Novel steroidal vinyl fluorides as inhibitors of steroid C17(20) lyase.

abstract：:A series of aryloxypropanolamines (5a-r) of different chalcones (3a-e) were synthesized and evaluated for antihyperglycemic activity in sucrose loaded (SLM) and streptozotocin (STZ) induced diabetic animal models. Among them compounds 5a, g, m, o, p and r showed significant reduction in blood glucose levels in both SL...

journal_title：Bioorganic & medicinal chemistry

authors： Satyanarayana M,Tiwari P,Tripathi BK,Srivastava AK,Pratap R

更新日期：2004-03-01 00:00:00

abstract：:The 3-aryl-2-cyanoacrylamide scaffold was designed as core pharmacophore for inhibitors of the Dengue and West Nile virus serine proteases (NS2B-NS3). A total of 86 analogs was prepared to study the structure-activity relationships in detail. Thereby, it turned out that the electron density of the aryl moiety and the ...

journal_title：Bioorganic & medicinal chemistry

authors： Nitsche C,Steuer C,Klein CD

更新日期：2011-12-15 00:00:00

abstract：:Hypoxia is a common characteristic of many types of solid tumors and is associated with tumor propagation, malignant progression, and resistance to anti-cancer therapy. HIF-1 pathway is one of the survival pathways activated in tumor in response to hypoxia. In hypoxic condition, hypoxia-inducible factor-1α (HIF-1α) is...

journal_title：Bioorganic & medicinal chemistry

authors： Li J,Xi W,Li X,Sun H,Li Y

更新日期：2019-04-01 00:00:00

abstract：:Soluble epoxide hydrolase (sEH) is a component of the arachidonic acid cascade and is a candidate target for therapies for hypertension or inflammation. Although many sEH inhibitors are available, their scaffolds are not structurally diverse, and knowledge of their specific interactions with sEH is limited. To obtain ...

journal_title：Bioorganic & medicinal chemistry

authors： Amano Y,Yamaguchi T,Tanabe E

更新日期：2014-04-15 00:00:00

abstract：:As a continuous research for the discovery of coumarin-based targeted anticancer agents, we designed and synthesized a series of novel histone deacetylases (HDAC) inhibitors using the 8-ethoxy-3-nitro-2H-chromene as the surface binding or cap group, linear dicarboxylic acid or ω-amino acid moiety with different length...

journal_title：Bioorganic & medicinal chemistry

authors： Tan S,He F,Kong T,Wu J,Liu Z

更新日期：2017-08-01 00:00:00

abstract：:Aspartate-β-semialdehyde dehydrogenase (ASADH) lies at the first branch point in the aspartate metabolic pathway which leads to the biosynthesis of several essential amino acids and some important metabolites. This pathway is crucial for many metabolic processes in plants and microbes like bacteria and fungi, but is a...

journal_title：Bioorganic & medicinal chemistry

authors： Thangavelu B,Bhansali P,Viola RE

更新日期：2015-10-15 00:00:00

abstract：:Studies have demonstrated the presence of allosteric binding sites on each of the muscarinic acetylcholine receptor (mAChR) subtypes. Since most drugs targeting muscarinic receptors bind to the highly conserved orthosteric binding site, they fail to achieve appreciable subtype selectivity. Targeting non-conserved allo...

journal_title：Bioorganic & medicinal chemistry

authors： Maheshwari A,Rao PS,Messer WS Jr

更新日期：2014-03-15 00:00:00

abstract：OBJECTIVE:A new family of 3'-(Mono, di or tri-substituted phenyl)-4'-(4-(methylsulfonyl) phenyl) spiroisoxazoline derivatives containing indanone spirobridge was designed, synthesized, and evaluated for their selective COX-2 inhibitory potency and cytotoxicity on different cell lines. METHODS:A synthetic reaction base...

journal_title：Bioorganic & medicinal chemistry

authors： Abolhasani H,Zarghi A,Komeili Movahhed T,Abolhasani A,Daraei B,Dastmalchi S

更新日期：2021-01-02 00:00:00

abstract：:Novel naphthalimides with two heterocyclic side chains of 2-nitroimidazole for bioreductive binding were designed, synthesized, and used as fluorescent markers for hypoxic cells. Their evaluation for imaging tumor hypoxia was carried out in V79 cells, CHO cells, and 95D cells in vitro by using fluorescence scan ascent...

journal_title：Bioorganic & medicinal chemistry

authors： Liu Y,Xu Y,Qian X,Liu J,Shen L,Li J,Zhang Y

更新日期：2006-05-01 00:00:00

abstract：:Four novel scaffolds consisting of total 24 compounds (1a-1o, 2a-2c, 3a-3c and 4a-4c) bearing aromatic sulfonamide and coumarin moieties connected through various linkers were synthesized in order to synergize the inhibition potential of both the moieties against four selected human carbonic anhydrase isoforms (hCA I,...

journal_title：Bioorganic & medicinal chemistry

authors： Chandak N,Ceruso M,Supuran CT,Sharma PK

更新日期：2016-07-01 00:00:00

abstract：:FAAH inhibitors offer safety advantages by augmenting the anandamide levels "on demand" to promote neuroprotective mechanisms without the adverse psychotropic effects usually seen with direct and chronic activation of the CB1 receptor. FAAH is an enzyme implicated in the hydrolysis of the endocannabinoid N-arachidonoy...

journal_title：Bioorganic & medicinal chemistry

authors： Lamani M,Malamas MS,Farah SI,Shukla VG,Almeida MF,Weerts CM,Anderson J,Wood JT,Farizatto KLG,Bahr BA,Makriyannis A

更新日期：2019-12-01 00:00:00

abstract：:Glucuronide derivatives of CBI-bearing CC-1065 analogues have been synthesized, and their cytotoxicities tested against U937 leukemia cells. The new compounds show potent antitumor activity in vitro. Compounds 1 and 2, and their corresponding glucuronides 3 and 4 have IC(50) values of 0.6, 0.1, 1.4 and 0.6 nM, respect...

journal_title：Bioorganic & medicinal chemistry

authors： Wang Y,Yuan H,Wright SC,Wang H,Larrick JW

更新日期：2003-04-03 00:00:00

abstract：:The emergence of multidrug-resistant bacterial and fungal strains poses a threat to human health that requires the design and synthesis of new classes of antimicrobial agents. We evaluated bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones for their antibacterial and antifungal activities against panels of...

journal_title：Bioorganic & medicinal chemistry

authors： Shrestha SK,Kril LM,Green KD,Kwiatkowski S,Sviripa VM,Nickell JR,Dwoskin LP,Watt DS,Garneau-Tsodikova S

更新日期：2017-01-01 00:00:00

abstract：:We described the discovery and optimization of a novel series of pyrimidopyrimidine derivatives as G-protein coupled receptor 119 (GPR119) agonists against type 2 diabetes. Most designed compounds displayed significant GPR119 agonistic activities. Optimized analogues 15a and 21e exhibited highly potent agonistic activ...

journal_title：Bioorganic & medicinal chemistry

authors： Fang Y,Xu J,Li Z,Yang Z,Xiong L,Jin Y,Wang Q,Xie S,Zhu W,Chang S

更新日期：2018-08-07 00:00:00

abstract：:Nociceptin (NOC) and dynorphin A (DYN) analogues containing 2',6'-dimethylphenylalanine (Dmp) in place of Phe or Tyr in position 1 and/or 4 were synthesized and their metabolic stability and receptor-binding properties were investigated. [Dmp1]NOC(1-13)-NH2 (1) possessed high ORL1 receptor affinity comparable to that ...

journal_title：Bioorganic & medicinal chemistry

authors： Sasaki Y,Kawano S,Kohara H,Watanabe H,Ambo A

更新日期：2006-04-01 00:00:00

abstract：:N-Thiolated beta-lactams are a new family of antibacterials that inhibit the growth of Staphylococcus bacteria. Unlike other beta-lactam drugs, these compounds retain their full antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) strains and operate through a different mode of action. The...

journal_title：Bioorganic & medicinal chemistry

authors： Turos E,Coates C,Shim JY,Wang Y,Leslie JM,Long TE,Reddy GS,Ortiz A,Culbreath M,Dickey S,Lim DV,Alonso E,Gonzalez J

更新日期：2005-12-01 00:00:00

abstract：:Analogues of mitoQ and idebenone were synthesized to define the structural elements that support oxygen consumption in the mitochondrial respiratory chain. Eight analogues were prepared and fully characterized, then evaluated for their ability to support oxygen consumption in the mitochondrial respiratory chain. While...

journal_title：Bioorganic & medicinal chemistry

authors： Duveau DY,Arce PM,Schoenfeld RA,Raghav N,Cortopassi GA,Hecht SM

更新日期：2010-09-01 00:00:00

abstract：:C1027 is a potent antitumor agent that damages DNA. It has the unusual ability to produce double strand breaks and interstrand cross-links (ICLs) intracellularly, which enable it to initiate concurrent ataxia-telangiestasia mutated (ATM) and Rad-3 related (ATR) independent damage responses. The latter form of damage i...

journal_title：Bioorganic & medicinal chemistry

authors： San Pedro JM,Beerman TA,Greenberg MM

更新日期：2012-08-01 00:00:00

abstract：:2-Alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones (F(2)-NH-DABOs) 4, 5 belonging to the dihydro-alkoxy-benzyl-oxopyrimidine (DABO) family and bearing different alkyl- and arylamino side chains at the C(2)-position of the pyrimidine ring were designed as active against wild type (wt) ...

journal_title：Bioorganic & medicinal chemistry

authors： Mai A,Artico M,Ragno R,Sbardella G,Massa S,Musiu C,Mura M,Marturana F,Cadeddu A,Maga G,La Colla P

更新日期：2005-03-15 00:00:00

abstract：:We have synthesized three categories of α,β-unsaturated carbonyl derivatives and evaluated their MAO-A and MAO-B inhibitory activities. Among them, compound 10b including α,β-unsaturated ketone group showed the most potent and selective MAO-B inhibitory activity (IC₅₀ human MAO-B 16 nM, >6000-fold selective vs MAO-A) ...

journal_title：Bioorganic & medicinal chemistry

authors： Choi JW,Jang BK,Cho NC,Park JH,Yeon SK,Ju EJ,Lee YS,Han G,Pae AN,Kim DJ,Park KD

更新日期：2015-10-01 00:00:00

abstract：:A series of potential DNA-binding antitumor agents, 2-[omega-(alkylamino)alkyl]-9-methoxy-5-nitro-2,6-dihydroindazolo[4,3-bc][1,5]naphthyridines (2a-f), 10-aza derivatives of PZA, has been prepared by condensation of 9-chloro-2-methoxy-6-nitro-5,10-dihydrobenzo[b][1,5]naphthyridin-10-one (6) with the appropriate (omeg...

journal_title：Bioorganic & medicinal chemistry

authors： Magnano A,Sparapani S,Lucciarini R,Michela M,Amantini C,Santoni G,Antonini I

更新日期：2004-11-15 00:00:00

abstract：:The success of inhibition of the proteasome by formation of covalent bonds is a major victory over the long held-view that this would lead to binding the wrong targets and undoubtedly lead to toxicity. Great challenges are now found in uncovering ensembles of new moieties capable of forming long lasting ties. We have ...

journal_title：Bioorganic & medicinal chemistry

authors： Brouwer AJ,Herrero Álvarez N,Ciaffoni A,van de Langemheen H,Liskamp RM

更新日期：2016-08-15 00:00:00

abstract：:The clinical success of covalent kinase inhibitors in the treatment of EGFR-dependent non-small cell lung cancer (NSCLC) has rejuvenated the appreciation of reactive small molecules. Acquired drug resistance against first-line EGFR inhibitors remains the major bottleneck in NSCLC and is currently addressed by the appl...

journal_title：Bioorganic & medicinal chemistry

authors： Basu D,Richters A,Rauh D

更新日期：2015-06-15 00:00:00

abstract：:Several rationally designed analogs of 3-fluoro-2-oxo-3-phenylpropionic acid were chemically synthesized, and the reactions of the hydrate form of these compounds with 4-hydroxyphenylpyruvate dioxygenase from pig liver as inhibitors were examined. Compounds 14a and 14b were found to be potent competitive inhibitors of...

journal_title：Bioorganic & medicinal chemistry

authors： Ling TS,Shiu S,Yang DY

更新日期：1999-07-01 00:00:00

abstract：:The structure-activity relationship of a number of synthetic green tea polyphenol analogs involving modifications of A ring and B ring of epi-gallocatechin gallate (EGCG) as proteasome inhibitors has been examined. It was found that in B ring, a decrease in the number of OH groups led to decreased potency. Introductio...

journal_title：Bioorganic & medicinal chemistry

authors： Wan SB,Landis-Piwowar KR,Kuhn DJ,Chen D,Dou QP,Chan TH

更新日期：2005-03-15 00:00:00

abstract：:Twenty analogues of the natural antitumor agent dolastatin 11, including majusculamide C, were synthesized and tested for cytotoxicity against human cancer cells and stimulation of actin polymerization. Only analogues containing the 30-membered ring were active. Molecular modeling and NMR evidence showed the low-energ...

journal_title：Bioorganic & medicinal chemistry

authors： Ali MA,Bates RB,Crane ZD,Dicus CW,Gramme MR,Hamel E,Marcischak J,Martinez DS,McClure KJ,Nakkiew P,Pettit GR,Stessman CC,Sufi BA,Yarick GV

更新日期：2005-07-01 00:00:00

abstract：:2-Phenyl-9-benzyl-8-azapurines, bearing at the 6 position an amido group interposed between the 8-azapurine moiety and an alkyl or a substituted phenyl group, have been synthesised and assayed as ligands for adenosine receptors. All the compounds show high affinity for the A(1) adenosine receptor, and many of them als...

journal_title：Bioorganic & medicinal chemistry

authors： Giorgi I,Leonardi M,Pietra D,Biagi G,Borghini A,Massarelli I,Ciampi O,Bianucci AM

更新日期：2009-03-01 00:00:00

abstract：:Verticipyrone has recently been isolated from the culture broth of Verticillium sp. and shown to inhibit NADH fumarate reductase, as well as NADH oxidoreductase (complex I) of the mitochondrial electron transport chain. In order to assess the structural elements in verticipyrone essential for complex I inhibitor, 15 s...

journal_title：Bioorganic & medicinal chemistry

authors： Leiris SJ,Khdour OM,Segerman ZJ,Tsosie KS,Chapuis JC,Hecht SM

更新日期：2010-05-15 00:00:00

abstract：:A series of twenty seven substituted 2-(2-oxobenzo[d]oxazol-3(2H)-yl)acetamide derivatives were designed based on our earlier reported Mycobacterium tuberculosis (MTB) enoyl-acyl carrier protein reductase (InhA) lead. Compounds were evaluated for MTB InhA inhibition study, in vitro activity against drug-sensitive and ...

journal_title：Bioorganic & medicinal chemistry

authors： Pedgaonkar GS,Sridevi JP,Jeankumar VU,Saxena S,Devi PB,Renuka J,Yogeeswari P,Sriram D

更新日期：2014-11-01 00:00:00

abstract：:The pH-rate profile for the hydrolysis of 3'-phosphoadenosine 5'-phosphosulfate (PAPS) in aqueous solution has been measured. Comparison with other data suggests that hydrolysis occurs by almost complete unimolecular elimination of sulfur trioxide, with weak involvement of a molecule of water in the transition state. ...

journal_title：Bioorganic & medicinal chemistry

authors： Bedford CT,Kirby AJ,Logan CJ,Drummond JN

更新日期：1995-02-01 00:00:00