- Design, synthesis, and mode of action studies of a mitomycin tetramer inducing double activations with a single probe
-
We report design, synthesis, and mechanistic studies of a new mitomycin tetramer 9 along with a new mitomycin dimer 10. Mitomycin 9 is a tetramer connected by the disulfide linker 11, and easily undergoes disulfide cleavage to provide two dimeric structures 9r that each contains a single thiol probe for activations. So, tetramer 9 as a precursor of 9r was specifically targeted to undergo double activations with a single probe. A tetramer 9 was synthesized using 1 and key intermediate 11, and a dimer 10 was synthesized from 1 and diamine 12. Activation studies revealed that 9 underwent effective double activations with a single probe by nucleophiles while the reference 10 did not. Evaluations of DNA ISC formations showed that 9 generated substantial levels of DNA ISC by nucleophilic activation while the references 10 and 2 did not. The effectiveness of 9 in activation and formation of DNA ISC per probe was verified by comparing with dimers 5–8 of double activations with two probes. These findings highlighted the role of a single thiol in 9r and demonstrated the intended double activations with a single probe, which marks the first case in mitomycin studies.
- Kim, Hyoung Rae,Park, Yeon Kyeong,Lee, Sang Hyup
-
-
Read Online
- A Click Chemistry Approach to Targeted DNA Crosslinking with cis-Platinum(II)-Modified Triplex-Forming Oligonucleotides
-
Limitations of clinical platinum(II) therapeutics include systemic toxicity and inherent resistance. Modern approaches, therefore, seek new ways to deliver active platinum(II) to discrete nucleic acid targets. In the field of antigene therapy, triplex-forming oligonucleotides (TFOs) have attracted interest for their ability to specifically recognise extended duplex DNA targets. Here, we report a click chemistry based approach that combines alkyne-modified TFOs with azide-bearing cis-platinum(II) complexes—based on cisplatin, oxaliplatin, and carboplatin motifs—to generate a library of PtII-TFO hybrids. These constructs can be assembled modularly and enable directed platinum(II) crosslinking to purine nucleobases on the target sequence under the guidance of the TFO. By covalently incorporating modifications of thiazole orange—a known DNA-intercalating fluorophore—into PtII-TFOs constructs, enhanced target binding and discrimination between target and off-target sequences was achieved.
- Brown, Tom,Farrell, Nicholas P.,Hennessy, Joseph,Kellett, Andrew,McGorman, Bríonna,Molphy, Zara,Singleton, Daniel
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supporting information
(2021/12/06)
-
- Rational Design of Covalent Cobaloxime-Covalent Organic Framework Hybrids for Enhanced Photocatalytic Hydrogen Evolution
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Covalent organic frameworks (COFs) display a unique combination of chemical tunability, structural diversity, high porosity, nanoscale regularity, and thermal stability. Recent efforts are directed at using such frameworks as tunable scaffolds for chemica
- Gottschling, Kerstin,Savasci, G?kcen,Vignolo-González, Hugo,Schmidt, Sandra,Mauker, Philipp,Banerjee, Tanmay,Rovó, Petra,Ochsenfeld, Christian,Lotsch, Bettina V.
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supporting information
p. 12146 - 12156
(2020/08/06)
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- Membrane Phospholipid Analogues as Molecular Rulers to Probe the Position of the Hydrophobic Contact Point of Lysophospholipid Ligands on the Surface of G-Protein-Coupled Receptor during Membrane Approach
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When lipid mediators bind to G-protein-coupled receptors (GPCRs), the ligand first enters the lipid bilayer, then diffuses laterally in the cell membrane to make hydrophobic contact with the receptor protein, and finally enters the receptor's binding pock
- Aoki, Junken,Inoue, Asuka,Ohwada, Tomohiko,Otani, Yuko,Sayama, Misa,Sekijima, Masakazu,Uwamizu, Akiharu
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p. 1173 - 1201
(2020/04/10)
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- Cisplatin probe system and preparation method and application thereof
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The invention provides a cisplatin probe system. The cisplatin probe system has a structure shown in a formula I. The cisplatin probe system is a metal probe system capable of rapidly enriching, acquiring and analyzing platinum-bound protein groups from cells, the study of the platinum-bound protein groups is promoted, the mechanism of action of platinum-based anticancer drugs can be understood further, and a theoretical basis for drug improvement is provided.
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Paragraph 0068; 0069
(2019/04/26)
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- SUBSTITUTED 1,1'-BIPHENYL COMPOUNDS, ANALOGUES THEREOF, AND METHODS USING SAME
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The present invention includes substituted 3,3'-bis(phenoxymethyl)-1,1'-biphenyl compounds, analogues thereof, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient.
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Page/Page column 90
(2019/10/23)
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- Covalent Linkers in Antibody-Drug Conjugates and Methods of Making and Using the Same
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The present invention provides novel and advantageous compositions having a linker capable of covalently coupling one or more free thiols of an antibody. Specifically, provided herein are the molecular structures, synthetic pathways, coupling mechanisms, and applications thereof as used in an antibody-drug conjugate (ADC).
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Paragraph 0192; 0193
(2018/03/25)
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- Traceable platinum(II) complexes with alkylene diamine-derived ligands: synthesis, characterization and in vitro studies
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Diiodido- (6a/6b) and dichloridoplatinum(II) complexes (7a/7b) with fluorescent ligands 2-[(2-aminoethyl)amino]ethyl-2-(methylamino)benzoate (5a) and 2-amino-1-(aminoethyl)ethyl-2-(methylamino)benzoate (5b) were prepared and characterized by elemental ana
- Walther, Till,Herzog, Renate,Kalu?erovi?, Milena R.,Wagner, Christoph,Schmidt, Harry,Kalu?erovi?, Goran N.
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p. 243 - 257
(2018/02/14)
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- LINKER-DRUG AND ANTIBODY-DRUG CONJUGATE (ADC) EMPLOYING THE SAME
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A linker-drug represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof is provided. In formula (I), C is a conjugator, L is a linker unit, D is a toxin unit, and n is an integer ranging from 1 to 4. The structure of the conjugator is represented by formula (II). In formula (II), X is a leaving group, each of R1 and R2 is independently a single bond or —NH—, and Z is substituted aryl, heteroaryl, linear alkyl, cycloalkyl, heterocycloalkyl, or a combination thereof. The antibody is conjugated to the linker unit through a cysteine residue of the antibody. An antibody-drug conjugate (ADC) employing the above linker-drug is also provided.
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Paragraph 0210-0212
(2018/07/05)
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- NEW ANTIBACTERIAL PRODUCTS
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The invention provides novel antibacterial compounds of formulae IA, IB and IC as defined herein. Optionally, the antibacterial compounds can be bonded to a delivery agent that is capable of bonding to one or more structures on a bacterial cell membrane. The invention also provides the use of such compounds in treating or preventing bacterial infections, and processes for their synthesis.
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Page/Page column 77
(2018/09/28)
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- AUTOPHAGY-INHIBITING COMPOUNDS AND USES THEREOF
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The present disclosure describes a compound for use in the treatment of cancer, infectious disease, and autoimmune disorders. The compounds herein can inhibit autophagy in an affected cell to promote cell death. Further, the compound can be used to overco
- -
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Paragraph 00217
(2017/04/04)
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- Synthesis of Enantiomeric Aminoalkylcarbamoylphosphonates and Their Evaluation as Dual-Action Anticancer MMP and Carbonic Anhydrase Inhibitors
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Carbamoylphosphonates (CPOs) have recently been identified as extracellular in vivo active inhibitors of the cancer and metastasis-promoting extracellular enzymes, carbonic anhydrases (CAs) IX and XII, and matrix metalloproteinase-2 (MMP-2). This article
- Veerendhar, Ainelly,Cohen, Shmuel,Frant, Julia,Supuran, Claudiu T.,Reich, Reuven,Breuer, Eli
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p. 257 - 269
(2015/07/15)
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- Synthesis and studies of anticancer properties of lupane-type triterpenoid derivatives containing a cisplatin fragment
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Both betulinic acid 1 and cisplatin are promising antitumor agents, which induce apoptotic cell death of cancer cells. In the present investigation a new series of betulinic acid-cisplatin conjugates were synthesized and cytotoxicity and selectivity were assessed against five different tumor cell lines. The aim was to combine two structural units, both related with apoptosis induction. The derivatives exerted a dose-dependent antiproliferative action at micromolar concentrations and the effect of these structural variations on anticancer activity was studied and discussed. Several compounds revealed significant antitumor activity, as the most active substance 3-O-acetylbetulinic (2-(2-aminoethyl)aminoethyl)amide (IC50 = 1.30-2.24 μM). Interestingly, Betulinic acid-cisplatin conjugates were less cytotoxic than the precursors.
- Emmerich, Daniel,Vanchanagiri, Kranthi,Baratto, Leopoldo C.,Schmidt, Harry,Paschke, Reinhard
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p. 460 - 466
(2014/03/21)
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- BORON CONTAINING POLYBASIC BACTERIAL EFFLUX PUMP INHIBITORS AND THERAPEUTICS USES THEREOF
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Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and theft methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent
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Page/Page column 47
(2012/08/28)
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- FUNCTIONALIZED SUBSTRATE AND USES THEREOF
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The present invention is directed towards proposing ligands of formula: and is also directed towards a substrate at the surface of which is immobilized at least one unit of formula:
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Page/Page column 6-7
(2011/10/31)
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- THIENOPYRIMIDINES CONTAINING A SUBSTITUTED ALKYL GROUP FOR PHARMACEUTICAL COMPOSITIONS
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The present invention relates to novel thienopyhmidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
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Page/Page column 38
(2011/09/30)
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- THIENOPYRIMIDINES CONTAINING A SUBSTITUTED ALKYL GROUP FOR PHARMACEUTICAL COMPOSITIONS
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The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
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Page/Page column 13
(2011/09/20)
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- ANTIMICROBIAL POLYMERS
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The invention generally relates to novel polymers (SMAMPs) and their syntheses and use. The polymers exhibit promising properties of AMPs. In particularly, for example, a ring-opening metathesis polymerization (ROMP) platform was developed that allows syntheses of SMAMPs that employ a minimum number of norbornene-based building blocks and/or enable easy and independent variation of hydrophobic and hydrophilic groups in the monomer units and/or along the polymeric backbone to finetune and select desirable properties of the polymers.
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Page/Page column 47; 49
(2010/12/29)
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- CARJBAMOYLPHOSPHONATES AS INHIBITORS AND USES THEREOF
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The present invention relates to novel metalloproteinase inhibitors having an aryloxybenzenesulfonamide moiety and a carbamoylphosphonic acid moiety, to pharmaceutical compositions comprising them, and to their uses in the prevention and/or treatment of disease or disorder associated with MMP.
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Page/Page column 42
(2010/08/18)
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- 2-[2-Substituted-3-(3,4-dichlorobenzylamino)propylamino]-1H-quinolin-4-ones as Staphylococcus aureus methionyl-tRNA synthetase inhibitors
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New analogues of 2-[2-substituted-3-(3,4-dichlorobenzylamino)propylamino]quinolin-4-ones, 26a, 26b, 31a-e, 34, 35, 38 and 40, have been synthesized and evaluated against Staphylococcus aureus methionyl-tRNA synthetase. All of the synthesized compounds were less active than the reference compound 2. The compounds were also screened against various strains of S. aureus and Enterococci for their antibacterial activities. Among the compounds, 26b, 31c and 31e displayed significant inhibitory properties against various strains of Enterococci compared to compound 2.
- Farhanullah,Kang, Taehee,Yoon, Eun-Jung,Choi, Eun-Chil,Kim, Sunghoon,Lee, Jeewoo
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experimental part
p. 239 - 250
(2009/04/07)
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- POLYBASIC BACTERIAL EFFLUX PUMP INHIBITORS AND THERAPEUTIC USES THEREOF
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Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.
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Page/Page column 51; 52
(2009/01/24)
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- Inhibitors of DNA Methyltransferase
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The invention relates to the inhibition of DNA methyltransferase isoforms DNMT1 and DNMT3b2. The invention provides compounds and methods for inhibiting DNMT1 and DNMT3b2.
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Page/Page column 33
(2008/12/05)
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- Compounds, compositions and methods
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Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
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Page/Page column 27
(2008/06/13)
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- Efficient synthesis of immolative carbamate dendrimer with olefinic periphery
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An efficient synthetic strategy for immolative carbamate dendrons and dendrimers is described that requires no protection/deprotection in the convergent growth step. 1,3-Diamino-2-propanol was used as AB2 building block and 4-nitrophenyl chloro
- Lee, Jeong-Kyu,Suh, Young-Woong,Kung, Mayfair C.,Downing, Christopher M.,Kung, Harold H.
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p. 4919 - 4923
(2008/02/08)
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- Optimized relaxivity and specificity hepatobiliary MRI contrast agent
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An adamantane functionalized magnetic resonance imaging (MRI) contrast agent has been synthesized, and shows high liver specificity, prolonged retention time in both the liver and kidneys, the highest relaxivity among clinical contrast agents, high water solubility, thermodynamic stability, signal intensity enhancement, hepatocellular uptake, and low osmolality and toxicity.
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Page/Page column 8
(2008/06/13)
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- Acylated aminopropanediols and analogues and therapeutic uses thereof
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The invention relates to novel acylated aminopropanediols and the nitrogen and sulfur analogues thereof, pharmaceutical compositions comprising same, therapeutic uses thereof, in particular for the treatment of cerebral ischemia. The invention also provides a method of preparing said derivatives.
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Page/Page column 22
(2008/06/13)
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- Therapeutic use of acyl glycerols and the nitrogen- and sulphur- containing analogues thereof
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The invention relates to the use of acyl glycerols and the nitrogen- and sulfur-containing analogues thereof in the therapeutic field, particularly in human health. The inventive compounds have advantageous pharmacological properties and are particularly of use for the prevention or treatment of neurodegenerative diseases.
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Page/Page column 37-38
(2008/06/13)
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- Uses of acylated aminopropanediols and sulphur and nitrogen analogues of same f
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The invention relates to the use of molecules, particularly in the fields of human and veterinary health and cosmetics. The inventive compounds are acylated aminopropanediols and the nitrogen- and sulfur-containing analogues thereof and have advantageous pharmacological and cosmetic properties. In particular, the inventive compounds can be used to prevent and/or treat dyslipidemias, cardiovascular diseases, syndrome X, restenosis, diabetes, obesity, hypertension, some cancers, dermatological diseases, and, in the field of cosmetics, to combat skin ageing and the effects of same, in particular the development of wrinkles and the like.
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Page/Page column 24
(2008/06/13)
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- HYDANTOIN DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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This invention relates to compounds of Formula (1) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF- or combinations thereof.
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Page/Page column 106
(2008/06/13)
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- Surface plasmon resonance imaging measurements of the inhibition of Shiga-like toxin by synthetic multivalent inhibitors
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A variety of new methodologies to pattern biomolecules on surfaces and to detect binding events are currently being developed for high-throughput assay applications. Carbohydrates serve as attachment sites for toxins, bacteria, and viruses. Immobilized ca
- Kanda, Vishal,Kitov, Pavel,Bundle, David R.,McDermott, Mark T.
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p. 7497 - 7504
(2008/02/04)
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- Small molecule inhibitors of dynamin I GTPase activity: Development of dimeric tyrphostins
-
Dynamin I is a GTPase enzyme required for endocytosis and is an excellent target for the design of potential endocytosis inhibitors. Screening of a library of tyrphostins, in our laboratory, against the GTPase activity of dynamin I gave rise to a ìèpotent lead, 2-cyano-3-(3,4- dihydroxyphenyl)thioacrylamide (1, IC50 70 μM). Our initial investigations suggested that only the dimeric form of 1 displayed dynamin I GTPase inhibitory activity. Subsequent synthetic iterations were based on dimeric analogues and afforded a number of small molecules, low μM potent, inhibitors of dynamin I GTPase, in particular, symmetrical analogues with a minimum of two free phenolic -OHs: catechol-acrylamide (9) (IC50 = 5.1 ± 0.6 μM), its 3,4,5-trihydroxy congener (10) (IC50 = 1.7 ± 0.2 μM), and the corresponding 3-methyl ether (11) (IC 50 = 9 ± 3 μM). Increasing the length of the central alkyl spacer from ethyl to propyl (22-24) afforded essentially identical activity with IC50's of 1.7 ± 0.2, 1.7 ± 0.2, and 5 ± 1 μM, respectively. No decrease in activity was noted until the introduction of a hexyl spacer. Our studies highlight the requirement for two free amido NHs with neither the mono-N-methyl (86) nor the bis-N-methyl (87) analogues inhibiting dynamin I GTPase. A similar effect was noted for the removal of the nitrile moieties. However, modest potency was observed with the corresponding ester analogues of 9-11: ethyl ester (90), propyl ester (91), and butyl ester (92), with IC50's of 42 ± 3, 38 ± 2, and 61 ± 2 μM, respectively. Our studies reveal the most potent and promising dynamin I GTPase inhibitor in this series as (22), which is also known as BisT.
- Hill, Timothy,Odell, Luke R.,Edwards, Jennifer K.,Graham, Mark E.,McGeachie, Andrew B.,Rusak, Jenny,Quan, Annie,Abagyan, Ruben,Scott, Janet L.,Robinson, Phillip J.,McCluskey, Adam
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p. 7781 - 7788
(2007/10/03)
-
- CEPHEM COMPOUNDS
-
The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl or hydroxy (lower) alkyl, and R2 is hydrogen or amino protecting group, or R1 and R2 are bonded together and form lower a
- -
-
Page/Page column 41-42
(2010/02/11)
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- Chemokine receptor binding heterocyclic compounds with enhanced efficacy
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The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
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-
-
- Synthesis and Esterolytic Activity of Catalytic Peptide Dendrimers
-
Peptide dendrimers were prepared by solid-phase peptide synthesis. Monomeric dendrimers were first obtained by assembly of a hexa-peptide sequence containing alternate standard a-amino acids with diamino acids as branching units. The monomeric dendrimers were then dimerized by disulfide-bridge formation at the core cysteine. The synthetic strategy is compatible with functional amino acids and different diamino acid branching units. Peptide dendrimers composed of the catalytic triad amino acids histidine, aspartate, and serine catalyzed the hydrolysis of N-methylquinolinium salts when the histidine residues were placed at the outermost position. The dendrimer-catalyzed hydrolysis of 7-isobutyryl-N-methylquinolinium followed saturation kinetics with a rate constant of catalysis/rate constant without catalysis (kcat/kuncat) value of 3350 and a rate constant of catalysis/Michaelis constant (kcat/KM) value 350-fold larger than the second-order rate constant of the 4-methylimidazole-catalyzed reaction; this corresponds to a 40-fold rate enhancement per histidine side chain. Catalysis can be attributed to the presence of histidine residues at the surface of the dendrimers.
- Lagnonx, David,Delort, Estelle,Douat-Casassus, Celine,Esposito, Annamaria,Reymond, Jean-Louis
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p. 1215 - 1226
(2007/10/03)
-
- Synthesis and properties of polyaromatic dendrimers possessing a repetitive amide-ester coupling sequence
-
A series of novel polyaromatic dendrimers that feature tris-(2-ethylamino)amine as the central core unit has been synthesized up to the third generation by employing a convergent growth strategy. The building blocks 1,3-diamino-2-hydroxypropane and 4-carb
- Romagnoli, Barbara,Ashton, Peter R.,Harwood, Laurence M.,Philp, Douglas,Price, David W.,Smith, Melanja H.,Hayes, Wayne
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p. 3975 - 3988
(2007/10/03)
-
- Bis-2-oxo amide triacylglycerol analogues: A novel class of potent human gastric lipase inhibitors
-
A novel class of potent human gastric lipase inhibitors, bis-2-oxo amide triacylglycerol analogues, was developed. These analogues of the natural substrate of lipases were prepared starting from 1,3-diaminopropan-2-ol. They were designed to contain the 2-
- Kotsovolou,Chiou,Verger,Kokotos
-
p. 962 - 967
(2007/10/03)
-
- AZETIDINONE DERIVATIVES AS BETA-LACTAMASE INHIBITORS
-
New 2-oxo-1-azetidine sulfonic acid derivatives with an aminoalkyl substituted "anti" (E-isomer) oxyimino group in the acylamino substituent at the 3 position of the monobactam ring. These compounds are potent inhibitors of bacterial beta-lactamases. These compounds can be used in combination with beta-lactam antibiotics to increase the effectiveness of the beta-lactam antibiotics in fighting infection caused by beta-lactamase producing bacteria.
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-
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- Inhibitors of retroviral proteases
-
The present invention relates to compounds of the formula I STR1 wherein A, Y, R2, R3, R4, R5, R6, l, m and the corresponding radicals labeled with * are defined as stated in the description, a process for their preparation and their use for the inhibition of retroviral proteases.
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-
- Synthesis of RNAse active site model systems using a steroid template
-
An RNAse active site model system is described. The rigid steroid backbone is used as the template on which guanidinium and imidazole moieties, necessary for the transesterification/cleavage. are assembled. By changing the stereochemistry at C11 of 2, and
- Oost, Thorsten,Kalesse, Markus
-
p. 8421 - 8438
(2007/10/03)
-
- Guanosine-specific DNA damage by a Co(II)·bithiazole complex
-
A bithiazole derivative structurally related to the bithiazole moiety of bleomycin (BLM) A2 was prepared. This derivative contained a 2-(1,3-diaminopropyl) substituent, rather than the 2-(2-aminoethyl) substituent normally present in BLM, in or
- Kane,Sasaki,Hecht
-
p. 9107 - 9118
(2007/10/02)
-
- Platinum(II) Complexes with Porphyrin Ligands: Synthesis and Synergisms in the Photodynamic Tumor Therapy
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Twelve porphyrin ligands (2-5, 8, 13-16, 19, 27, 28) and their platinum(II) complexes (29-40) were synthesized and characterized.Nine of the porphyrins are derived from hemin, and three are based on tetraphenylporphyrin.The ligands were transformed into diamine-dicarboxylatoplatinum(II) complexes and diamine-dichloroplatinum(II) complexes.The antitumor activity in the photodynamic therapy of the ligands and their complexes was tested in vitro towards the MDA-MB-231 mammary carcinoma cell line.The results obtained showed an additive effect of the photodynamic activity of the porphyrin skeleton when irradiated with visible red light and the cytotoxic activity of the platinum moiety in the complexes. - Key Words: Porphyrins/ Platinum(II) complexes/ Photodynamic therapy/ Antitumor activity
- Brunner, Henri,Obermeier, Herbert,Szeimies, Rolf-Markus
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p. 173 - 182
(2007/10/02)
-
- Synthesis of nitroimidazole substituted 3,3,9,9-tetramethyl-4,8-diazaundecane-2,10-dione dioximes (propylene amine oximes, PnAOs): Ligands for technetium-99m complexes with potential for imaging hypoxic tissue
-
A series of 2-substituted-1,3-diaminopropanes (1b-1f, 1h) have been synthesized as precursors to nitroimidazole-substituted 3,3,9,9-tetramethyl-4,8-diazaundecane-2,10-dione dioxime (21b, 21d, 21e and 26a-26c) (Propylene Amine Oxime, PnAO) ligands. 3-Chlor
- Ramalingam, Kondareddiar,Raju, Natarajan,Nanjappan, Palaniappa,Nowotnik, David P.
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p. 2875 - 2894
(2007/10/02)
-
- Cyclic amidinyl and cyclic guanidinyl thio carbapenems
-
Compounds of the formula: STR1 and the pharmaceutically acceptable salts thereof wherein X is STR2 wherein each R is hydrogen or alkyl of 1 to 6 carbon atoms are disclosed. The compounds are useful as antibiotics.
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