is removed from peripheral tissues and atherosclerotic plaque. One approach to increase plasma HDL is through inh...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.05.048

    authors： Kim SH,Johnson JA,Jiang J,Parkhurst B,Phillips M,Pi Z,Qiao JX,Tora G,Ye Chen A,Liu E,Yin X,Yang R,Zhao L,Taylor DS,Basso M,Behnia K,Onorato J,Chen XQ,Abell LM,Lu H,Locke G,Caporuscio C,Adam LP,Gordon D,Wex

    更新日期：2019-08-01 00:00:00

  • Folic acid conjugates of a bleomycin mimic for selective targeting of folate receptor positive cancer cells.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.05.047

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

    更新日期：2019-08-01 00:00:00

  • Synthesis and comparison of substituted 1,2,3-dithiazole and 1,2,3-thiaselenazole as inhibitors of the feline immunodeficiency virus (FIV) nucleocapsid protein as a model for HIV infection.

    abstract：:We report the first biological evaluation the 1,2,3-thiaselenazole class of compound and utilising a concise synthetic approach of sulfur extrusion, selenium insertion of the 1,2,3-dithiazoles. We created a small diverse library of compounds to contrast the two ring systems. This approach has highlighted new structure...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.05.016

    authors： Asquith CRM,Meili T,Laitinen T,Baranovsky IV,Konstantinova LS,Poso A,Rakitin OA,Hofmann-Lehmann R

    更新日期：2019-07-15 00:00:00

  • Dual-targeting GroEL/ES chaperonin and protein tyrosine phosphatase B (PtpB) inhibitors: A polypharmacology strategy for treating Mycobacterium tuberculosis infections.

    abstract：:Current treatments for Mycobacterium tuberculosis infections require long and complicated regimens that can lead to patient non-compliance, increasing incidences of antibiotic-resistant strains, and lack of efficacy against latent stages of disease. Thus, new therapeutics are needed to improve tuberculosis standard of...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.04.034

    authors： Washburn A,Abdeen S,Ovechkina Y,Ray AM,Stevens M,Chitre S,Sivinski J,Park Y,Johnson J,Hoang QQ,Chapman E,Parish T,Johnson SM

    更新日期：2019-07-01 00:00:00

  • A new lateral root growth inhibitor from the sponge-derived fungus Aspergillus sp. LS45.

    abstract：:Two new γ-lactones, aspergilactones A (1) and B (2), were discovered along with two known compounds, annularin A (3) and pericoterpenoid A (4), from a culture of the sponge-associated fungus Aspergillus sp. LS45. The planar structures of 1-4 were characterized using comprehensive spectroscopic methods and comparison w...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.04.051

    authors： Huang L,Ding L,Li X,Wang N,Yan Y,Yang M,Cui W,Benjamin Naman C,Cheng K,Zhang W,Zhang B,Jin H,He S

    更新日期：2019-07-01 00:00:00

  • Synthesis, fungicidal activity and SAR of 3,4-dichloroisothiazole-based cycloalkylsulfonamides.

    abstract：:To develop more valuable and effective fungicide candidates, a novel series of 3,4-dichloroisothioxazole-based cycloalkylsulfonamides were synthesized and their structures were identified by 1H NMR, 13C NMR, MS and elemental analysis. Compound 3k was further confirmed by X-ray single crystal diffraction. The in vitro ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.03.047

    authors： Zhang Y,Wang M,Ahmed M,He L,Ji M,Qi Z,Li X

    更新日期：2019-06-01 00:00:00

  • Benzothiophene derivatives as phosphodiesterase 10A (PDE10A) inhibitors: Hit-to-lead studies.

    abstract：:A novel series of benzothiophene derivatives was discovered as phosphodiesterase 10A (PDE10A) inhibitors. Structure-activity relationship studies on high-throughput screening hit compound 1 led to the identification of 7-acetyl-3-methyl-N-(quinolin-2-yl)-1-benzothiophene-2-carboxamide (16), with potent inhibitory acti...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.03.021

    authors： Kawamoto Y,Tomino M,Hiramatsu K,Oyama Y,Hayashi Y

    更新日期：2019-06-01 00:00:00

  • Discovery of niclosamide and its O-alkylamino-tethered derivatives as potent antibacterial agents against carbapenemase-producing and/or colistin resistant Enterobacteriaceae isolates.

    abstract：:Carbapenemase-producing Enterobacteriaceae (CPE) represents the most worrisome evolution of the antibiotic resistance crisis, which is almost resistant to most of available antibiotics. This situation is getting even worse particularly due to the recent emergence of colistin resistance. Herein, niclosamide, an FDA-app...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.03.032

    authors： Xu J,Pachón-Ibáñez ME,Cebrero-Cangueiro T,Chen H,Sánchez-Céspedes J,Zhou J

    更新日期：2019-06-01 00:00:00

  • Radiosynthesis of a carbon-11-labeled AMPAR allosteric modulator as a new PET radioligand candidate for imaging of Alzheimer's disease.

    abstract：:To develop PET tracers for imaging of Alzheimer's disease, a new carbon-11-labeled AMPAR allosteric modulator 4-cyclopropyl-7-(3-[11C]methoxyphenoxy)-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide ([11C]8) has been synthesized. The reference standard 4-cyclopropyl-7-(3-methoxyphenoxy)-3,4-dihydro-2H-benzo[e][1,...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.03.027

    authors： Miao C,Dong F,Jia L,Li W,Wang M,Zheng QH,Xu Z

    更新日期：2019-05-15 00:00:00

  • Bioactivity-guided identification of flavonoids with cholinesterase and β-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.

    abstract：:Millettia pachycarpa Benth, a widely used anthelminthic drug in folk, is rich in flavonoids with various bioactivities. This study aimed to identify active flavonoids with anti-Alzheimer's disease (AD) effect from its seeds by a bioassay-guided isolation. A novel rotenoid with unusual oxidative ring-opening skeleton (...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.03.024

    authors： Tu Y,Wu C,Kang Y,Li Q,Zhu C,Li Y

    更新日期：2019-05-15 00:00:00

  • Potassium channel blocking 1,2-bis(aryl)ethane-1,2-diamines active as antiarrhythmic agents.

    abstract：:Atrial fibrillation (AF) is a major cause of stroke, heart failure, sudden death and cardiovascular morbidity. The Kv1.5 potassium channel conducts the IKur current and has been demonstrated to be predominantly expressed in atrial versus ventricular tissue. Blockade of Kv1.5 has been proven to be an effective approach...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.03.006

    authors： Kajanus J,Antonsson T,Carlsson L,Jurva U,Pettersen A,Sundell J,Inghardt T

    更新日期：2019-05-15 00:00:00

  • Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study.

    abstract：:Amide- and ester-linked kinase inhibitor-cytotoxin conjugates were rationally designed and synthesised as prototype hypoxia-activated anticancer mutual prodrugs. Chemical reduction of an aryl nitro trigger moiety was shown to initiate a spontaneous cyclisation/fragmentation reaction that simultaneously released the ki...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.03.015

    authors： Sansom GN,Kirk NS,Guise CP,Anderson RF,Smaill JB,Patterson AV,Kelso MJ

    更新日期：2019-05-15 00:00:00

  • Structure-based design, synthesis and biological evaluation of a novel series of isoquinolone and pyrazolo[4,3-c]pyridine inhibitors of fascin 1 as potential anti-metastatic agents.

    abstract：:Fascin is an actin binding and bundling protein that is not expressed in normal epithelial tissues but overexpressed in a variety of invasive epithelial tumors. It has a critical role in cancer cell metastasis by promoting cell migration and invasion. Here we report the crystal structures of fascin in complex with a s...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.01.035

    authors： Francis S,Croft D,Schüttelkopf AW,Parry C,Pugliese A,Cameron K,Claydon S,Drysdale M,Gardner C,Gohlke A,Goodwin G,Gray CH,Konczal J,McDonald L,Mezna M,Pannifer A,Paul NR,Machesky L,McKinnon H,Bower J

    更新日期：2019-04-15 00:00:00

  • Discovery of a small molecule RXFP3/4 agonist that increases food intake in rats upon acute central administration.

    abstract：:The relaxin family peptide receptors have been implicated in numerous physiological processes including energy homeostasis, cardiac function, wound healing, and reproductive function. Two family members, RXFP3 and RXFP4, are class A GPCRs with endogenous peptide ligands (relaxin-3 and insulin-like peptide 5 (INSL5), r...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.02.013

    authors： DeChristopher B,Park SH,Vong L,Bamford D,Cho HH,Duvadie R,Fedolak A,Hogan C,Honda T,Pandey P,Rozhitskaya O,Su L,Tomlinson E,Wallace I

    更新日期：2019-04-15 00:00:00

  • Biotinylated-spiperone ligands for quantum dot labeling of the dopamine D2 receptor in live cell cultures.

    abstract：:We have synthesized 3 analogs of the dopamine D2 receptor (D2 DR) antagonist spiperone that can be conjugated to streptavidin-coated quantum dots via a pegylated biotin derivative. Using fluorescent imaging we demonstrate that substitution on the spiro position is tolerated, whilst the length and rigidity of a spacer ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.02.024

    authors： Tomlinson ID,Kovtun O,Crescentini TM,Rosenthal SJ

    更新日期：2019-04-15 00:00:00

  • Discovery of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridines as potent anaplastic lymphoma kinase (ALK) inhibitors.

    abstract：:A new series of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridine compounds have been discovered as potent anaplastic lymphoma kinase (ALK) inhibitors. The 4-hydroxyphenyl in the 6-position of 1H-pyrazolo[3,4-b]pyridine were crucial and a fluorine atom substitution could give promising inhibitory activity. The IC50 of compound 9v...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.01.037

    authors： Chen C,Pan P,Deng Z,Wang D,Wu Q,Xu L,Hou T,Cui S

    更新日期：2019-04-01 00:00:00

  • Synthesis and anti-tumor activity study of water-soluble PEG-celastrol coupling derivatives as self-assembled nanoparticles.

    abstract：:To improve the drug-ability of celastrol, a series of PEGylation celastrol (PEGC) were designed and synthesized by conjugation with different kinds of polyethylene glycols (PEGs) with celastrol. Most of PEGCs could easily dissolve in water. In particular, one of them (DC1000) could be dispersed in water to form nanopa...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.01.042

    authors： Shan WG,Wang HG,Wu R,Zhan ZJ,Ma LF

    更新日期：2019-03-01 00:00:00

  • Synthesis of the reported structure of homocereulide and its vacuolation assay.

    abstract：:Homocereulide, isolated from marine bacterium Bacillus cereus, is an analog of emetic toxin cereulide. There is no report on its structure determination and involvement in B. cereus-associated food poisoning. Homocereulide is a cyclic dodecadepsipeptide composed of l-O-Val-l-Val-d-O-Leu-d-Ala and l-O-allo-Ile-d-Val-d-...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.01.007

    authors： Naka T,Hattori Y,Takenaka H,Ohta Y,Kirihata M,Tanimori S

    更新日期：2019-03-01 00:00:00

  • Discovery of novel pan-genotypic HCV NS5A inhibitors containing a novel tetracyclic core.

    abstract：:A series of novel tetracyclic core-containing HCV NS5A inhibitors has been discovered. Incorporation of tetrahydropyran-substituted amino acid moiety improved their potency and yielded HCV NS5A inhibitors with a minimum potency shift from the GT1a strain compared to other genotypes and mutants. Compounds 53 and 54 sho...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.01.031

    authors： Yu W,Hu B,Zhong B,Hao J,Lei Z,Agrawal S,Rokosz L,Liu R,Chen S,Asante-Appiah E,Kozlowski JA

    更新日期：2019-03-01 00:00:00

  • Advances in Lead Generation.

    abstract：:Lead Generation represents a critical drug discovery phase where chemical starting points and their respective mechanism of action, quality, and potential liabilities are largely predefined. Recent advances such as DNA-encoded libraries or fragment-, chemical biology-, and virtual screening-based approaches are today ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章,评审

    doi：10.1016/j.bmcl.2018.12.001

    authors： Holenz J,Stoy P

    更新日期：2019-02-15 00:00:00

  • Lead generation and optimization of novel GPR119 agonists with a spirocyclic cyclohexane structure.

    abstract：:We describe here the generation of a lead compound and its optimization studies that led to the identification of a novel GPR119 agonist. Based on a spirocyclic cyclohexane structure reported in our previous work, we identified compound 8 as a lead compound, being guided by ligand-lipophilicity efficiency (LLE), which...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2018.12.041

    authors： Harada K,Mizukami J,Watanabe T,Mori G,Ubukata M,Suwa K,Fukuda S,Negoro T,Sato M,Inaba T

    更新日期：2019-02-01 00:00:00

  • Synthesis and biological evaluation of clovamide analogues with catechol functionality as potent Parkinson's disease agents in vitro and in vivo.

    abstract：: ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2018.11.030

    authors： Feng JH,Hu XL,Lv XY,Wang BL,Lin J,Zhang XQ,Ye WC,Xiong F,Wang H

    更新日期：2019-01-15 00:00:00

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