- Synthesis and biological activity of imidazole based 1,4-naphthoquinones
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Design and development of drugs in multi-drug resistant (MDR) infections have been of growing interest. We report the syntheses, and antibacterial and antifungal activities of imidazole-based 1,4-naphthoquinones (I-1toI-4; 1-alkyl-2-methyl-1H-naphtho[2,3-d]imidazole-4,9-dione (alkyl = methyl to butyl)) and their precursors (B-3;N-(3-chloro-1,-dioxo-1,4-dihydronaphthalen-2-yl)acetamide) andA-1toA-4;N-(3-(alkylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)acetamide (alkyl = methyl to butyl). Crystal structures ofB-3A-1toA-3andI-2toI-4were obtained through single crystal X-ray diffraction experiments. Electronic structure and charge distribution have further been characterized with the use of Density Functional Theory. Seven of these derivatives display a broad spectrum of antibacterial activity against few selected bacterial strains (Gram-positive and Gram-negative). As demonstrated MIC values withB-2andB-3against bacterial isolates were 8-64 μg ml?1and those against pathogenic yeast,C. albicans, were observed in the range of 128-256 μg ml?1. MIC data of these derivatives suggest them to be promising against pathogens.
- Chakravarty, Debamitra,Choudhari, Dinkar,Gejji, Shridhar P.,Gonnade, Rajesh,Lande, Dipali N.,Puranik, Vedavati G.,Rao, Pradeep Kumar,Salunke-Gawali, Sunita,Satpute, Surekha,Shaikh, Samir R.
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- Functionalized Dioxonaphthoimidazoliums: A Redox Cycling Chemotype with Potent Bactericidal Activities against Mycobacterium tuberculosis
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Disruption of redox homeostasis in mycobacteria causes irreversible stress induction and cell death. Here, we report the dioxonaphthoimidazolium scaffold as a novel redox cycling antituberculosis chemotype with potent bactericidal activity against growing and nutrient-starved phenotypically drug-resistant nongrowing bacteria. Maximal potency was dependent on the activation of the redox cycling quinone by the positively charged scaffold and accessibility to the mycobacterial cell membrane as directed by the lipophilicity and conformational characteristics of the N-substituted side chains. Evidence from microbiological, biochemical, and genetic investigations implicates a redox-driven mode of action that is reliant on the reduction of the quinone by type II NADH dehydrogenase (NDH2) for the generation of bactericidal levels of the reactive oxygen species (ROS). The bactericidal profile of a potent water-soluble analogue 32 revealed good activity against nutrient-starved organisms in the Loebel model of dormancy, low spontaneous resistance mutation frequency, and synergy with isoniazid in the checkerboard assay.
- Cook, Gregory M.,Dick, Thomas,Fridianto, Kevin T.,Go, Mei-Lin,Hards, Kiel,Lam, Yulin,Li, Ming,Negatu, Dereje A.
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supporting information
p. 15991 - 16007
(2021/11/16)
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- Use of naphthoquinone derivative as inhibitor for IDO1 and/or TDO
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The invention discloses a use of a naphthoquinone derivative as an inhibitor for IDO1 and/or TDO. The derivative is shown as a general formula (I), and the definition of each substituent is detailed in the specification. The compound represented by the general formula (I) has an inhibitory effect on indoleamine-2,3-dioxygenase 1 (IDO1) and/or tryptophan-2,3-dioxygenase (TDO), and can be used for treating diseases with IDO1- and/or TDO-mediated tryptophan metabolism as pathological features, including but not limited to tumors, autoimmune diseases, infectious diseases, Alzheimer's disease, depression, and anxiety disorder.
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Paragraph 0278-0279
(2020/01/31)
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- Antimalarial N1, N3-Dialkyldioxonaphthoimidazoliums: Synthesis, Biological Activity, and Structure-activity Relationships
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Here we report the nanomolar potencies of N1,N3-dialkyldioxonaphthoimidazoliums against asexual forms of sensitive and resistant Plasmodium falciparum. Activity was dependent on the presence of the fused quinone-imidazolium entity and lipophilicity imparted by the N1/N3 alkyl residues on the scaffold. Gametocytocidal activity was also detected, with most members active at IC50 1 μM. A representative analog with good solubility, limited PAMPA permeability, and microsomal stability demonstrated oral efficacy on a humanized mouse model of P. falciparum.
- Ahenkorah, Stephen,Birkholtz, Lyn-Marie,Coertzen, Dina,Fridianto, Kevin,Go, Mei-Lin,Haynes, Richard K.,Lam, Yulin,Tan, Kevin S. W.,Tong, Jie Xin,Wittlin, Sergio
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- Discovery of Novel 2-Aniline-1,4-naphthoquinones as Potential New Drug Treatment for Leber's Hereditary Optic Neuropathy (LHON)
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Leber's hereditary optic neuropathy (LHON) is a rare genetic mitochondrial disease and the primary cause of chronic visual impairment for at least 1 in 10 ?000 individuals in the U.K. Treatment options remain limited, with only a few drug candidates and therapeutic approaches, either approved or in development. Recently, idebenone has been investigated as drug therapy in the treatment of LHON, although evidence for the efficacy of idebenone is limited in the literature. NAD(P)H:quinone oxidoreductase 1 (NQO1) and mitochondrial complex III were identified as the major enzymes involved in idebenone activity. Based on this mode of action, computer-aided techniques and structure-activity relationship (SAR) optimization studies led to the discovery of a series naphthoquinone-related small molecules, with comparable adenosine 5′-triphosphate (ATP) rescue activity to idebenone. Among these, three compounds showed activity in the nanomolar range and one, 2-((4-fluoro-3-(trifluoromethyl)phenyl)amino)-3-(methylthio)naphthalene-1,3-dione (1), demonstrated significantly higher potency ex vivo, and significantly lower cytotoxicity, than idebenone.
- Varricchio, Carmine,Beirne, Kathy,Aeschlimann, Pascale,Heard, Charles,Rozanowska, Malgorzata,Votruba, Marcela,Brancale, Andrea
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p. 13638 - 13655
(2020/11/30)
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- Design, synthesis and biological evaluation of novel naphthoquinone derivatives as IDO1 inhibitors
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Indoleamine 2,3-dioxygenase 1 (IDO1) mediated kynurenine pathway of tryptophan degradation is identified as an appealing and novel target in immunotherapy for the treatment of cancer. In this study, a novel series of naphthoquinone derivatives were synthesized, characterized and evaluated for their inhibitory activities against IDO1, and their structure?activity relationship was investigated. Among them, compounds T16, T44, T47, T49, T53 and T54 displayed potent IDO1 inhibitory activities with IC50 values ranging between 18 and 61 nM, which are more potent than INCB024360 undergoing clinical trial III evaluation. In addition, compounds T28, T44 and T53 decreased the kynurenine levels in rat plasma by 30%–50%. Compounds exhibiting excellent IDO1 inhibitory activities were also evaluated for their inhibitory activities against tryptophan 2,3-dioxygenase (TDO). Of which, compound T28 (IDO1 IC50 = 120 nM) showed promising TDO inhibition (IC50 72 nM) and was identified as an IDO1/TDO dual inhibitor.
- Pan, Liangkun,Zheng, Qiang,Chen, Yu,Yang, Rui,Yang, Yanyan,Li, Zhongjun,Meng, Xiangbao
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p. 423 - 436
(2018/08/17)
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- Synthesis and biological evaluation of novel 2-arylvinyl-substituted naphtho[2,3-d]imidazolium halide derivatives as potent antitumor agents
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Two series of novel 2-arylvinyl-naphtho[2,3-d]imidazol-3-ium iodide derivatives and 2-arylvinyl-naphtho[2,3-d]imidazol-3-ium bromide derivatives were designed and synthesized by the structural combination of YM155 with stilbenoids. All compounds were tested for anti-proliferative activity against PC-3, A375 and HeLa human cancer cell lines. Two of the compounds were selected for further investigation: 12b, which showed potent cytotoxicity against the three tested cell lines with IC50 values in the range of 0.06–0.21 μM, and 7l, which displayed excellent selectivity for PC-3 cells with an IC50 of only 22 nM. Western blot analysis results indicated that both 12b and 7l suppress the expression of Bcl-2 and Survivin proteins, which helps induce apoptosis. As determined by the percent of Annexin V-FITC-positive apoptotic cells, 12b was not only significantly more effective than 7l at a concentration of 100 nM in PC-3 cells but also induced apoptosis in a dose-dependent manner with more potency than 7l at a concentration of 1000 nM in A375 cells. Therefore, compound 12b was chosen for further in-depth studies investigating the mechanism of apoptosis. The results showed that it could activate caspase-3, hydrolyze PARP, and even inactivate ERK. Moreover, 12b arrested A375 cells at S phase in a time-dependent and dose-dependent manner, while having a visible effect on microtubule dynamics. In addition, (E)-2-(2-(1H-indol-3-yl)vinyl)-1-benzyl-3-(2-methoxyethyl)-4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium bromide (12b) exhibited significant antitumor activity when evaluated in a subcutaneous solid tumor model. Our study reveals that 2-arylvinyl-substituted naphtho[2,3-d]imidazolium scaffolding is a promising new entity for the development of multi-target anticancer drugs.
- Wei, Qingyun,Li, Ju,Tang, Feng,Yin, Yin,Zhao, Yong,Yao, Qizheng
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p. 504 - 516
(2018/01/02)
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- Synthesis and antimicrobial evaluation of amino sugar-based naphthoquinones and isoquinoline-5,8-diones and their halogenated compounds
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Antibiotic resistance has emerged as a serious global public health problem and lately very few antibiotics have been discovered and introduced into clinical practice. Therefore, there is an urgent need for the development of antibacterial compounds with new mechanism of action, especially those capable of evading known resistance mechanisms. In this work two series of glycoconjugate and non-glycoconjugate amino compounds derived from of isoquinoline-5,8-dione and 1,4-naphthoquinone and their halogenated derivatives were synthesized and evaluated for antimicrobial activity against Gram-positive (Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 25923, S. epidermidis ATCC 12228, S. simulans ATCC 27851) and Gram-negative bacteria (E. coli ATCC 25922, Proteus mirabilis ATCC 15290, K. pneumoniae ATCC 4352 and P. aeruginosa ATCC 27853) strains of clinical importance. This study revealed that glycoconjugate compounds derived from halogeno-substituted naphthoquinones were more active against Gram-negative strains, which cause infections whose treatment is even more difficult, according to the literature. These molecules were also more active than isoquinoline-5,8-dione analogues with minimum inhibitory concentration (MIC = 4–32 μg/mL) within Clinical and Laboratory Standard Institute MIC values (CLSI 0.08–256 μg/mL). Interestingly the minimal bactericidal concentration (MBC) values of the most active compounds were equal to MIC classifying them as bactericidal agents against Gram-negative bacteria. Sixteen compounds among eighteen carbohydrate-based naphthoquinones tested showed no hemolytic effects on health human erythrocytes whereas more susceptibility to hemolytic cleavage was observed when using non-glycoconjugate amino compounds. In silico Absorption, Distribution, Metabolism, Excretion and Toxicity (ADMET) evaluation also pointed out that these compounds are potential for oral administration with low side effects. In general, this study indicated that these compounds should be exploited in the search for a leading substance in a project aimed at obtaining new antimicrobials more effective against Gram-negative bacteria.
- Dias, Flaviana R.F.,Novais, Juliana S.,Devillart, Talita A. do Nascimento Santos,da Silva, Wanderson Amaral,Ferreira, Matheus O.,Loureiro, Raquel de S.,Campos, Vinícius R.,Ferreira, Vitor F.,de Souza, Maria C.B.V.,Castro, Helena C.,Cunha, Anna C.
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- A simple synthesis of 3,4-dihydrobenzo[f]quinoxalin-6(2H)-one derivatives substituted in the ring B
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[Figure not available: see fulltext.] We followed a simple, inexpensive, and efficient route to synthesize a series of 3,4-dihydrobenzo[f]quinoxalin-6(2H)-one derivatives substituted in the ring B, with the expectation that this scaffold might exhibit antineoplastic activity. 5-Chlorobenzo[f]quinoxalin-6-ylacetate and 4-benzylbenzo[f]quinoxalin-6(4H)-one were obtained for the first time.
- Castro-Castillo, Vicente,Suárez-Rozas, Cristian,Simpson, Sebastián,Barriga-González, Andrés
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p. 553 - 559
(2017/08/30)
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- Polymorphism in chloro derivatives of 1,4-naphthoquinone: Experiment and density functional theoretic investigations
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Molecular interactions underlying polymorphs of chlorine containing 1,4-naphthoquinone derivatives have been investigated by employing single crystal X-ray, 1H NMR, FTIR and electronic spectra experiments combined with density functional theory. Two polymorphs of 2,3-dichloro-1,4-naphthoquinone possessing (i) triclinic space group P-1(A1 and A3), and (ii) orthorhombic with Pb21a (A2) space group were obtained. The polymorph A3 has two molecules in its asymmetric unit which facilitate [Formula presented] interactions engendeing polymeric planar sheets. The two polymorphs of 2-amino-3-chloro-1,4-naphthoquinone reveal monoclinic forms with Pc (B1) and C2/C (B2) space groups. A tetramer of B2 molecule possess [Formula presented] interactions. The polymorphs of 2-chloro-3-hydroxy-1,4-naphthoquinone crystallizes in monoclinic space groups Pc (C1) and Pn (C2). Polymeric chain of C2 molecules results via [Formula presented] interactions and the chains further are connected through [Formula presented] and π-π stacking interactions those arise from benzenoid and quinonoid centroid. Moreover A3 facilitates the dimer via the halogen bonding interactions. Furthermore hydrogen bonding renders stability to the dimer C2. On the other hand compound B2 does not favor dimer formation. These inferences based on experimental observations are rationalized through the use of the dispersion corrected M06-2x functional based density functional theory. Further time dependent density functional theory has been used to assign the electronic transitions in UV–visible spectra of A3, B2 and C2.
- Chaudhari, Dinkar,Gejji, Shridhar P.,Lande, Dipali N.,Chakravarty, Debamitra,Salunke-Gawali, Sunita
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p. 281 - 293
(2016/07/14)
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- Antiproliferative, DNA intercalation and redox cycling activities of dioxonaphtho[2,3-d]imidazolium analogs of YM155: A structure-activity relationship study
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The anticancer agent YM155 is widely investigated as a specific survivin suppressant. More recently, YM155 was found to induce DNA damage and this has raised doubts as to whether survivin is its primary target. In an effort to assess the contribution of DNA damage to the anticancer activity of YM155, several analogs were prepared and evaluated for antiproliferative activity on malignant cells, participation in DNA intercalation and free radical generation by redox cycling. The intact positively charged scaffold was found to be essential for antiproliferative activity and intercalation but was less critical for redox cycling where the minimal requirement was a pared down bicyclic quinone. Side chain requirements at the N1 and N3 positions of the scaffold were more alike for redox cycling and intercalation than antiproliferative activity, underscoring yet again, the limited structural overlaps for these activities. Furthermore, antiproliferative activities were poorly correlated to DNA intercalation and redox cycling. Potent antiproliferative activity (IC50 9-23 nM), exceeding that of YM155, was found for a minimally substituted methyl analog AB7. Like YM155 and other dioxonaphthoimidazoliums, AB7 was a modest DNA intercalator but with weak redox cycling activity. Thus, the capacity of this scaffold to inflict direct DNA damage leading to cell death may not be significant and YM155 should not be routinely classified as a DNA damaging agent.
- Ho, Si-Han Sherman,Sim, Mei-Yi,Yee, Wei-Loong Sherman,Yang, Tianming,Yuen, Shyi-Peng John,Go, Mei-Lin
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supporting information
p. 42 - 56
(2015/10/19)
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- METHODS FOR TREATING LEISHMANIASIS
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Methods are provided to inhibit proliferation of Leishmania parasites, and in particular Leishmania donovani with imido-substituted 1,4-naphthoquinones, including novel compounds. Administering an imido-substituted 1,4-naphthoquinone can be used to provide prophylaxis or treatment to a patient in need of treatment against leishmaniasis disease.
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Page/Page column 28
(2013/06/05)
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- BRANCHED CATIONIC LIPIDS FOR NUCLEIC ACIDS DELIVERY SYSTEM
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The present invention is directed to cationic lipid for the delivery of oligonucleotides and methods of modulating an expression of a targeted gene using the nanoparticle compositions. In particular, the invention relates to cholesterol and its derivatives having multiple positively charged moieties via branching spacers, and nanoparticle compositions of oligonucleotides encapsulated in a mixture of a cationic lipid, a fusogenic lipid and a PEG lipid.
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- Solid-phase synthesis of 2-amino-3-chloro-5- and 8-nitro-1,4- naphthoquinones: A new and general colorimetric test for resin-bound amines
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Treatment of resin-bound primary or secondary alkyl and arylamines with 2,3-dichloro-5-nitro-1,4-naphthoquinone leads to the rapid formation of intensely colored (red) beads. The resulting 2-amino-3-chloro-5- and 8-nitro-1,4-naphthoquinones can be cleaved rapidly from acid-labile supports in high yields and purities. The reaction is of value as a sensitive and general qualitative test for amino groups on-resin that can be followed by cleavage for characterization and quantification of the chromogen(s) responsible for the color.
- Blackburn, Christopher
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p. 1405 - 1409
(2007/10/03)
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- Sulfur-containing derivatives of 1,4-naphthoquinone, part 1: Disulfide synthesis
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Bisulfides of 1,4-naphthoquinone were synthesized, and different methods of their synthesis were investigated. High yields and purity of disulfides were obtained from the oxidation of thiol derivatives. The latter were prepared in high yields and purity from isothiuronic salts. The obtained disulfides are synthones for compounds with a wide spectrum of biological activity.
- Stasevych, Maryna V.,Plotnikov, Maxym Yu.,Platonov, Mykola O.,Sabat, Svitlana I.,Musyanovych, Rostyslav Ya.,Novikov, Volodymyr P.
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p. 205 - 211
(2007/10/03)
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- Methods for the purification of levofloxacin
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Levofloxacin has been purified by dissolving levofloxacin in a polar solvent at an elevated temperature and crystallizing purified levofloxacin. Preferably, an antioxidant is added to increase the purity.
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- Synthesis of a new polypyridinic highly conjugated ligand with electron-acceptor properties
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A new acceptor polypyridinic ligand functionalized with a quinone fragment is reported. The ligand, dipyrido[3,2-a:2′,3′-c]-benzo[3,4]-phenazine-11,16-quinone, Nqphen, was synthesized by condensation of 1,10-phenanthroline-5,6-dione and 2,3-diamino-1,4-naphthoquinone. The syntheses of two rhenium complexes with this ligand are also reported.
- Díaz, Ramiro,Reyes, Oscar,Francois, Angélica,Leiva, Ana María,Loeb, Bárbara
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p. 6463 - 6467
(2007/10/03)
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- Synthesis and Structure of Chlorine-Containing 2-Amino-1,4-naphthoquinone Derivatives
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Exhaustive chlorination of 2-amino-1,4-naphthoquinone derivatives yields 3,3-dichloro-2-imino-2,3-dihydro-1,4-naphthoquinones.
- Litvin, B. L.,Gubrii, Z. V.,Shermolovich, Yu. G.,Novikov, V. P.
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p. 377 - 383
(2007/10/03)
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- Iodine catalyzed chlorination of naphthoquinones using metal (II) chlorides
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The active quinonoid position of various naphthoquinones is chlorinated by metal(II) chloride (Cu/Hg) and iodine in acetic acid in single step reaction with excellent yields.
- Thapliyal, Prakash Chander
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p. 1123 - 1126
(2007/10/03)
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- Process for the preparation of ruthenium hydrogenation catalysts and products thereof
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This invention relates to a process for the preparation of ruthenium complexes of the formula RuH2 L2 (PR3)2, wherein each L is independently H2 or an additional equivalent of PR3, and each R is independently H, a hydrocarbyl group, or an assembly of at least two hydrocarbyl groups connected by ether or amine linkages, comprising contacting a source of ruthenium and PR3 with gaseous hydrogen in the presence of a strong base, a phase transfer catalyst, water and an organic solvent; and the use of certain classes of ruthenium complexes as catalysts in hydrogenation, and reductive hydrolysis processes.
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- Ruthenium hydrogenation catalysts
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The invention relates to a novel ruthenium complex having the formula Ru(η3 -C6 H8 -PCy2)(PCy3)Cl, wherein Cy is cyclohexyl; its use in the preparation of RuHCl(H2)(PCy3)2 and RuH2 (H2)2 (PCy3)2 ; and the use of the complexes as catalysts in hydrogenation, imination and reductive hydrolysis processes.
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- SYNTHESIS OF SOME NOVEL NAPHTHOQUINONE FUSED SELENAZOLES AND 2-AMINO-3-ALKYLSELENO-1,4-NAPHTHOQUINONES
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A variety of 2-aryl-4,9-dioxonaphthoselenazoles (4) are prepared from reactions of appropriate aromatic aldehydes and 2-amino-3-seleno-1,4-naphthoquinone sodium salt (3), which is prepared from 2-amino-3-chlornaphthoquinone (2), sodium and selenium powder without isolation.The intermediate (3) reacts with a range of alkyl halides to give 2-amino-3-alkylseleno-1,4-naphthoquinones (5).
- Ruan, Ming-De,Wu, Zheng-Jie,Fan, Wei-Qiang,Zhou, Xun-Jun
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p. 323 - 330
(2007/10/02)
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- Mode for Herbicidal Action of 2-Amino-3-chloro-1,4-naphthoquinone (ACN)
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The characteristic mode for the herbicidal action of 2-amino-3-chloro-1,4-naphthoquinone (ACN) was investigated by using autotropic green microalgae (Scenedesmus acutus).The effects of ACN on the growth, chlorophyll content, protoporphyrin-IX accumulation, and ethane production in Scenedesmus cells were measured in comparison with three reference herbicides, i.e., ioxynil, dinoseb, and chlorophthalim.ACN appeared to have a different mechanism for action from these three herbicides.S. acutus cells grown with ACN produced ethane, but the mechanism for its production is considered to have been different from that of chlorophthalim.ACN may inhibit porphyrin biosynthesis at a different stage from that by chlorophthalim.
- Koura, Seigo,Takasuka, Kiyoshi,Katsuyama, Noriyoshi,Ogino, Chifuyu,Sato, Yukiharu,Wakabayashi, Ko
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p. 1210 - 1212
(2007/10/02)
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- Novel chloroacetanilide derivatives and herbicides containing the same for use in paddy field
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Disclosed herein are novel chloroacetanilide derivatives which act as remarkably effective herbicides when sprayed in a paddy field, the chloroacetanilide derivatives being 2',6'-diethyl-N-[(cis-alkenyloxy)methyl]-2-chloroacetanilides [A] represented by the general formula STR1 wherein R is a cis-form alkenyl group having 4 or 5 carbon atoms. Also disclosed are herbicide compositions for use in a paddy field and containing at least one of said chloroacetanilide derivatives [A] and at least one pyrazole derivative [B] represented by the general formula STR2 wherein R is a hydrogen atom or methyl group and X is a 4-toluenesulfonyl group or benzoylmethyl group; or-α-(2-naphtoxy)-propyonanilide [C] represented by the formula STR3
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- REACTION OF THIOAMIDES WITH 2,3-DICHLORO-1,4-NAPHTHOQUINONE. A NOVEL SYNTHESIS OF NAPHTHOTHIAZOLE-4,9-DIONES
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The reaction of thioamide II with 2,3-dichloro-1,4-naphthoquinone (I) in ethanol gave naphtho-thiazole-4,9-diones (IV).The intermediates, 2-thioamido-3-chloro-1,4-naphthoquinones III were also isolated from the reaction medium and could be separately transformed to IV by further boiling in aqueous ethanol containing bicarbonate.The reaction of thiosemicarbazide with I under similar conditions gave naphtho-2-amino-4H-1,3,4-thiadiazine-5,10-dione (VII).
- Hammam, A.S.,Bayoumy, B.E.
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- Controlled release pesticides
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Controlled release pesticide-polymers are prepared by reacting a polymer having a pendant group containing a reactive hydrogen with a chloroformamide derivative of a pesticide. In a preferred embodiment, metribuzin chloroformamide is prepared by reacting metribuzin with phosgene at a temperature of about 40° C. The metribuzin chloroformamide is then reacted with cellulose to form a pesticide-polymer from which the metribuzin is released under use conditions by hydrolytic degradation of the carbamate bond attaching the metribuzin to the polymer.
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- Substituted 1,4-Naphthoquinones vs. the Ascitic Sarcoma 180 of Mice
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Twelve 1,4-naphthoquinones have been tested against the ascitic form of sarcoma 180 in Swiss mice.Statistical analysis shows that the most important molecular parameter determining their effectiveness in prolonging the life of mice bearing this tumor is their redox potentials.Although the toxicities of the compounds are also related to the redox potentials in the same way, the therapeutic indexes can be increased by adding substituents of greater lipophilicity.The naphthoquinones differ greatly in antitumor activities and may inhibit the growth of malignant cells by different mechanisms
- Hodnett, Ernest M.,Wongwiechintana, Chinda,Dunn, William J.,Marrs, Pam
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p. 570 - 574
(2007/10/02)
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- Pesticide-polymer systems prepared from vinyl monomers
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Controlled release pesticide-polymer systems are prepared by the polymerization of vinyl monomers containing pendant pesticides. The vinyl monomers are prepared by reacting an acrylic acid derivative with a pesticide or a pesticide derivative having an active hydrogen. The pesticide-polymer systems prepared from the pesticide vinyl monomers release the active pesticide material by hydrolysis or chemical depolymerization under conditions of use.
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