Design and synthesis of novel substituted quinazoline derivatives as antileishmanial agents.

abstract：:Four new lignans, strebluslignanol F (1), (7'R,8'S,7″R,8″S)-erythro-strebluslignanol G (2), isomagnaldehyde (3) and isostrebluslignanaldehyde (4), along with 12 known lignans (5-16) were isolated from the ethyl acetate-soluble part of MeOH extract of the root of Streblus asper. Their structures were elucidated through...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li J,Meng AP,Guan XL,Li J,Wu Q,Deng SP,Su XJ,Yang RY

更新日期：2013-04-01 00:00:00

abstract：:Three novel inosine-based dinuclear platinum complexes have been synthesized via a solid-phase strategy. In these compounds, the metal is linked both to the N-7 of the purine nucleus and to the terminal amine group of a hexylamine side chain installed on N-1. Cis- or trans- diamine as well as ethylenediamine ligands a...

journal_title：Bioorganic & medicinal chemistry letters

authors： D'Errico S,Oliviero G,Piccialli V,Amato J,Borbone N,D'Atri V,D'Alessio F,Di Noto R,Ruffo F,Salvatore F,Piccialli G

更新日期：2011-10-01 00:00:00

abstract：:Oxidation of 4-methylcatechol previously exposed to aqueous calcium chloride was shown by ion chromatography to be associated with release of calcium ions. The catechol was oxidised to the corresponding orthoquinone by the use of tyrosinase from Agaricus bisporus. The oxidative release of calcium from the catechol is ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Riley PA,Stratford MR

更新日期：2015-04-01 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

abstract：:Over-expressions of miRNAs are being increasingly linked with many diseases including different types of cancer. In this study, the role of some known small molecular therapeutics has been investigated for their ability to bind with the pre-miRNA target (hsa-mir-155) and thereby to interfere with the Dicer catalyzed m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Maiti M,Nauwelaerts K,Herdewijn P

更新日期：2012-02-15 00:00:00

abstract：:A series of pentapeptides, based on hMC4R pentapeptide agonist (Bu-His(6)-DPhe(7)-Arg(8)-Trp(9)-Gly(10)-NH(2)), was prepared in which either DPhe(7) or Trp(9) residue was systematically substituted. A number of interesting DPhe surrogates (D-Thi, D-3-CF(3)Phe, D-2-Nal and D-3,4-diClPhe) as well as Trp surrogates (2-Na...

journal_title：Bioorganic & medicinal chemistry letters

authors： Danho W,Swistok J,Cheung AW,Kurylko G,Franco L,Chu XJ,Chen L,Yagaloff K

更新日期：2003-02-24 00:00:00

abstract：:Cannabinoid CB(1) receptor antagonists reduce body weight in rodents and humans, but their clinical utility as anti-obesity agents is limited by centrally mediated side effects. Here, we describe the first mixed CB(1) antagonist/CB(2) agonist, URB447 ([4-amino-1-(4-chlorobenzyl)-2-methyl-5-phenyl-1H-pyrrol-3-yl](pheny...

journal_title：Bioorganic & medicinal chemistry letters

authors： LoVerme J,Duranti A,Tontini A,Spadoni G,Mor M,Rivara S,Stella N,Xu C,Tarzia G,Piomelli D

更新日期：2009-02-01 00:00:00

abstract：:Rational design by the MO calculation disclosed 5,6-dihydrovaltrate (2) as the bioisostere of valtrate (1), the Rev-export inhibitor with anti-HIV activity. The synthesis of 2 was accomplished by ingenious use of asymmetric Diels-Alder reaction and stereoselective epoxidation associated with the adjacent hydroxyl grou...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tamura S,Shimizu N,Fujiwara K,Kaneko M,Kimura T,Murakami N

更新日期：2010-04-01 00:00:00

abstract：:Naturally occurring flavonoids co-exist as glycoside conjugates, which dominate aglycones in their content. To unveil the structure-activity relationship of a naturally occurring flavonoid, we investigated the effects of the glycosylation of naringenin on the inhibition of enzyme systems related to diabetes (protein t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jung HA,Paudel P,Seong SH,Min BS,Choi JS

更新日期：2017-06-01 00:00:00

abstract：:SAR studies on the extension of P3 unit of Boceprevir (1, SCH 503034) with amides and lactams and their synthesis is described. Extensive SAR studies resulted in the identification of 36 bearing 4, 4-dimethyl lactam as the new P4 cap unit with improved potency (K(i)( *)=15nM, EC 90=70nM) and pharmacokinetic properties...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nair LG,Sannigrahi M,Bogen S,Pinto P,Chen KX,Prongay A,Tong X,Cheng KC,Girijavallabhan V,George Njoroge F

更新日期：2010-01-15 00:00:00

abstract：:Novel benzo[b]thiophene diamine thrombin inhibitors were investigated, focusing on a contracted C4'-side chain series. SAR studies identified compounds with either a pyrrolidino or morpholino group as potent, active site directed thrombin inhibitors when the amino group was connected to the C3-phenyl ring with a methy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Takeuchi K,Kohn TJ,Harper RW,Lin HS,Gifford-Moore DS,Richett ME,Sall DJ,Smith GF,Zhang M

更新日期：2000-06-05 00:00:00

abstract：:Identification of an HIV integrase inhibitor with micromolar affinity for the CGRP receptor led to the discovery of a series of structurally novel CGRP receptor antagonists. Optimization of this series produced compound 16, a low-molecular weight CGRP receptor antagonist with good pharmacokinetic properties in both ra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zartman CB,Bell IM,Gallicchio SN,Graham SL,Kane SA,Mallee JJ,Rutledge RZ,Salvatore CA,Vacca JP,Williams TM

更新日期：2011-11-15 00:00:00

abstract：:West Nile Virus (WNV) is a potentially deadly mosquito-borne flavivirus which has spread rapidly throughout the world. Currently there is no effective vaccine against flaviviral infections. We previously reported the identification of pyrazole ester derivatives as allosteric inhibitors of WNV NS2B-NS3 proteinase. Thes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sidique S,Shiryaev SA,Ratnikov BI,Herath A,Su Y,Strongin AY,Cosford ND

更新日期：2009-10-01 00:00:00

abstract：:Clinically relevant Lys103Asn (K103N) mutant frequently observed in HIV-1 reverse transcriptase (RT) confers drug resistance. To obtain useful structural information necessary for targeted-inhibitor design, molecular docking combined with 3D-QSAR CoMFA and CoMSIA was applied to a set of 53 structurally diverse HIV-RT ...

journal_title：Bioorganic & medicinal chemistry letters

authors： San Juan AA

更新日期：2008-02-01 00:00:00

abstract：:The enzyme ATP citrate lyase (ACL) catalyzes the formation of cytosolic acetyl CoA, the starting material for de novo lipid and cholesterol biosynthesis. The dysfunction and upregulation of ACL in numerous cancers makes it an attractive target for developing anticancer therapies. ACL inhibition by shRNA knockdown limi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jernigan FE,Hanai JI,Sukhatme VP,Sun L

更新日期：2017-02-15 00:00:00

abstract：:A series of oligo-peptide based catalysts were prepared using Fmoc solid-phase peptide synthesis. It was found that peptides with N-terminal proline residues catalyzed an aldol reaction yielding enantiomeric enriched product. Peptide H-Pro-Glu-Leu-Phe-OH catalyzed the reaction with good activity and moderate enantiose...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kofoed J,Nielsen J,Reymond JL

更新日期：2003-08-04 00:00:00

abstract：:Nitric oxide (NO), a mediator of various physiological and pathophysiological processes, is synthesized by three isozymes of nitric oxide synthase (NOS). Potential candidate clinical drugs should be devoid of inhibitory activity against endothelial NOS (eNOS), since eNOS plays an important role in maintaining normal b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Le Bourdonnec B,Leister LK,Ajello CA,Cassel JA,Seida PR,O'Hare H,Gu M,Chu GH,Tuthill PA,DeHaven RN,Dolle RE

更新日期：2008-01-01 00:00:00

abstract：:A versatile and high yielding synthesis of novel androgen receptor (AR) antagonists is presented. Using this methodology, six 1,4-substituted-1,2,3-triazole derived bicalutamide mimics were synthesised in five steps and in isolated overall yields from 41% to 85%. Evaluation of these compounds for their anti-proliferat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Altimari JM,Niranjan B,Risbridger GP,Schweiker SS,Lohning AE,Henderson LC

更新日期：2014-11-01 00:00:00

abstract：:Inhibition of BCR-ABL tyrosine kinase activity has shown to be essential for the treatment of chronic myelogenous leukemia (CML). However, drug resistance has quickly arisen in recent clinical trials for STI571 (Gleevec), which is the first approved drug of CML by inhibiting ABL tyrosine kinase. It is desirable to dev...

journal_title：Bioorganic & medicinal chemistry letters

authors： Peng H,Huang N,Qi J,Xie P,Xu C,Wang J,Yang C

更新日期：2003-11-03 00:00:00

abstract：:This work demonstrated the high efficiency of a sub-milligram-synthesis based medicinal chemistry method. Totally 72 compounds, consisting a tri-substituted pyrrolidine core, were prepared. Around 0.1mg of each compound was solid-phase synthesized. Based on the additive property of UV absorptions of unconjugated chrom...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tian Y,Jin J,Wang C,Lv W,Li X,Che X,Gong Y,Li Y,Li Q,Hou J,Wang PG,Shen J

更新日期：2016-05-15 00:00:00

abstract：:A series of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives have been designed, synthesized and evaluated for their potential antiproliferation activity and Aurora-A kinase inhibitory activity. Among all the compounds, compound 10e possessed the most potent biological activity against HCT116 and MCF-7 cell lines...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li X,Lu X,Xing M,Yang XH,Zhao TT,Gong HB,Zhu HL

更新日期：2012-06-01 00:00:00

abstract：:In our efforts to identify potent CRF(1) antagonists with proper physicochemical properties, a series of 3-phenylpyrazolo[1,5-a]pyrimidines bearing polar groups, such as amino, hydroxyl, methoxy, sulfoxide, were designed and synthesized. Several positions of the core structure were identified, where a polar group was ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen C,Wilcoxen KM,Huang CQ,McCarthy JR,Chen T,Grigoriadis DE

更新日期：2004-07-16 00:00:00

abstract：:Bis-(aryl)thioureas were found to be potent and selective inhibitors of cytomegalovirus (CMV) in cultured HFF cells. Of these, the thiazole analogue 38 was investigated as a potential development candidate. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bloom JD,DiGrandi MJ,Dushin RG,Curran KJ,Ross AA,Norton EB,Terefenko E,Jones TR,Feld B,Lang SA

更新日期：2003-09-01 00:00:00

abstract：:Thirteen new 2-pyrazoline derivatives bearing benzenesulfonamide moiety (2a-m) were synthesized by condensing appropriate chalcones with 4-hydrazinonbenzenesulfonamide hydrochloride and tested for anticancer and anti-inflammatory actions. According to the protocol of the National Cancer Institute (NCI) in vitro diseas...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bashir R,Ovais S,Yaseen S,Hamid H,Alam MS,Samim M,Singh S,Javed K

更新日期：2011-07-15 00:00:00

abstract：:A new series of 3,3-disubstituted-5-aryloxindoles has been synthesized and evaluated for progesterone receptor antagonist (PR) activity in a T47D cell alkaline phosphatase assay and for their ability to bind PR in competition binding studies. In this communication, the synthesis and structure-activity relationships (S...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fensome A,Bender R,Cohen J,Collins MA,Mackner VA,Miller LL,Ullrich JW,Winneker R,Wrobel J,Zhang P,Zhang Z,Zhu Y

更新日期：2002-12-02 00:00:00

abstract：:The paper describes the dominating role of surface tension (ST) on the modeling, monitoring, and estimating pK(a) for a large series of 43 substituted sulfonamides. Because of the direct correlation of ST with parachor (Pc) vis-a-vis molecular volume (MV), ST is considered as a steric parameter. Single as well as mult...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thakur M,Thakur A,Khadikar PV,Supuran CT

更新日期：2005-01-03 00:00:00

abstract：:S1P(1) receptor driven lymphopenia has proven utility in the treatment of an array of autoimmune disease states. As a part of our efforts to develop potent and selective S1P(1) receptor agonists, we have identified a novel chemical series of 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acid S1P(1) r...

journal_title：Bioorganic & medicinal chemistry letters

authors： Buzard D,Han S,Thoresen L,Moody J,Lopez L,Kawasaki A,Schrader T,Sage C,Gao Y,Edwards J,Barden J,Thatte J,Fu L,Solomon M,Liu L,Al-Shamma H,Gatlin J,Le M,Xing C,Espinola S,Jones RM

更新日期：2011-10-01 00:00:00

abstract：:A series of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides were synthesized in an effort to prepare novel atypical antipsychotic agents. The compounds were synthesized by either microwave irradiation technique or by conventional synthesis and were characterized by spectral data (IR, (1)H N...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sekhar KV,Rao VS,Devambatla RKV,Kumar MM

更新日期：2008-12-01 00:00:00

abstract：:The synthesis and immunogenicity of a tetanus toxoid (TT)-conjugate of the hexasaccharide portion of the cell-wall polysaccharide (CWPS) of the Group A Streptococcus (GAS) is described. The synthesis relies on the reaction of an allyl glycoside of the hexasaccharide with cysteamine, followed by the reaction of the res...

journal_title：Bioorganic & medicinal chemistry letters

authors： Auzanneau FI,Borrelli S,Pinto BM

更新日期：2013-11-15 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