FR131535, a novel water-soluble echinocandin-like lipopeptide: synthesis and biological properties.

abstract：:Phosphopeptide prodrugs bearing two S-acyl-2-thioethyl (SATE) biolabile phosphate protections were developed. They are capable to inhibit the Shc/Grb2 interaction and MAP kinases (ERK1 and ERK2) phosphorylation in cellular assay. The S-acetyl-2-thioethyl (MeSATE) analogue showed an IC50 of 1 microM in the inhibition o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu WQ,Vidal M,Mathé C,Périgaud C,Garbay C

更新日期：2000-04-03 00:00:00

abstract：:The human epidermal growth factor receptor (EGFR) family is known to be involved in cell signaling pathways. The extracellular domain of EGFR consists of four domains, of which domain II and domain IV are known to be involved in the dimerization process. Overexpression of these receptors is known to play a significant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Naik H,Gauthier T,Singh S,Jois S

更新日期：2018-12-01 00:00:00

abstract：:The catalytic subunit of the Ser/Thr protein phosphatase 1 (PP1cat) hydrolyses N-acetyl Arg-Arg-Ala-phosphoThr-Val-Ala (K(M) = 3.7 mM) in a reaction that is inhibited competitively by inorganic phosphate (Pi, Ki = 1.6 mM) but unaffected by the product peptide alcohol at concentrations up to 3 mM. The enzyme does not c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sanvoisin J,Gani D

更新日期：2001-02-26 00:00:00

abstract：:Based on the structures of aminopyridine thrombin inhibitors (1), a series of aminoalkyl- and guanidinoalkyl-substituted diarylsulfonamides were prepared. The most potent derivative, N-[3-(4-guanidinobutoxy)-5-methyl-phenyl]-benzenesulfonamide (6c) had Ki = 0.18 microM for thrombin and did not inhibit trypsin, plasmin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Weber IR,Neidlein R,von der Saal W,Grams F,Leinert H,Strein K,Engh RA,Kucznierz R

更新日期：1998-07-07 00:00:00

abstract：:The synthesis and biological activities of a series of new 1beta-methylcarbapenems 1a-h having heteroaromatic thioether moiety at C-5 position of pyrrolidine were described. Among these compounds, 1,2,3-thiadiazole derivative 1h showed the most potent antibacterial activity and advanced pharmacokinetics in comparison ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shin KJ,Koo KD,Yoo KH,Kang YK,Park SW,Kim DJ

更新日期：2001-09-03 00:00:00

abstract：:A series of 3,4-dihydroquinazoline derivatives consisting of the selected compounds from our chemical library on the diversity basis and the new synthetic compounds were in vitro tested for their inhibitory activities for both acetylcholinesterase (AChE, from electric eel) and butyrylcholinesterase (BChE, from equine ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park B,Nam JH,Kim JH,Kim HJ,Onnis V,Balboni G,Lee KT,Park JH,Catto M,Carotti A,Lee JY

更新日期：2017-03-01 00:00:00

abstract：:A series of sixteen β-carbolines, bearing chalcone moiety at C-1 position, were prepared from easily accessible 1-acetyl-β-carboline and various aldehydes under basic conditions followed by N2-alkylation using different alkyl bromides. The prepared compounds were evaluated for in vitro cytotoxicity against a panel of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Venkataramana Reddy PO,Hridhay M,Nikhil K,Khan S,Jha PN,Shah K,Kumar D

更新日期：2018-05-01 00:00:00

abstract：:We report here the synthesis and biological evaluation of a series of 37 compounds as precursors of potent antimalarial bis-thiazolium salts (T3 and T4). These prodrugs were either thioester, thiocarbonate or thiocarbamate type and were synthesized in one step by reaction of an alkaline solution of the parent drug wit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Caldarelli SA,Boisbrun M,Alarcon K,Hamzé A,Ouattara M,Salom-Roig X,Maynadier M,Wein S,Peyrottes S,Pellet A,Calas M,Vial H

更新日期：2010-07-01 00:00:00

abstract：:The induction of conformationally restricted N-(aryl or heteroaryl)-3-azabicyclo[3.1.0]hexane derivatives at P(2) region of compounds of 2-cyanopyrrolidine class was explored to develop novel DPP-IV inhibitors. The synthesis, structure-activity relationship, and selectivity against related proteases are delineated. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sattigeri JA,Andappan MM,Kishore K,Thangathirupathy S,Sundaram S,Singh S,Sharma S,Davis JA,Chugh A,Bansal VS

更新日期：2008-07-15 00:00:00

abstract：:A test series of 32 phenylpiperazines III with affinity for 5-HT1A and alpha1 receptors was subjected to QSAR analysis using artificial neural networks (ANNs), in order to get insight into the structural requirements that are responsible for 5-HT1A/alpha1 selectivity. Good models and predictive power were obtained for...

journal_title：Bioorganic & medicinal chemistry letters

authors： López-Rodríguez ML,Morcillo MJ,Fernández E,Rosado ML,Orensanz L,Beneytez ME,Manzanares J,Fuentes JA,Schaper KJ

更新日期：1999-06-21 00:00:00

abstract：:The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis of a series of substituted 4-[2-amino-1,3-thiazolyl]-thiophene-2-carboxamidines is described. Further optimization of this series by substitution of the termina...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wilson KJ,Illig CR,Subasinghe N,Hoffman JB,Rudolph MJ,Soll R,Molloy CJ,Bone R,Green D,Randall T,Zhang M,Lewandowski FA,Zhou Z,Sharp C,Maguire D,Grasberger B,DesJarlais RL,Spurlino J

更新日期：2001-04-09 00:00:00

abstract：:Crambescin B carboxylic acid, a synthetic analog of crambescin B, was recently found to inhibit the voltage-sensitive sodium channels (VSSC) in a cell-based assay using neuroblastoma Neuro 2A cells. In the present study, whole-cell patch-clamp recordings were conducted with three heterologously expressed VSSC subtypes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tsukamoto T,Chiba Y,Nakazaki A,Ishikawa Y,Nakane Y,Cho Y,Yotsu-Yamashita M,Nishikawa T,Wakamori M,Konoki K

更新日期：2017-03-01 00:00:00

abstract：:A group of sixteen iridoids isolated from plants used as anti-inflammatory remedies in Mexican folk medicine were evaluated for their potential to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes. From these assays, loganic acid (10) was identified as the most promising compound with both COX-1 (3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ramírez-Cisneros MÁ,Rios MY,Aguilar-Guadarrama AB,Rao PP,Aburto-Amar R,Rodríguez-López V

更新日期：2015-10-15 00:00:00

abstract：:The effects of PEGylation of glucose-dependent insulinotropic polypeptide (GIP) on potency and dipeptidyl peptidase IV (DPPIV) stability are reported. N-terminal modification of GIP(1-30) with 40 kDa polyethylene glycol (PEG) abrogates functional activity. In contrast, C-terminal PEGylation of GIP(1-30) maintains full...

journal_title：Bioorganic & medicinal chemistry letters

authors： Salhanick AI,Clairmont KB,Buckholz TM,Pellegrino CM,Ha S,Lumb KJ

更新日期：2005-09-15 00:00:00

abstract：:Lipase-catalyzed acylation of Guanfu alcohol-amine (GFAA) with vinyl acetate (VA) was performed in non-aqueous system for the preparation of Guanfu base G (GFG), a plant-originated alkaloid with significant antiarrhythmic activity. Among the eight lipases from different origins, Novozym 435 was found to be the best bi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xia Y,Liu JH,Liu JH,Yu BY

更新日期：2012-05-01 00:00:00

abstract：:Modifications at C6 and C7 positions of 3-cyanoquinolines 6 and 7 led to potent inhibitors of the ErbB family of kinases particularly against EGFRWT and Her4 enzymes in the radioisotope filter binding assay. The lead (4, SAB402) displayed potent dual biochemical activities with EGFRWT/Her4 IC50 ratio of 80 due to its ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mansour TS,Pallepati RR,Basetti V

更新日期：2020-08-15 00:00:00

abstract：:Cancer cells isolated from two patients with malignant non-Hodgkin B-cell lymphomas that became resistant to chemotherapy during clinical treatment were made ≥fourfold resistant in culture to anticancer drugs, that is cisplatin, etoposide, methotrexate and bortezomib. Because most resistant lines showed significantly ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Schulz R,Emmrich T,Lemmerhirt H,Leffler U,Sydow K,Hirt C,Kiefer T,Link A,Bednarski PJ

更新日期：2012-11-01 00:00:00

abstract：:Novel CCR2 antagonists with a novel 2-aminooctahydrocyclopentalene-3a-carboxamide scaffold were designed. SAR studies led to a series of potent compounds. For example, compound 51 had a good PK profile in both dog and monkey, and exhibited excellent efficacy when dosed orally in an inflammation model in hCCR2 KI mice....

journal_title：Bioorganic & medicinal chemistry letters

authors： Cai C,Kang FA,Hou C,O'Neill JC,Opas E,McKenney S,Johnson D,Sui Z

更新日期：2013-01-01 00:00:00

abstract：:The 18-deoxy derivative (3) of a simplified analogue (1) of aplysiatoxin with antiproliferative activity was synthesized to examine the role of the phenolic hydroxyl group at position 18 in the biological activities of 1. Compound 3 as well as 1 showed significant affinity for protein kinase Cδ (PKCδ), and the antipro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yanagita RC,Kamachi H,Tanaka K,Murakami A,Nakagawa Y,Tokuda H,Nagai H,Irie K

更新日期：2010-10-15 00:00:00

abstract：:A new near-infrared fluorescent compound containing two cyclic RGD motifs, cypate-[c(RGDfK)](2) (1), was synthesized based on a carbocyanine fluorophore bearing two carboxylic acid groups (cypate) for integrin α(v)β(3)-targeting. Compared with its monovalent counterpart cypate-c(RGDfK) (2), 1 exhibited remarkable impr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ye Y,Akers W,Xu B,Bloch S,Odonkor C,Achilefu S

更新日期：2012-09-01 00:00:00

abstract：:In this study, we synthesized an Azo-py phosphoramidite, featuring azobenzene and pyrene units, as a novel fluorescent and isomeric (trans- and cis-azobenzene units) material, which we incorporated in an i-motif DNA sequence. We then monitored the structural dynamics and changes in fluorescence as the modified DNA seq...

journal_title：Bioorganic & medicinal chemistry letters

authors： Joo HN,Van Thi Nguyen T,Chae HK,Seo YJ

更新日期：2017-06-01 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：:We have discovered that phenyltriazolinone is a novel and potent P1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has reoriented resulting in a novel S1 binding pocket which is larger in size to accommodate the p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Quan ML,Pinto DJ,Rossi KA,Sheriff S,Alexander RS,Amparo E,Kish K,Knabb RM,Luettgen JM,Morin P,Smallwood A,Woerner FJ,Wexler RR

更新日期：2010-02-15 00:00:00

abstract：:Bioassay-guided separation of the extract of the medicinal plant, Puerariae Flos, disclosed the two isoflavones tectorigenin (1) and genistein (2) as the inhibitors for expression of IgE receptor (FcepsilonRI), the key molecule triggering the allergic reactions, on human mast cells. As a result of analysis of structur...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tamura S,Yoshihira K,Tokumaru M,Zisheng X,Murakami N

更新日期：2010-07-01 00:00:00

abstract：:Microsomal prostaglandin E(2) synthase-1 (mPGES-1) is a novel therapeutic target for the treatment of inflammation and pain. In the preceding letter, we detailed the discovery of clinical candidate PF-04693627, a potent mPGES-1 inhibitor possessing a novel benzoxazole structure. While PF-04693627 was undergoing furthe...

journal_title：Bioorganic & medicinal chemistry letters

authors： Walker DP,Arhancet GB,Lu HF,Heasley SE,Metz S,Kablaoui NM,Franco FM,Hanau CE,Scholten JA,Springer JR,Fobian YM,Carter JS,Xing L,Yang S,Shaffer AF,Jerome GM,Baratta MT,Moore WM,Vazquez ML

更新日期：2013-02-15 00:00:00

abstract：:After the widespread use of the acyclic purine nucleoside analogues for therapy of herpes simplex virus (HSV) infection since the 1980s, new antiviral strategies are urgently needed to counter the emergence of drug-resistant clinical isolates. In this report, we define the anti-HSV efficacies of three optimized 2-amin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiang YF,Qian CW,Xing GW,Hao J,Xia M,Wang YF

更新日期：2012-07-15 00:00:00

abstract：:We report herein the synthesis and stereochemical structure-activity relationships of novel morpholine analogues 12 and 13 with regards to NK1, NK2 and NK3 tachykinin receptor binding affinity. An essential requirement for more potent binding affinities was controlled by absolute configuration. (S,R)-12 and (S,R)-13 e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nishi T,Ishibashi K,Takemoto T,Nakajima K,Fukazawa T,Iio Y,Itoh K,Mukaiyama O,Yamaguchi T

更新日期：2000-08-07 00:00:00

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

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

abstract：:Different types of heterogenized catalysts were involved in asymmetric reactions. Hydrogen transfer reduction was performed with amino alcohols derived from poly((S)-(GMA-co-EGDMA or DVB)) and hydrogenation with BINAP grafted onto PEG or copolymerized with isocyanates as ligands. Attempts of catalysts recycling are re...

journal_title：Bioorganic & medicinal chemistry letters

authors： Saluzzo C,Lamouille T,Hérault D,Lemaire M

更新日期：2002-07-22 00:00:00

abstract：:In this letter, we report our efforts to design, synthesize and evaluate biological activities of a series of novel hybridized compounds containing 1-tetrazole and 4-pyridinyl-1,2,4-triazole-3-one. An analysis of structure-activity data indicates that the target compounds with bulky and hydrophobic side chains exhibit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qian A,Zheng Y,Wang R,Wei J,Cui Y,Cao X,Yang Y

更新日期：2018-02-01 00:00:00