Synthesis and biological evaluation of methoxyphenyl porphyrin derivatives as potential photodynamic agents.

abstract：:Focusing on alpha-pyridoin (1, 1,2-di(2-pyridyl)-1,2-ethenediol) as the lead compound of the novel antioxidative enediol, we synthesized 5,5'- or 6,6'-bis-substituted derivatives of 1 from disubstituted pyridines. The antioxidant activity of 1 and its synthetic derivatives 2-7 was evaluated by DPPH (1,1-diphenyl-2-pic...

journal_title：Bioorganic & medicinal chemistry

authors： Hatanaka M,Takahashi K,Nakamura S,Mashino T

更新日期：2005-12-15 00:00:00

abstract：:Abnormal β-amyloid peptide accumulation and aggregation is considered to be responsible for the formation and cerebral deposition of senile plaques in the brains of patients with Alzheimer's disease (AD). Inhibition of the formation of β-amyloid (Aβ) fibrils would be an attractive therapeutic target for the treatment ...

journal_title：Bioorganic & medicinal chemistry

authors： Richard T,Poupard P,Nassra M,Papastamoulis Y,Iglésias ML,Krisa S,Waffo-Teguo P,Mérillon JM,Monti JP

更新日期：2011-05-15 00:00:00

abstract：:In this study, both pure DMPC and DMPC/cholesterol mixed membrane monolayer were built to compare the physical-chemical properties and dynamics properties through molecular dynamics simulation and normal-mode analysis. The results show that the addition of cholesterol decreases the area of per molecule of membrane, in...

journal_title：Bioorganic & medicinal chemistry

authors： Liu J,Yang L

更新日期：2006-04-01 00:00:00

abstract：:6-Benzofuryl-, styryl, benzyl, and furfurylpurines as well as 6-[1(3H)-isobenzofuranylidenemethyl]purines have been synthesized and their activities against Mycobacterium tuberculosis (Mtb) determined. Several compounds displayed profound antimycobacterial activity in combination with low toxicity towards mammalian ce...

journal_title：Bioorganic & medicinal chemistry

authors： Braendvang M,Bakken V,Gundersen LL

更新日期：2009-09-15 00:00:00

abstract：:Focused libraries of multi-substituted epidithiodiketopiperazines (ETP) were prepared and evaluated for efficacy of inhibiting the nucleocapsid protein function of the Feline Immunodeficiency Virus (FIV) as a model for HIV. This activity was compared and contrasted to observed toxicity utilising an in-vitro cell cultu...

journal_title：Bioorganic & medicinal chemistry

authors： Asquith CRM,Sil BC,Laitinen T,Tizzard GJ,Coles SJ,Poso A,Hofmann-Lehmann R,Hilton ST

更新日期：2019-09-15 00:00:00

abstract：:Cell invasion and migration are required for the parent solid tumor cells to metastasize to distant organs. Microtubules form a polarized network, enabling organelle and protein movement throughout the cell. Cytoskeletal elements coordinately regulate cell's motility, adhesion, migration, exocytosis, endocytosis, and ...

journal_title：Bioorganic & medicinal chemistry

authors： Abdel Bar FM,Khanfar MA,Elnagar AY,Badria FA,Zaghloul AM,Ahmad KF,Sylvester PW,El Sayed KA

更新日期：2010-01-15 00:00:00

abstract：:Esa1 (essential Sas2-related acetyltransferase 1) and Tip60 (HIV-1 TAT-interactive protein, 60 kDa) are key members of the MYST family of histone acetyltransferases (HATs) and play important functions in many cellular processes. In this work, we designed, synthesized and evaluated a series of substrate-based analogs f...

journal_title：Bioorganic & medicinal chemistry

authors： Wu J,Xie N,Wu Z,Zhang Y,Zheng YG

更新日期：2009-02-01 00:00:00

abstract：:Gangjee et al. recently reported a novel series of 2-amino-4-methyl-5-phenylethyl substituted-7-benzyl-pyrrolo[2,3-d]pyrimidines, some of which exhibited two digit nanomolar antitumor and antimitotic activity and were not subject to P-glycoprotein (Pgp) or multidrug resistance protein 1 (MRP1) mediated tumor resistanc...

journal_title：Bioorganic & medicinal chemistry

authors： Gangjee A,Namjoshi OA,Keller SN,Smith CD

更新日期：2011-07-15 00:00:00

abstract：:Novel ent-kaurane glucosides were synthezised by a Koenigs-Knorr reaction between C17 and C19 alcohols derived from kaurenoic acid and 2,3,4,6-tetra-O-acetyl-glucopyranosyl bromide, followed by the hydrolysis of the acetates. Main products were assayed in vitro and in vivo against blood trypomastigote forms of Trypano...

journal_title：Bioorganic & medicinal chemistry

authors： Batista R,Humberto JL,Chiari E,de Oliveira AB

更新日期：2007-01-01 00:00:00

abstract：:Selective targeting of RNA has become a recent priority in drug design strategies due to the emergence of retroviruses, the need for new antibiotics to counter drug resistance, and our increased awareness of the essential role RNA and RNA structures play in the progression of disease. Most organic compounds known to s...

journal_title：Bioorganic & medicinal chemistry

authors： Li K,Fernandez-Saiz M,Rigl CT,Kumar A,Ragunathan KG,McConnaughie AW,Boykin DW,Schneider HJ,Wilson WD

更新日期：1997-06-01 00:00:00

abstract：:We describe a new route for the synthesis of (S)-N-Boc-5-oxaproline. This building block is a key element for the chemical synthesis of proteins with the α-ketoacid-hydroxylamine (KAHA) ligation. The new synthetic pathway to the enantiopure oxaproline is based on a chiral amine mediated enantioselective conjugate addi...

journal_title：Bioorganic & medicinal chemistry

authors： Murar CE,Harmand TJ,Bode JW

更新日期：2017-09-15 00:00:00

abstract：:Luteolin, 5,7-dihydroxy-2-(3,4-dihydroxyphenyl)-4H-chromen-4-one, has been proposed and proved to be a novel dopamine transporter (DAT) activator. In order to develop this potential of luteolin, a series of novel luteolin derivatives were designed, synthesized, and evaluated for their DAT agonistic activities, utilizi...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang J,Liu X,Lei X,Wang L,Guo L,Zhao G,Lin G

更新日期：2010-11-15 00:00:00

abstract：:Inhibition of group IIA secreted phospholipase A2 (GIIA sPLA2) has been an important objective for medicinal chemists. We have previously shown that inhibitors incorporating the 2-oxoamide functionality may inhibit human and mouse GIIA sPLA2s. Herein, the development of new potent inhibitors by molecular docking calcu...

journal_title：Bioorganic & medicinal chemistry

authors： Vasilakaki S,Barbayianni E,Leonis G,Papadopoulos MG,Mavromoustakos T,Gelb MH,Kokotos G

更新日期：2016-04-15 00:00:00

abstract：:Bioactive compounds present in grapefruit juice are known to increase the bioavailability of certain medications by acting as potent CYP 3A4 inhibitors. An efficient technique has been developed for isolation and purification of three furocoumarins. The isolated compounds have been tested for the inhibition of human C...

journal_title：Bioorganic & medicinal chemistry

authors： Girennavar B,Poulose SM,Jayaprakasha GK,Bhat NG,Patil BS

更新日期：2006-04-15 00:00:00

abstract：:In order to find novel and environmental friendly insecticides targeting the ryanodine receptor, three series of novel phthalamides containing heptafluoroisopropyl group, low fluorine atoms group and non-fluorine group were designed and synthesized. 35 novel structures of three series were obtained. Insecticidal activ...

journal_title：Bioorganic & medicinal chemistry

authors： Chen Y,Li Y,Pan L,Liu J,Wan Y,Chen W,Xiong L,Yang N,Song H,Li Z

更新日期：2014-11-15 00:00:00

abstract：:2-Hydrazinyl-1,4,5,6-tetrahydropyrimidin-5-ol dihydrochloride 2, as well as 2-hydrazinyl-4,5-dihydro-1H-imidazole dihydrochloride 1, was synthesized as metal-free DNA cleaving agent. Agarose gel electrophoresis was used to assess the plasmid pUC 19 DNA cleavage activities in the presence of 1 and 2. DNA cleavage effic...

journal_title：Bioorganic & medicinal chemistry

authors： Shao Y,Ding Y,Jia ZL,Lu XM,Ke ZH,Xu WH,Lu GY

更新日期：2009-07-01 00:00:00

abstract：:Concise total syntheses of (R)- and (S)-argentilactone have been developed via enantioselective catalytic allylation (ECA) and ring-closing metathesis pathways (four steps, 39% overall yield and 82-84% ee) from 2-octynal and their in vitro activity against cancer cells is described. ...

journal_title：Bioorganic & medicinal chemistry

authors： de Fatima A,Kohn LK,Antônio MA,de Carvalho JE,Pilli RA

更新日期：2004-10-15 00:00:00

abstract：:To clarify the structure-activity relationships of flavonoids for nitric oxide (NO) production inhibitory activity, we examined the inhibitory effects of 73 flavonoids on NO production in lipopolysaccharide-activated mouse peritoneal macrophages. Among those flavonoids, apigenin (IC(50)=7.7 microM), diosmetin (8.9 mic...

journal_title：Bioorganic & medicinal chemistry

authors： Matsuda H,Morikawa T,Ando S,Toguchida I,Yoshikawa M

更新日期：2003-05-01 00:00:00

abstract：:A series of benzazolone compounds were synthesized utilizing benzoxazolinonic and benzothiazolinonic heterocycles as the building unit. The antioxidant activity of these compounds was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the presence of CuSO(4) or 2,2'-azobis(2-amidinopro...

journal_title：Bioorganic & medicinal chemistry

authors： Yekini I,Hammoudi F,Martin-Nizard F,Yous S,Lebegue N,Berthelot P,Carato P

更新日期：2009-11-15 00:00:00

abstract：:DNA methylation is an important epigenetic modification catalyzed by DNA methyltransferases (DNMTs). Abnormal expression of endogenous DNMTs in human causes alterations in the genome methylation patterns which subsequently lead to the development of cancers. Thus detection of endogenous DNMT activities and efficient i...

journal_title：Bioorganic & medicinal chemistry

authors： Zhu B,Ge J,Yao SQ

更新日期：2015-06-15 00:00:00

abstract：:Optimization of a new series of S-adenosyl-L-homocysteine hydrolase (AdoHcyase) inhibitors based on non-adenosine analogs led to very potent compounds 14n, 18a, and 18b with IC50 values of 13 ± 3, 5.0 ± 2.0, and 8.5 ± 3.1 nM, respectively. An X-ray crystal structure of AdoHcyase with NAD(+) and 18a showed a novel open...

journal_title：Bioorganic & medicinal chemistry

authors： Nakao A,Suzuki H,Ueno H,Iwasaki H,Setsuta T,Kashima A,Sunada S

更新日期：2015-08-01 00:00:00

abstract：:A set of 116 structurally very diverse compounds, mainly drugs, was characterized by 1630 molecular descriptors. The biological property modelled in this study was the transdermal permeability coefficient logK(p). The main objective was to find a limited set of suitable model compounds for skin penetration studies. Th...

journal_title：Bioorganic & medicinal chemistry

authors： Baert B,Deconinck E,Van Gele M,Slodicka M,Stoppie P,Bodé S,Slegers G,Vander Heyden Y,Lambert J,Beetens J,De Spiegeleer B

更新日期：2007-11-15 00:00:00

abstract：:Human dipeptidyl peptidase I (hDPPI, cathepsin C, EC 3.4.14.1) is a novel putative drug target for the treatment of inflammatory diseases. Using 1 as a starting point (IC50>10 microM), we have improved potency by more than 500-fold and successfully identified novel inhibitors of DPPI via screening of a one-bead-two-co...

journal_title：Bioorganic & medicinal chemistry

authors： Bondebjerg J,Fuglsang H,Valeur KR,Kaznelson DW,Hansen JA,Pedersen RO,Krogh BO,Jensen BS,Lauritzen C,Petersen G,Pedersen J,Naerum L

更新日期：2005-07-15 00:00:00

abstract：:Fully N- and O-sulfated homooligomers from octamer to nonadecamer of tyrosine were obtained as their sodium salts, aO3S-[Tyr(SO3Na)]n-ONa (n = 8-19), from reaction mixtures of tyrosine with sulfur trioxide trimethylamine and pyridine comlexes, respectively, in pyridine. Their anti-HIV activity increased along with the...

journal_title：Bioorganic & medicinal chemistry

authors： Ueki M,Watanabe S,Saitoh T,Nakashima H,Yamamoto N,Ogawara H

更新日期：2001-02-01 00:00:00

abstract：:Searching for new substances with antileishmanial activity, we synthesized and evaluated a series of α,α-difluorohydrazide and α,α-difluoramides against Leishmania amazonensis arginase (LaArg). Four α,α-difluorohydrazide derivatives showed activity against LaArg with Ki in the range of 1.3-26 μM. The study of the kine...

journal_title：Bioorganic & medicinal chemistry

authors： Crizanto de Lima E,Castelo-Branco FS,Maquiaveli CC,Farias AB,Rennó MN,Boechat N,Silva ER

更新日期：2019-09-01 00:00:00

abstract：:A quencher-free molecular beacon capable of generating pyrene excimer fluorescence has been constructed using strategically positioned pyrene-UNA monomers. Hybridization of a fully complementary RNA target was accompanied by a pyrene excimer emission increase of more than 900%, and detection of RNA in living cells was...

journal_title：Bioorganic & medicinal chemistry

authors： Karlsen KK,Okholm A,Kjems J,Wengel J

更新日期：2013-10-15 00:00:00

abstract：:The fungus Aspergillus japonicus MF275 produces himeic acid A (1), containing a 4-pyrone ring, along with its congeners, himeic acids B (2) and C (3). During culture, 1 was gradually converted to 3, the corresponding 4-pyridone derivative. A study of the relationship between the culture pH and the fungal metabolites s...

journal_title：Bioorganic & medicinal chemistry

authors： Katsuki A,Kato H,Tahara Y,Hashimoto M,Fujii I,Tsukamoto S

更新日期：2018-05-01 00:00:00

abstract：:Fourteen hybrids of farnesylthiosalicylic acid (FTS) with various diamines were synthesized and biologically evaluated. It was found that FTS-monoamide molecules (10a-g) displayed strong anti-proliferative activity against seven human cancer cell lines, superior to FTS and FTS-bisamide compounds (11a-g). The mono-amid...

journal_title：Bioorganic & medicinal chemistry

authors： Ling Y,Wang Z,Zhu H,Wang X,Zhang W,Wang X,Chen L,Huang Z,Zhang Y

更新日期：2014-01-01 00:00:00

abstract：:The cyclohexyl piperazine 1 (1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydro-naphthalen-1-yl)-propyl]-piperazine) has been shown to be a potent and selective sigma-2 receptor ligand. In the present study, we prepared [(11)C]1 by O-alkylation of the phenolic precursor 2 with [(11)C]CH(3)I. [(11)C]1 was obtained in a 29...

journal_title：Bioorganic & medicinal chemistry

authors： Kassiou M,Dannals RF,Liu X,Wong DF,Ravert HT,Scheffel UA

更新日期：2005-06-01 00:00:00

abstract：:A facile synthesis of dl-6,10,14-trimethylpentadecan-2-ol (1) a pheromone component of rice moth, Corcyra cephalonica Stainton and 5,9,13-trimethyltetradecanoic acid (2) a component of marine sponge, Cinachyrella alloclada Uliczka, using a common, intermediate, hexahydrofarnesol is accomplished. The salient features f...

journal_title：Bioorganic & medicinal chemistry

authors： Rane SS,Chadha MS,Mamdapur VR

更新日期：1993-12-01 00:00:00