Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.

abstract：:Substituted pyrazoles, 1,2,4-triazoles, and tetrazoles are good surrogates for cis-amide bonds in a series of boronate ester thrombin inhibitors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Duncia JV,Santella JB 3rd,Higley CA,VanAtten MK,Weber PC,Alexander RS,Kettner CA,Pruitt JR,Liauw AY,Quan ML,Knabb RM,Wexler RR

更新日期：1998-04-07 00:00:00

abstract：:Piperazinyl benzamidines were prepared and found to bind to the rat delta (delta) opioid receptor. The most active compounds had a N,N-diethylcarboxamido group and a N-benzyl piperazine. The most potent among these was N,N-diethyl-4-[4-(phenylmethyl)-1-piperazinyl][2-(trifluoromethyl)phenyl]iminomethyl]benzamide (27) ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nortey SO,Baxter EW,Codd EE,Zhang SP,Reitz AB

更新日期：2001-07-09 00:00:00

abstract：:A series of novel arylsulfonylpropargylglycinamide derivatives was investigated as thrombin inhibitors in which the SAR was focused on substituents at the acetylenic terminus. Several compounds in this series were identified as potent thrombin inhibitors (Ki up to 5 nM) that are highly selective over trypsin and other...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee K,Hwang SY,Park CW

更新日期：1999-04-05 00:00:00

abstract：:This study explores the possible use of reactive oxygen-activated DNA modifying agents against acute myeloid leukemia (AML). A key amine on the lead agent was investigated via cytotoxicity assays and was found necessary for potency. The two best compounds were screened via the NCI-60 cell panel. These two compounds ha...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bell-Horwath TR,Vadukoot AK,Thowfeik FS,Li G,Wunderlich M,Mulloy JC,Merino EJ

更新日期：2013-05-15 00:00:00

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：:The synthesis and biological activity of a novel series of tricyclic retinoic acid receptor antagonists are described. These compounds bind with high affinity to the RARs and are potent antagonists of retinoid function in in vitro and in vivo systems. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vuligonda V,Standeven AM,Escobar M,Chandraratna RA

更新日期：1999-03-08 00:00:00

abstract：:A series of genistein derivatives, prepared by alkylation and difluoromethylation, were tested for their inhibitory effects on the hydrogen peroxide induced impairment in human umbilical vein endothelial (HUVE-12) cells in vitro. The HUVE-12 cells were pretreated with either the vehicle solvent (DMSO), genistein, or d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fu XH,Wang L,Zhao H,Xiang HL,Cao JG

更新日期：2008-01-15 00:00:00

abstract：:A new abietane, namely, 20-hydroxyferruginol (1), together with known ferruginol (2), 18-hydroxyferruginol (3), sugiol (4), and 6alpha-hydroxysugiol (5), were isolated from the cones of Sequoia sempervirens. Their structures were elucidated through spectral data. Compounds 1 and 5 strongly inhibited colon, lung, and b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Son KH,Oh HM,Choi SK,Han DC,Kwon BM

更新日期：2005-04-15 00:00:00

abstract：:The structure-based approaches were implemented to design and rationally select the molecules for synthesis and anti-HCV activity evaluation. The systematic structure-activity relationships of previously discovered molecules (types I, II, III) were analyzed to design new molecules (type IV) by bioisosteric replacement...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thiyagarajan A,Salim MT,Balaraju T,Bal C,Baba M,Sharon A

更新日期：2012-12-15 00:00:00

abstract：:Quinolizidinyl derivatives of the tricyclic systems characterizing pirenzepine and nuvenzepine, were prepared and tested as ligands for muscarinic M1, M2 and M3 receptors; 5,11-dihydro-11-[(S-lupinyl)-thioacetyl]-6H-pyrido[2,3-b][1, 4]benzodiazepin-6-one exhibited IC50 = 10 nM for M1 and 760 nM for both M2 and M3 subt...

journal_title：Bioorganic & medicinal chemistry letters

authors： Novelli F,Sparatore A,Tasso B,Sparatore F

更新日期：1999-10-18 00:00:00

abstract：:The synthesis and anti-angiogenic activities of linomide and its analogues are reported. Three of the analogues are 3.3-69 times more potent than linomide at inhibiting blood vessel formation in the CAM angiogenesis assay. These compounds possessed considerable anti-proliferative activity against isolated HUVEC cells ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shi J,Xiao Z,Ihnat MA,Kamat C,Pandit B,Hu Z,Li PK

更新日期：2003-03-24 00:00:00

abstract：:New ligands for in vivo brain imaging of serotonin transporter (SERT) with single photon emission tomography (SPECT) were prepared and evaluated. An efficient synthesis and radiolabeling of a biphenylthiol, FLIP-IDAM, 4, was accomplished. The affinity of FLIP-IDAM was evaluated by an in vitro inhibitory binding assay ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zheng P,Lieberman BP,Ploessl K,Lemoine L,Miller S,Kung HF

更新日期：2013-02-01 00:00:00

abstract：:The natural polyether ionophore antibiotics might be important chemotherapeutic agents for the treatment of cancer. In this article, the pharmacology and anticancer activity of the polyether ionophores undergoing pre-clinical evaluation are reviewed. Most of polyether ionophores have shown potent activity against the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huczyński A

更新日期：2012-12-01 00:00:00

abstract：:Several p-terphenyl compounds have been isolated from the edible Chinese mushroom Thelephora vialis. Vialinin A, a p-terphenyl compound, strongly inhibits tumor necrosis factor-α production and release. Vialinin A inhibits the enzymatic activity of ubiquitin-specific peptidase 5, one of the target molecules in RBL-2H3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yoshioka Y,Namiki D,Makiuchi M,Sugaya K,Onose J,Ashida H,Abe N

更新日期：2016-09-01 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：:By developing a new synthetic procedure for introduction of side chains onto the camptothecin ring system, we were able to achieve the preparation of a number of analogs bearing bulky, hydrophobic groups directly attached to the 7-position. These include 7-tert-butylcamptothecin, 7-benzylcamptothecin and the correspon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Manikumar G,Wadkins RM,Bearss D,Von Hoff DD,Wani MC,Wall ME

更新日期：2004-11-01 00:00:00

abstract：:Suzuki cross-coupling has been used to access a wide range of 3- and 5-substituted 2-pyrones, which show remarkable inhibitory activity against bacteria, yeasts and fungi. 3-Octenyl and 5-octenyl 2-pyrones inhibit human ovarium carcinoma (A2780) and human chronic myelogenous leukaemia (K562) cell lines at the micromol...

journal_title：Bioorganic & medicinal chemistry letters

authors： Marrison LR,Dickinson JM,Fairlamb IJ

更新日期：2003-08-18 00:00:00

abstract：:N(tau)-Aryl-histidine derivatives were synthesized using a modified one-step Cu-catalyzed coupling of aryl halides and N-acetylhistidine methyl ester. The latter is much less reactive than imidazole toward aryl halides. p-Chloroiodobenzene coupled with iodine displacement only, whereas m- and p-bromoiodobenzene both g...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yue W,Lewis SI,Koen YM,Hanzlik RP

更新日期：2004-04-05 00:00:00

abstract：:The synthesis and structure-activity relationships of zygosporamide, a known potent and selective cytotoxic natural product against SF-268 and RXF 393 cell lines, are described. The potencies of the synthetic zygosporamide are similar to those reported for the natural product toward all cancer cell lines examined with...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang Y,Zhang F,Zhang Y,Liu JO,Ma D

更新日期：2008-08-01 00:00:00

abstract：:The orexin 1 receptor (OX1R) antagonists carrying a morphinan skeleton such as YNT-707 (2) and YNT-1310 (3) showed potent and extremely high selective antagonistic activity against OX1R. In the course of our study of the essential structure of YNT-707 for high binding affinity against OX1R, we prepared derivatives of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Saitoh T,Seki K,Nakajima R,Yamamoto N,Kutsumura N,Nagumo Y,Irukayama-Tomobe Y,Ogawa Y,Ishikawa Y,Tanimura R,Yanagisawa M,Nagase H

更新日期：2019-09-15 00:00:00

abstract：:In the study, we demonstrated that freezing was able to facilitate the short DNA strand T(4)G(4) to self-assemble into a tetramolecular G-quadruplex with a low DNA concentration in the absence of any ligand, providing a fast approach to configure intermolecular G-quadruplexes. The fast formation of intermolecular G-qu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhai Q,Deng M,Xu L,Zhang X,Zhou X

更新日期：2012-01-15 00:00:00

abstract：:Glucose transporters (GLUTs) facilitate glucose uptake and are overexpressed in most cancer cells. Inhibition of glucose transport has been shown to be an effective method to slow the growth of cancer cells both in vitro and in vivo. We have previously reported on the anticancer activity of an ester derived glucose up...

journal_title：Bioorganic & medicinal chemistry letters

authors： Roberts DA,Wang L,Zhang W,Liu Y,Shriwas P,Qian Y,Chen X,Bergmeier SC

更新日期：2020-09-15 00:00:00

abstract：:Serine racemase, the enzyme responsible for d-serine synthesis in the central nervous system, has been identified as a potential therapeutic target to treat N-methyl-d-aspartate receptors-related pathologies. The search for specific inhibitors of the enzyme has revealed that serine racemase is a difficult target, with...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dellafiora L,Marchetti M,Spyrakis F,Orlandi V,Campanini B,Cruciani G,Cozzini P,Mozzarelli A

更新日期：2015-10-01 00:00:00

abstract：:The bacterial repair enzyme MutT hydrolyzes the damaged nucleotide OdGTP (the 5'-triphosphate derivative of 8-oxo-2'-deoxyguanosine; OdG), which is a known mutagen and has been linked to antibacterial action. Previous work has indicated important roles for the C8-oxygen, N7-hydrogen, and C2-exocyclic amine during OdGT...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hamm ML,McFadden EJ,Ghio M,Lindell MA,Gerien KS,O'Handley SF

更新日期：2016-04-15 00:00:00

abstract：:Protein conjugation with ubiquitin and ubiquitin-like small molecules, such as UFM1, is important for promoting cancer cell survival and proliferation. Herein, the development of the first selective micromolar inhibitor of the UBA5 E1 enzyme that initiates UFM1 protein conjugation is described. This organometallic inh...

journal_title：Bioorganic & medicinal chemistry letters

authors： da Silva SR,Paiva SL,Bancerz M,Geletu M,Lewis AM,Chen J,Cai Y,Lukkarila JL,Li H,Gunning PT

更新日期：2016-09-15 00:00:00

abstract：:In this paper, we describe the synthesis of N-(6-cyano-1,3-dimethyl-2,4-dioxo-5-substituted-1,3-dihydropyridino[2,3-d] pyrimidin-7-yl)imides 1. We will show the synthesis of 1 using both conventional heating and microwave techniques. In addition, the imide was attached to polystyrene and this immobilized imide was equ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nicewonger RB,Ditto L,Kerr D,Varady L

更新日期：2002-07-22 00:00:00

abstract：:With the aim of improving HCV protease inhibitors reported in our previous manuscripts, we synthesized and evaluated a series of 1a-based tetrapeptidyl alpha-ketoamides with additional P4 modification. The promising analog discovered through this SAR, 5a, was further derivatized at P1' or P1 position. As a result of t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yip Y,Victor F,Lamar J,Johnson R,Wang QM,Glass JI,Yumibe N,Wakulchik M,Munroe J,Chen SH

更新日期：2004-10-04 00:00:00

abstract：:ExoU is a potent virulence factor of Pseudomonas aeruginosa and is considered a potential therapeutic target. In order to discover novel ExoU inhibitors, we screened an in-house chemical library utilizing a yeast-based screening system. Some sulfonamides displayed significant activity without nonspecific cytotoxicity....

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim D,Baek J,Song J,Byeon H,Min H,Min KH

更新日期：2014-08-15 00:00:00

abstract：:We report the design, synthesis, biological activity and docking studies of series of novel pyrazolo[3,4-d]pyrimidinones as DPP-IV inhibitors in diabetes. Molecules were synthesized and evaluated for their DPP-IV inhibition activity. Compounds 5e, 5k, 5o and 6a were found to be potent inhibitors of DPP-IV enzyme. Amon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sagar SR,Agarwal JK,Pandya DH,Dash RP,Nivsarkar M,Vasu KK

更新日期：2015-10-15 00:00:00

abstract：:A novel series of N-benzenesulfonyl matrinic amine/amide and matrinic methyl ether analogues were designed, synthesized and evaluated for their in vitro anti-coxsackievirus B3 (CVB3) activities. The structure-activity relationship (SAR) studies revealed that introduction of a suitable amide substituent on position 4' ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang SG,Kong LY,Li YH,Cheng XY,Su F,Tang S,Bi CW,Jiang JD,Li YH,Song DQ

更新日期：2015-09-01 00:00:00