Simple and an efficient method for the synthesis of 1-[2-dimethylamino-1-(4-methoxy-phenyl)-ethyl]-cyclohexanol hydrochloride: (+/-) venlafaxine racemic mixtures.

abstract：:Matrix metalloproteinase-13 (MMP-13) has been implicated as the protease responsible for collagen degradation in cartilage during osteoarthritis (OA). Compounds that inhibit the metalloproteinase at the Zn binding site typically lack specificity among MMP family members. Analogs of the low-micromolar lead MMP-13 inhib...

journal_title：Bioorganic & medicinal chemistry letters

authors： Roth J,Minond D,Darout E,Liu Q,Lauer J,Hodder P,Fields GB,Roush WR

更新日期：2011-12-01 00:00:00

abstract：:In the course of ongoing research on protein tyrosine phosphatase 1B (PTP1B) inhibitory compounds from Antarctic lichens, four new diterpene furanoids, hueafuranoids A-D (1-4) have been isolated from the MeOH extract of Antarctic lichen Huea sp. by various chromatographic methods. The structures of these compounds wer...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cui Y,Yim JH,Lee DS,Kim YC,Oh H

更新日期：2012-12-15 00:00:00

abstract：:We report the discovery of a series of 4-aryl-2-aminoalkylpyrimidine derivatives as potent and selective JAK2 inhibitors. High throughput screening of our in-house compound library led to the identification of hit 1, from which optimization resulted in the discovery of highly potent and selective JAK2 inhibitors. Adva...

journal_title：Bioorganic & medicinal chemistry letters

authors： Forsyth T,Kearney PC,Kim BG,Johnson HW,Aay N,Arcalas A,Brown DS,Chan V,Chen J,Du H,Epshteyn S,Galan AA,Huynh TP,Ibrahim MA,Kane B,Koltun ES,Mann G,Meyr LE,Lee MS,Lewis GL,Noguchi RT,Pack M,Ridgway BH,Shi X,

更新日期：2012-12-15 00:00:00

abstract：:RNA regulation and maintenance are critical for proper cell function. Small molecules that specifically alter RNA sequence would be exceptionally useful as probes of RNA structure and function or as potential therapeutics. Here, we demonstrate a photochemical approach for altering the trinucleotide expanded repeat cau...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guan L,Luo Y,Ja WW,Disney MD

更新日期：2018-09-01 00:00:00

abstract：:Mifepristone is a non-selective antagonist of 3-oxosteroid receptors with both abortifacient and anti-endometriotic activities. Non-steroidal mimetics of mifepristone and progesterone are important templates for modulation of the progesterone receptor (PR). For our PR program, we sought an unexplored, synthetically ac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jones DG,Liang X,Stewart EL,Noe RA,Kallander LS,Madauss KP,Williams SP,Thompson SK,Gray DW,Hoekstra WJ

更新日期：2005-07-01 00:00:00

abstract：:A series of phenoxy benzoxaboroles were synthesized and screened for their inhibitory activity against PDE4 and cytokine release. 5-(4-Cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2728) showed potent activity both in vitro and in vivo. This compound is now in clinical development for the topical treatment ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Akama T,Baker SJ,Zhang YK,Hernandez V,Zhou H,Sanders V,Freund Y,Kimura R,Maples KR,Plattner JJ

更新日期：2009-04-15 00:00:00

abstract：:A series of m-carborane derivatives was prepared based upon the structures of antiestrogenic drugs and their activities were evaluated by estrogen receptor alpha (ERalpha) binding assay and transactivation assay using human breast cancer cell line, MCF-7 cells. The m-carborane bisphenol 5 exhibited about a thousand ti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ogawa T,Ohta K,Yoshimi T,Yamazaki H,Suzuki T,Ohta S,Endo Y

更新日期：2006-08-01 00:00:00

abstract：:During the course of our investigations in the field of azole antimicrobial agents, we have identified BM212 a pyrrole derivative with good in vitro activity against mycobacteria and candidae. These findings prompted us to prepare new pyrrole derivatives 2-6 in the hope of increasing the activity. The microbiological ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Biava M,Fioravanti R,Porretta GC,Deidda D,Maullu C,Pompei R

更新日期：1999-10-18 00:00:00

abstract：:A series of N-4-substituted-benzyl-N'-tert-butylbenzyl thioureas were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor in rat DRG neurons. Their structure-activity relationship reveals that not only the two oxygens and amide hydrogen of sulfonamido group, but also the optimal...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park HG,Choi JY,Choi SH,Park MK,Lee J,Suh YG,Cho H,Oh U,Lee J,Kang SU,Lee J,Kim HD,Park YH,Su Jeong Y,Kyu Choi J,Jew SS

更新日期：2004-02-09 00:00:00

abstract：:The structure of the S1P2 antagonist 1 has been modified with the aim of improving its oral bioavailability. The chemical modification of the alkyl chain and carboxylic acid moieties of 1 led to significant improvements in the oral exposure of compounds belonging to this series. The optimization of the ring size of th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kusumi K,Shinozaki K,Yamaura Y,Hashimoto A,Kurata H,Naganawa A,Otsuki K,Matsushita T,Sekiguchi T,Kakuuchi A,Yamamoto H,Seko T

更新日期：2016-02-15 00:00:00

abstract：:The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing a butynyloxy P1' group was explored. In particular, compound 5k has excellent in vitro potency against TACE enzyme and in cells, and oral activity in an in vivo model of TNF-alpha production and a collagen-induced arthritis model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Levin JI,Chen JM,Laakso LM,Du M,Du X,Venkatesan AM,Sandanayaka V,Zask A,Xu J,Xu W,Zhang Y,Skotnicki JS

更新日期：2005-10-01 00:00:00

abstract：:A computer-aided drug design strategy leads to the identification of a new class of p38 inhibitors based on the 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) scaffold. The tolyl triazole amides provided a potent platform amenable to optimization. Further exploration leads to compounds with greater than 100-fold improveme...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cogan DA,Aungst R,Breinlinger EC,Fadra T,Goldberg DR,Hao MH,Kroe R,Moss N,Pargellis C,Qian KC,Swinamer AD

更新日期：2008-06-01 00:00:00

abstract：:Naphthalimide-derived azoles as a new type of antimicrobial agents were synthesized and evaluated for their efficiency in vitro against eight bacteria and two fungi by two fold serial dilution technique. Most title compounds exhibited good antimicrobial potency with low MIC values ranging from 1 to 16μg/mL. Notably, s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang YY,Zhou CH

更新日期：2011-07-15 00:00:00

abstract：:We describe the identification, SAR, and in vivo pharmacology of a new series of Src-family selective Lck inhibitors. These thienopyridines were designed based on a desire to access the unique residues in the extended hinge region of Lck. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Abbott L,Betschmann P,Burchat A,Calderwood DJ,Davis H,Hrnciar P,Hirst GC,Li B,Morytko M,Mullen K,Yang B

更新日期：2007-03-01 00:00:00

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

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

abstract：:Our series of competitive antagonists against the G-protein coupled receptor P2Y(14) were found to be highly shifted in the presence of serum (>99% protein bound). A binding assay using 2% human serum albumin (HSA) was developed to guide further SAR studies and led to the identification of the zwitterion 2, which is s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Robichaud J,Fournier JF,Gagné S,Gauthier JY,Hamel M,Han Y,Hénault M,Kargman S,Levesque JF,Mamane Y,Mancini J,Morin N,Mulrooney E,Wu J,Black WC

更新日期：2011-07-15 00:00:00

abstract：:Four platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with different bidentate dicarboxylates (1 oxalate, 2 malonate, 3 1,1-cyclobutanedicarboxylate and 4 3-hydroxy-1,1-cyclobutanedicarboxylate) as leaving groups were synthesized and characterized by elemental analyses, IR and (1)HNMR spectra together w...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu G,Zhao J,Gou S,Pang J

更新日期：2015-01-15 00:00:00

abstract：:Structure- and ligand-based virtual-screening methods (docking, 2D- and 3D-similarity searching) were analyzed for their effectiveness in virtual screening against FFAR2. To evaluate the performance of these methods, retrospective virtual screening was performed. Statistical quality of the methods was evaluated by BED...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fells JI,Ai X,Weinglass A,Feng W,Lei Y,Finley M,Hoveyda HR,Fraser GL,Machacek M

更新日期：2020-11-01 00:00:00

abstract：:The carbodiimides 2, obtained from aza-Wittig reactions of iminophosphorane 1 with aromatic isocyanates, reacted with ammonia to give ethyl 3,4-dihydro-6-methyl-4-oxo-2-arylamino-furo[2,3-d]pyrimidine-5-carboxylate 3. Further reaction of 3 with POCl(3) and various amines generated ethyl 4-alkylamino-2-arylamino-6-meth...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hu YG,Wang Y,Du SM,Chen XB,Ding MW

更新日期：2010-11-01 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：:Novel and artificial anthraquinone-carbohydrate hybrids were designed and synthesized, and found to effectively cleave DNA under irradiation with a long wavelength UV light and also exhibit cytotoxicity against HeLa S3 cells. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Toshima K,Maeda Y,Ouchi H,Asai A,Matsumura S

更新日期：2000-10-02 00:00:00

abstract：:Pyrrole-imidazole polyamides can be synthesized to target predetermined sequences of DNA with nanomolar affinity and high specificity, and have been shown to modulate gene transcription both in vitro and in vivo. To make polyamides more readily available to biological laboratories, we have developed a rapid solid-phas...

journal_title：Bioorganic & medicinal chemistry letters

authors： Krutzik PO,Chamberlin AR

更新日期：2002-08-19 00:00:00

abstract：:The 4-(3-phenylprop-1-yl)piperidine moiety of the 1,3,4-trisubstituted pyrrolidine CCR5 antagonist 1 was modified with electron deficient aromatics as well as replacement of the benzylic methylene with sulfones, gem-difluoromethylenes and alcohols in an effort to balance the antiviral potency with reasonable pharmacok...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lynch CL,Willoughby CA,Hale JJ,Holson EJ,Budhu RJ,Gentry AL,Rosauer KG,Caldwell CG,Chen P,Mills SG,MacCoss M,Berk S,Chen L,Chapman KT,Malkowitz L,Springer MS,Gould SL,DeMartino JA,Siciliano SJ,Cascieri MA,Carella

更新日期：2003-01-06 00:00:00

abstract：:(S)-4-(Carboxamido)phenylalanine (Cpa) is examined as a bioisosteric replacement for the terminal tyrosine (Tyr) residue in a variety of known peptide ligands for the mu, delta and kappa opioid receptors. The Cpa-containing peptides, assayed against cloned human opioid receptors, display comparable binding affinity (K...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dolle RE,Machaut M,Martinez-Teipel B,Belanger S,Cassel JA,Stabley GJ,Graczyk TM,DeHaven RN

更新日期：2004-07-05 00:00:00

abstract：:The our previous study synthesized the chrysin-chromene-spirooxindole hybrids 3, and further found compound 3e had good antitumor activity against A549 cells in vitro through multi-target co-regulation of the p53 signalling pathway to inhibit the proliferation of A549 cells. This study was designed to evaluate the ant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang WH,Chen S,Liu XL,Bing-Lin,Liu XW,Zhou Y

更新日期：2020-09-01 00:00:00

abstract：:We previously identified the methylsulfonylnitrobenzoates (MSNBs) that block the interaction of the thyroid hormone receptor with its obligate transcriptional coactivators and prevent thyroid hormone signaling. As part of our lead optimization work we demonstrated that sulfonylnitrophenylthiazoles (SNPTs), which repla...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hwang JY,Attia RR,Carrillo AK,Connelly MC,Guy RK

更新日期：2013-03-15 00:00:00

abstract：:The new binuclear platinum(II) complexes, (1,3-benzenedimethanethiolate-S)di(2,2',2"-terpyridine)diplatinum(II) chloride tetrahydrate, 5, and (1,4-benzenedimethanethiolate-S)di(2,2',2"-terpyridine)diplatinum(II) chloride tetrahydrate, 6, were synthesized in order to investigate the binding of platinum(II) complex with...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kurosaki H,Yamakawa N,Sumimoto M,Kimura K,Goto M

更新日期：2003-03-10 00:00:00

abstract：:Cyclobranol 8A, an analog of the cycloartenol substrate 1A for the plant sterol C24-methyltransferase (SMT), was shown to be an acceptor of the soybean SMT1 as well as an inhibitor of enzyme action. The K(m) and k(cat) for 8A was 37 microM and 0.006 min(-1), respectively. The enzyme-generated product was identified by...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang J,Nes WD

更新日期：2008-07-15 00:00:00

abstract：:Beauveria bassiana AM278 and Absidia coerulea AM93 converted 8-prenylnaringenin (1) into two glycoside derivatives (7-O-β-D-glucopyranoside) (2) and 7-O-β-D-4'''-O-methylglucopyranoside) (3) in high yields in processes conducted in Saboraud medium. 8-Prenylnaringenin 7-O-β-D-4'''-O-methylglucopyranoside (3) is a new c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bartmańska A,Tronina T,Huszcza E

更新日期：2012-10-15 00:00:00

abstract：:A series of 3-substituted benzamide derivatives structurally related to STI-571 (imatinib mesylate), a Bcr-Abl tyrosine kinase inhibitor used to treat chronic myeloid leukemia (CML), was prepared and evaluated for antiproliferative activity against the Bcr-Abl-positive leukemia cell line K562. About ten 3-halogenated ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Asaki T,Sugiyama Y,Hamamoto T,Higashioka M,Umehara M,Naito H,Niwa T

更新日期：2006-03-01 00:00:00