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

abstract：:A series of new imines and amines have been synthesized by condensation of 1H-3-ferrocenyl-1-phenylpyrazole-4-carboxaldehyde with the corresponding amines, followed by reduction with sodium borohydride. The synthesized compounds have been screened for their in vitro antimicrobial activity against 11 bacteria and three...

journal_title：Bioorganic & medicinal chemistry letters

authors： Damljanović I,Vukićević M,Radulović N,Palić R,Ellmerer E,Ratković Z,Joksović MD,Vukićević RD

更新日期：2009-02-15 00:00:00

abstract：:Several unnatural derivatives of narciclasine were prepared in which the C-7 carbon was replaced with nitrogen. The 7-aza derivative and its N-oxide were prepared by the coupling of iodopicolinic acid with a conduramine unit derived chemoenzymatically from bromobenzene. Intramolecular Heck reaction was used to constru...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vshyvenko S,Reisenauer MR,Rogelj S,Hudlicky T

更新日期：2014-09-01 00:00:00

abstract：:A series of novel oxime-containing pyrazole derivatives were synthesized by the reaction of ethyl 3-phenyl-1H-pyrazole-5-carboxylate derivatives and 2-bromo-1-phenylethanone followed by the reaction with hydroxylamine hydrochloride. The structures were determined by IR, (1)H NMR, HRMS, and X-ray analysis. A dose- and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zheng LW,Li Y,Ge D,Zhao BX,Liu YR,Lv HS,Ding J,Miao JY

更新日期：2010-08-15 00:00:00

abstract：:The synthesis of amidinoaryloxy 9-benzyl-8-methyl-9H-purine, 7,8-dihydropteridine-6(5H)-one and 5,7-dihydropyrimido[4,5-b][1,4]oxazine-6-one inhibitors of Factor Xa is described. These compounds show nanomolar potency against FXa and maintain high selectivity over thrombin and trypsin. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Buckman BO,Mohan R,Koovakkat S,Liang A,Trinh L,Morrissey MM

更新日期：1998-08-18 00:00:00

abstract：:Novel isocyanate and diazoketone linkers possessing polyoxypropylenediamine as a spacer for small-molecule microrray are developed. White light interferometry is introduced to detect bound proteins on the glass slides without using chemically modified proteins. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kurosu M,Mowers WA

更新日期：2006-07-01 00:00:00

abstract：:Inactivation of the NF-κB signaling pathway by inhibition of IKKβ is a well-known approach to treat inflammatory diseases such as rheumatoid arthritis and cancer. Thienopyrimidine-based analogues were designed through modification of the known IKKβ inhibitor, SPC-839, and then biologically evaluated. The resulting ana...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park CH,Lee C,Yang JS,Joe BY,Chun K,Kim H,Kim HY,Kang JS,Lee JI,Kim MH,Han G

更新日期：2014-06-15 00:00:00

abstract：:The optimization of a series of 4-(dimethylamino)quinazoline antagonists of the melanin-concentrating hormone receptor 1 (MCH-R1) is described. The combination of the elaboration of both the linker portion and the terminal phenyl ring provided N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-3,4-difluorob...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kanuma K,Omodera K,Nishiguchi M,Funakoshi T,Chaki S,Semple G,Tran TA,Kramer B,Hsu D,Casper M,Thomsen B,Sekiguchi Y

更新日期：2005-09-01 00:00:00

abstract：:The design and synthesis of new 1alpha,25-dihydroxy-19-norvitamin D(3) analogues 3a-c, which have an amide bond in the molecule instead of the diene, are described. The A-ring moiety was constructed by a (3S,5S)-3,5-dihydroxypiperidine derivative (9, 11, or 13) prepared from D-mannose, and a CD-ring carboxylic acid 16...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suhara Y,Kittaka A,Ono K,Kurihara M,Fujishima T,Yoshida A,Takayama H

更新日期：2002-12-16 00:00:00

abstract：:In an effort to identify novel, broad-spectrum inhibitors against the metallo-β-lactamases (MβLs), several N-heterocyclic derivatives were tested as inhibitors of MβLs CcrA, ImiS, and L1, which are representative enzymes from the distinct MβL subclasses. Three N-heterocyclic dicarboxylic acid derivatives were competit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Feng L,Yang KW,Zhou LS,Xiao JM,Yang X,Zhai L,Zhang YL,Crowder MW

更新日期：2012-08-15 00:00:00

abstract：:Antagonists of the integrin receptor alpha(v)beta(3) are expected to have utility in the treatment of osteoporosis through inhibition of bone resorption. A series of potent, chain-shortened, pyrrolidinone-containing alpha(v)beta(3) receptor antagonists is described. Two sets of diasteromeric pairs of high-affinity ant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Perkins JJ,Duong LT,Fernandez-Metzler C,Hartman GD,Kimmel DB,Leu CT,Lynch JJ,Prueksaritanont T,Rodan GA,Rodan SB,Duggan ME,Meissner RS

更新日期：2003-12-15 00:00:00

abstract：:The investigation of the Vietnamese marine sponge Spongia sp. led to the isolation of three new sesquiterpene phenols, langconols A-C (1-3), and one new sesquiterpene hydroxyquinone, langcoquinone C (4), together with two known meroterpenoids (5 and 6). Their structures were determined on the basis of spectroscopic an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nguyen HM,Ito T,Kurimoto SI,Ogawa M,Win NN,Hung VQ,Nguyen HT,Kubota T,Kobayashi J,Morita H

更新日期：2017-07-15 00:00:00

abstract：:A series of N-7-methyl-imidazolopyrimidine inhibitors of the mTOR kinase have been designed and prepared, based on the hypothesis that the N-7-methyl substituent on imidazolopyrimidine would impart selectivity for mTOR over the related PI3Kα and δ kinases. The corresponding N-Me substituted pyrrolo[3,2-d]pyrimidines a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee W,Ortwine DF,Bergeron P,Lau K,Lin L,Malek S,Nonomiya J,Pei Z,Robarge KD,Schmidt S,Sideris S,Lyssikatos JP

更新日期：2013-09-15 00:00:00

abstract：:Herein we report the discovery and SAR of an indole-based protease activated receptor-4 (PAR-4) antagonist scaffold derived from a similarity search of the Vanderbilt HTS collection, leading to MLPCN probe ML354 (VU0099704). Using a novel PAC-1 fluorescent αIIbβ3 activation assay this probe molecule antagonist was fou...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wen W,Young SE,Duvernay MT,Schulte ML,Nance KD,Melancon BJ,Engers J,Locuson CW 2nd,Wood MR,Daniels JS,Wu W,Lindsley CW,Hamm HE,Stauffer SR

更新日期：2014-10-01 00:00:00

abstract：:Several chemical modifications in the N(1)-benzenesulfonamide ring of celecoxib are presented. The series with a hydroxymethyl group adjacent to the sulfonamide was found to be the most potent modification that yielded many compounds selectively active against COX-2 enzyme in vitro. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh SK,Reddy PG,Rao KS,Lohray BB,Misra P,Rajjak SA,Rao YK,Venkateswarlu A

更新日期：2004-01-19 00:00:00

abstract：:In order to define the structural requirements of quinazoline-2(1H)-thiones 1 for their inhibitory activity on melanogenesis, a novel series of 3,4-dihydroquinazoline-2(1H)-thiones (3a-h) were prepared and screened for their melanogenesis inhibition on melanoma B16 cell line under the stimulant of alpha-MSH. The anti-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thanigaimalai P,Sharma VK,Lee KC,Yun CY,Kim Y,Jung SH

更新日期：2010-08-15 00:00:00

abstract：:In our efforts to develop CGRP receptor antagonists as backups to MK-3207, 2, we employed a scaffold hopping approach to identify a series of novel oxazolidinone-based compounds. The development of a structurally diverse, potent (20, cAMP+HS IC50=0.67 nM), and selective compound (hERG IC50=19 μM) with favorable rodent...

journal_title：Bioorganic & medicinal chemistry letters

authors： Crowley BM,Stump CA,Nguyen DN,Potteiger CM,McWherter MA,Paone DV,Quigley AG,Bruno JG,Cui D,Culberson JC,Danziger A,Fandozzi C,Gauvreau D,Kemmerer AL,Menzel K,Moore EL,Mosser SD,Reddy V,White RB,Salvatore CA,Kane S

更新日期：2015-11-01 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：:As a continuation of our efforts to discover and develop the apoptosis inducing 4-aryl-4H-chromenes as novel anticancer agents, we explored the SAR of 4-aryl-4H-chromenes with modifications at the 7- and 5-, 6-, 8-positions. It was found that a small hydrophobic group, such as NMe2, NH2, NHEt, and OMe, is preferred at...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kemnitzer W,Kasibhatla S,Jiang S,Zhang H,Zhao J,Jia S,Xu L,Crogan-Grundy C,Denis R,Barriault N,Vaillancourt L,Charron S,Dodd J,Attardo G,Labrecque D,Lamothe S,Gourdeau H,Tseng B,Drewe J,Cai SX

更新日期：2005-11-01 00:00:00

abstract：:Cage amines 1-4 are potent peripheral anionic site-bound reversible inhibitors of both acetylcholinesterase and butyrylcholinesterase. Cage amines 1-3 are selective butyrylcholinesterase inhibitor versus acetylcholinesterase. For both enzymes, the -log K(i) values linearly correlate with the difference of substituted ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lin G,Tsai HJ,Tsai YH

更新日期：2003-09-01 00:00:00

abstract：:The methylendioxyphenyl group, present in a number of potent endothelin receptor antagonists, could have undesirable metabolic interactions with cytochrome P450 in vivo. Using a self-organizing neural network we analysed the features of molecular electrostatic potentials of several endothelin receptor ligands. A libra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Anzali S,Mederski WW,Osswald M,Dorsch D

更新日期：1998-01-06 00:00:00

abstract：:A series of 6/7-mono and disubstituted quinolone-3-carboxamide derivatives (1-12) were synthesized and their in vitro methemoglobin producing capacity have been delineated. The compounds 5, 6, 9 and 10 showed minimum methemoglobin toxicity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Srivastava S,Srivastava SK,Shukla A,Chauhan PM,Puri SK,Bhaduri AP,Pandey VC

更新日期：1999-01-04 00:00:00

abstract：:A non-methionine FT inhibitor lead structure (1) was designed through computer modeling of the peptidomimetic FT inhibitor ABT839. Optimization of this lead resulted in compounds 2e and 2g, with FT IC(50) values of 1.3 and 1.8 nM, GGT IC(50) of 1400 nM, and EC(50) (Ras processing) values of 13 and 11 nM, respectively....

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang GT,Wang X,Wang W,Hasvold LA,Sullivan G,Hutchins CW,O'Conner S,Gentiles R,Sowin T,Cohen J,Gu WZ,Zhang H,Rosenberg SH,Sham HL

更新日期：2005-01-03 00:00:00

abstract：:NAD(P)H-dependent oxidoreductases play important roles in biology. Recently, we reported that the luminescence lifetime of some Tb(3+) complexes is sensitive to NAD(P)H, and we used this phenomenon to detect activities of these enzymes. However, conventional time-resolved luminescence assays are susceptible to static ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Terai T,Ito H,Hanaoka K,Komatsu T,Ueno T,Nagano T,Urano Y

更新日期：2016-05-01 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：:Novel 3-[4-(dimethylamino)phenyl]alkyl-2-oxindole analogs were synthesized by either of the following two pathways: (1) a sequence of Knoevenagel condensation of oxindole with (4-dimethylamino)cinnamaldehyde-hydrogenation, or (2) alkylation of oxindole dianion with [(4-dimethylamino)phenyl]alkyl halides. Subsequent al...

journal_title：Bioorganic & medicinal chemistry letters

authors： Furuta K,Kawai Y,Mizuno Y,Hattori Y,Koyama H,Hirata Y

更新日期：2017-09-15 00:00:00

abstract：:Although PK11195 binds to the peripheral benzodiazepine receptor with nanomolar affinity, significant data exist which suggest that it has another cellular target distinct from the PBR. Here we demonstrate that PK11195 inhibits F(1)F(0)-ATPase activity in an OSCP-dependent manner, similar to the pro-apoptotic benzodia...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cleary J,Johnson KM,Opipari AW Jr,Glick GD

更新日期：2007-03-15 00:00:00

abstract：:Three novel steroidal antiestrogen-geldanamycin conjugates were prepared using a convergent strategy. The antiestrogenic component utilized the 11β-(4-functionalized-oxyphenyl) estradiol scaffold, while the geldanamycin component was derived by replacement of the 17-methoxy group with an appropriately functionalized a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Adam Hendricks J,Hanson RN,Amolins M,Mihelcic JM,Blagg BS

更新日期：2013-06-15 00:00:00

abstract：:By performing RNA-targeted structure-activity relationship studies, we discovered a novel peptidomimetic containing squaryldiamide as a potential bioisostere replacement for guanidine that binds transactivation responsive RNA with high affinity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee CW,Cao H,Ichiyama K,Rana TM

更新日期：2005-10-01 00:00:00

abstract：:A survey of isosteric replacements of the phosphonoalanine side chain coupled with a process of conformational constraint of a bisbenzimidazole-based, Zn(2+)-dependent inhibitor of hepatitis C virus (HCV) NS3 serine protease resulted in the identification of novel series of active compounds with extended side chains. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yeung KS,Meanwell NA,Qiu Z,Hernandez D,Zhang S,McPhee F,Weinheimer S,Clark JM,Janc JW

更新日期：2001-09-03 00:00:00

abstract：:We report (a) on the synthesis of a long-wavelength fluorescent coumarin containing an allyloxy acetate moiety, (b) the synthesis of two linkers containing an allyloxy acetate and an alkyne or azide function, respectively, and (c) the selective modification human serum albumin by a sequential method involving Pd(II) c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cserép GB,Herner A,Wolfbeis OS,Kele P

更新日期：2013-11-01 00:00:00