- Cell-specific activation of gemcitabine by endogenous H2S stimulation and tracking through simultaneous fluorescence turn-on
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The endogenous H2S-driven theranosticH2S-Gemhas been invented. The theranostic prodrugH2S-Gemis selectively activated in cancer cells, releasing active gemcitabine with a simultaneous fluorescence turn-on.H2S-Gemselectively inhibited cancer cell growth compared to the mother chemotherapeutic gemcitabine. Overall, it is a unique protocol for tracking and transporting chemotherapeutic agents to tumor areas without the guidance of tumor-directive ligands.
- Maiti, Mrinmoy,Yoon, Shin A,Cha, Yujin,Athul,Bhuniya, Sankarprasad,Lee, Min Hee
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Read Online
- Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors
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The cumulative evidence supports STAT3, a transcriptional mediator of oncogenic signaling, as a therapeutic target in cancer. The development of STAT3 inhibitors remain an active area of research as no inhibitors have yet to be approved for cancer treatment. In a continuing effort to develop more potent STAT3 inhibitors based on our previously identified hit compound 16w, a series of benzothiazole derivatives with unique binding mode in SH2 domain of STAT3 were designed, synthesized and biologically evaluated. Of note, compound B19 demonstrated excellent activity against IL-6/STAT3 signaling pathway with the IC50 value as low as 0.067 μM as determined by a luciferase reporter assay. Moreover, multiple compounds displayed potent antiproliferative activity against MDA-MB-468 and JAK2 mutant HEL cell lines. Further biochemical study using Western blot assay indicated that B19 blocked the phosphorylation of STAT3 at Tyr 705 and Ser 727 and thus suppressed STAT3-mediated gene expression of c-MYC and MCL-1. Simultaneously, it induced cancer cell G2/M phase arrest and apoptosis both in MDA-MB-468 and HEL cell lines. Finally, molecular docking study along with surface plasmon resonance (SPR) and fluorescence polarization (FP) assays disclosed the binding mode of B19 in STAT3 SH2 domain. Taken together, our finding suggests that B19 is a promising therapeutic STAT3 inhibitor for cancer treatment.
- Gao, Dingding,Jin, Nan,Fu, Yixian,Zhu, Yueyue,Wang, Yujie,Wang, Ting,Chen, Yuehong,Zhang, Mingming,Xiao, Qiang,Huang, Min,Li, Yingxia
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- Exploring boron applications in modern agriculture: A structure-activity relationship study of a novel series of multi-substitution benzoxaboroles for identification of potential fungicides
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Several boron-containing small molecules have been approved by the US FDA to treat human diseases. We explored potential applications of boron-containing compounds in modern agriculture by pursuing multiple research and development programs. Here, we report a novel series of multi-substitution benzoxaboroles (1–36), a compound class that we recently reported as targeting geranylgeranyl transferase I (GGTase I) and thereby inhibiting protein prenylation (Kim et al., 2020). These compounds were designed, synthesized, and tested against the agriculturally important fungal pathogens Mycosphaerella fijiensis and Colletotrichum sublineolum in a structure–activity relationship (SAR) study. Compounds 13, 28, 30, 34 and 36 were identified as active leads with excellent antifungal MIC95 values in the range of 1.56–3.13 ppm against M. fijiensis and 0.78–3.13 ppm against C. sublineolum.
- Liu, Chunliang,Steere, Luke,McGregor, Cari,Frederick, Brittany H.,Pastoor, Timothy,Zhou, Yasheen,Liu, C. Tony,Cai, Yan,Zhou, Haibo,Xu, Musheng,Wang, Jiangong,Kim, Sang Hu,Whitesell, Luke,Cowen, Leah E.,Zhang, Yong-Kang
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- BORON CONTAINING COMPOUNDS AND THEIR USES
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The present disclosure contemplates novel boron-containing compounds and their uses as active agents that exhibit pesticidal activity such as antimicrobial, insecticidal, arachnicidal, and/or anti parasitic activity. An agrochemical composition containing such a compound and its use in, animal health, agriculture, or horticulture is also contemplated. A method for promoting plant performance and/or controlling, reducing, preventing, ameliorating, or inhibiting microbes, insects, arachnids, and/or parasites on or in an animal, a plant, a plant part, plant propagation material, and/or harvested fruits or vegetables is also contemplated.
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Paragraph 0348; 0349
(2020/03/29)
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- Bypassing Biocatalytic Substrate Limitations in Oxidative Dearomatization Reactions by Transient Substrate Mimicking
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Enzymatic oxidative dearomatization is an efficient way to generate chiral molecules from simple arenes. One example is the flavin-dependent monooxygenase SorbC involved in sorbicillinoid biosynthesis. However, SorbC requires a long-chain keto substituent at its phenolic substrate, thus preventing its application beyond the synthesis of natural sorbicillinoids or close structural analogues. This work describes an approach to broaden the accessible product spectrum of SorbC by employing an ester functionality mimicking the natural substrate structure during enzymatic oxidation.
- Milzarek, Tobias M.,Einsiedler, Manuel,Aldemir, Hülya,D'Agostino, Paul M.,Evers, Julia K.,Hertrampf, Gesa,Lamm, Katharina,Malay, Mert,Matura, Anke,Müller, Jonas I.,Gulder, Tobias A. M.
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supporting information
p. 4520 - 4524
(2019/06/27)
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- (S)-N-(1-phenethyl) thioacetamide compound as well as medicinal composition and application thereof
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The invention belongs to the field of medicinal chemicals, relates to a STAT3 inhibitor, and in particular to a (S)-N-(1-phenethyl) thioacetamide compound of a structure of formula (I) as shown in the specification, a medicinal composition of the compound as an STAT3 (Signal Transducer and Activator of Transcription 3) signal path inhibitor, and application of the compound in preparing anti-tumor medicines. Results of cell experiment show that the compound targets a Phe-Lys-Thr-Lys-Leu pentapeptide binding region in an STAT3 SH2 structure domain, then inhibits STAT3 protein monomer dimerization and silencing STAT3 signal transduction and functions, has a remarkable anti-tumor effect and good physical and chemical properties, is particularly capable of effectively preventing cell proliferative activity in breast cancer cells with high expression of STAT3 and HEL cells on which JAK2/STAT3 signal paths depend with JAK2 V671F mutation, and moreover is capable of effectively inhibiting phosphorylation of STAT3 in the breast cancer cells with high expression of STAT3 and expression of downstream target genes such as CyclinD1 and Bc1-2.
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Paragraph 0042; 0049; 0050; 0051
(2017/08/31)
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- Stereoselective Total Synthesis of Bisorbicillinoid Natural Products by Enzymatic Oxidative Dearomatization/Dimerization
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Natural products are a virtually inexhaustible source of small molecules with spectacular molecular architectures and biomedical potential. Their structural complexity generates formidable challenges to total synthesis but often also precludes time- and resource-efficient, stereoselective synthetic access. Biosynthetically, nature frequently uses dimerization and oligomerization reactions to produce highly challenging frameworks from simple starting materials. Impressive examples are the bisorbicillinoids, a family of fungal natural products thought to originate from the polyketide precursor sorbicillin. Utilizing the recombinant oxidoreductase SorbC from the sorbicillin biosynthetic gene cluster, a robust, fully stereoselective synthesis of bisorbicillinoid natural products and unnatural side-chain analogues was developed.
- Sib, Anna,Gulder, Tobias A. M.
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supporting information
p. 12888 - 12891
(2017/09/14)
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- Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate
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Carboxamide pyrazinyloxy benzoxaboroles were investigated with the goal to identify a molecule with satisfactory antimalarial activity, physicochemical properties, pharmacokinetic profile, in vivo efficacy, and safety profile. This optimization effort discovered 46, which met our target candidate profile. Compound 46 had excellent activity against cultured Plasmodium falciparum, and in vivo against P. falciparum and P. berghei in infected mice. It exhibited good PK properties in mice, rats, and dogs. It was highly active against the other 11 P. falciparum strains, which are mostly resistant to chloroquine and pyrimethamine. The rapid parasite in vitro reduction and in vivo parasite clearance profile of 46 were similar to those of artemisinin and chloroquine, two rapid-acting antimalarials. It was nongenotoxic in an Ames assay, an in vitro micronucleus assay, and an in vivo rat micronucleus assay when dosed orally up to 2000 mg/kg. The combined properties of this novel benzoxaborole support its progression to preclinical development.
- Zhang, Yong-Kang,Plattner, Jacob J.,Easom, Eric E.,Jacobs, Robert T.,Guo, Denghui,Freund, Yvonne R.,Berry, Pamela,Ciaravino, Vic,Erve, John C. L.,Rosenthal, Philip J.,Campo, Brice,Gamo, Francisco-Javier,Sanz, Laura M.,Cao, Jianxin
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p. 5889 - 5908
(2017/07/22)
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- PROCESS FOR THE PREPARATION OF 2-SUBSTITUTED-2-(6-(SUBSTITUTED)-7-METHYLBENZO[D][1,3]DIOXOL-4-YL)ACETIC ACID DERIVATIVES
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Present invention relates to an improved and commercial process for the preparation of 2-sustituted-2-(6-(substituted)-7-methylbenzo[d][1,3]dioxol-4-yl)acetic acid derivatives of formula-I [Formula should be inserted here], wherein R1 is a O-protecting group such as methoxymethyl, ethoxymethyl, trialkylsilyl, arylmethyl, tetrahydropyran-2-yl, allyl; X is hydroxyl, halogen, mesylate, triflate, tosylate, acetate; Y is oxygen atom, NH or sulfur atom; R2 is C1-C6 alkyl. 2,4-Dihydroxy-3-methylbenzal-dehyde is selectively protected at C-4 position in the form of an ether compound of formula-XII, oxidized the aldehyde function to get the diol of formula-XIII, and condensed with ethyl glyoxalate under Casiraghi reaction conditions to get the compound of formula-XV. Compound of formula-XV is converted to compound of formula-I by conventional chemistry. Compounds of formula-I are key intermediates in the synthesis of ecteinascidines like trabectedin
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Paragraph 0035
(2015/05/05)
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- 1 -HYDROXY-BENZOOXABOROLES AS ANTIPARASITIC AGENTS
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Provided are compounds useful for controlling endoparasites both in animals and agriculture. Further provided are methods for controlling endoparasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling endoparasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. The claimed compounds are described by the following Markush formula:A typical example for a compound according to above formula is: A typical example for a compound according to above formula is:
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Page/Page column 40
(2014/10/03)
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- FLUORESCENT PROBES FOR DETECTION OF COPPER
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The invention provides fluorescent sensors for the selective detection of a metal such as copper. The sensors may be considered to be derivatives of cyanine, fluorescein, rhodamine, rhodol, Tokyo green, or BODIPY. The sensors find particular use in detecting copper in cells and living animals.
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Paragraph 0205; 0249; 0265-0266
(2014/03/24)
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- IMPROVED PROCESS FOR THE PREPARATION OF 2-SUSTITUTED-2-(6-(SUBSTITUTED)-7-METHYLBENZO[D][1,3]DIOXOL-4-YL)ACETIC ACID DERIVATIVES
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Present invention relates to an improved and commercial process for the preparation of 2-sustituted-2-(6-(substituted)-7-methylbenzo[d][1,3]dioxol-4-yl)acetic acid derivatives of formula-I [Formula should be inserted here], wherein R1 is a O-protecting group such as methoxymethyl, ethoxymethyl, trialkylsilyl, arylmethyl, tetrahydropyran-2-yl, allyl; X is hydroxyl, halogen, mesylate, triflate, tosylate, acetate; Y is oxygen atom, NH or sulfur atom; R2 is C1-C6 alkyl. 2,4-Dihydroxy-3-methylbenzaldehyde is selectively protected at C-4 position in the form of an ether compound of formula-XII, oxidized the aldehyde function to get the diol of formula-XIII, and condensed with ethyl glyoxalate under Casiraghi reaction conditions to get the compound of formula-XV. Compound of formula-XV is converted to compound of formula-I by conventional chemistry. Compounds of formula-I are key intermediates in the synthesis of ecteinascidines like trabectedin
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Page/Page column 9-10
(2014/01/09)
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- 3-arylcoumarin derivatives manifest anti-proliferative activity through Hsp90 inhibition
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The potential therapeutic benefits associated with Hsp90 modulation for the treatment of cancer and neurodegenerative diseases highlight the importance of identifying novel Hsp90 scaffolds. KU-398, a novobiocin analogue, and silybin were recently identified as new Hsp90 inhibitors. Consequently, a library of 3-arylcoumarin derivatives that incorporated the structural features of KU-398 and silybin was designed, synthesized, and evaluated against two breast cancer cell lines. Western blot analysis confirmed that the resulting 3-arylcoumarin hybrids target the Hsp90 protein folding machinery.
- Zhao, Huiping,Yan, Bin,Peterson, Laura B.,Blagg, Brian S. J.
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scheme or table
p. 327 - 331
(2012/05/20)
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- A concise synthetic approach to the sorbicillactones: Total synthesis of sorbicillactone A and 9-epi-sorbicillactone A
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A concise (12 step) total synthesis of sorbicillactone A and 9-epi-sorbicillactone A is reported. Unlike typical routes to the sorbicillinoids, this strategy does not start from sorbicillin and allows for the production of the bicyclic core on a multigram scale. The intramolecular conjugate addition of a tethered malonate serves as an effective means of introducing the lactone ring and provides a synthetic handle for installing the amide nitrogen.
- Volp, Kelly A.,Johnson, Diane M.,Harned, Andrew M.
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supporting information; experimental part
p. 4486 - 4489
(2011/10/09)
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- Regioselective and stereoselective cyclizations of cyclohexadienones tethered to active methylene groups
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The cyclization of 2,5-cyclohexadienones tethered to activated methylene groups was studied. The substitution around the cyclohexadienone ring serves to regioselectively direct these cyclizations based primarily on electronic effects. In the case of brominated substrates, these reactions proceed to give highly unusual electron-deficient tricyclic cyclopropanes. By using a Cinchona alkaloid-based phase-transfer catalyst, prochiral cyclohexadienones can be desymmetrized with moderate stereoselectivity.
- Tello-Aburto, Rodolfo,Kalstabakken, Kyle A.,Volp, Kelly A.,Harned, Andrew M.
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supporting information; experimental part
p. 7849 - 7859
(2011/12/04)
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- Synthesis and characterization of new 3-acyl-7-hydroxy-6,8-substituted- coumarin and 3-acyl-7-benzyloxy-6,8-substituted-coumarin derivatives
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(Chemical Equation Presented) A new series of 3-acyl-6,7,8-substituted coumarin derivatives has been synthesized in high yields (79-99%) and characterized by means of elemental analysis, mass spectrometry, IR, and 1H NMR spectroscopy. We examined with particular attention the presence of an acyl group at position 3 (ethyl ester, carboxylic acid, and acyl chloride), and of a hydroxyl group at position 7 or a functionalized one like benzyloxy or phthalimido. The hydroxyl group has been modified by an etherification in presence of crown ether with substituted benzyl bromide or chloride to evaluate the influence on chemical characteristics and lipophilicity of coumarin nucleus. Halogens (Cl, Br) and methyl group were introduced in position 6 and 8 of the coumarin ring, respectively, in order to study their effect on reaction feasibility. Some of these 3-acyl derivatives have been recently assayed as MAO inhibitors and as intermediates (i.e. reactive chloride derivative) to design new anti-Helicobacter pylori agents.
- Chimenti, Franco,Bolasco, Adriana,Secci, Daniela,Bizzarri, Bruna,Chimenti, Paola,Granese, Arianna,Carradori, Simone
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experimental part
p. 729 - 733
(2010/08/22)
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- Trans-A2B-corroles bearing a coumarin moiety - From synthesis to photophysics
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Four dyads comprised of cor-role and coumarin units have been synthesised. Three coumarincarboxalde-hydes were synthesized and transformed into the corresponding trans-A2B-corroles by reaction with 5 (pentafluorophenyl)dipyrromethane. It has been proven that this type of direct condensation can lead to the corresponding corroles in moderate yields. The reaction of hydroxybenzaldehydes with vinylphosphonium salts has been identified as the most general method for the preparation of formyl-coumar-ins with various patterns of substitu-ents. The dyad consisting of ketobis-coumarin and corrole was synthesized by Sonogashira coupling. Spectroscopic and photophysical investigations revealed that there is an efficient energy transfer from the coumarin moiety to corrole in all four dyads. Energy transfer can be clearly ascribed to a dipole-dipole mechanism (Foerster) for all dyads that contain luminescent coumarins and to an electron exchange mechanism (Dexter) for the dyad with the non-luminescent one. In the case of the dyad that bears coumarin with a hydroxy group at position 5, an electron-transfer was detected from corrole to coumarin. The latter process is possible because of the suitably low reduction potential of coumarins of this type.
- Tasior, Mariusz,Gryko, Daniel T.,Pielacmska, Dominika J.,Zanelli, Alberto,Flamign, Lucia
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scheme or table
p. 130 - 140
(2010/04/23)
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- Click chemistry to probe Hsp90: Synthesis and evaluation of a series of triazole-containing novobiocin analogues
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A series of triazole-containing novobiocin analogues has been designed, synthesized and their inhibitory activity determined. These compounds contain a triazole ring in lieu of the amide moiety present in the natural product. The anti-proliferative effects of these compounds were evaluated against two breast cancer cell lines (SKBr-3 and MCF-7), and manifested activities similar to their amide-containing counterparts. In addition, Hsp90-dependent client protein degradation was observed via Western blot analyses, supporting a common mode of Hsp90 inhibition for both structural classes.
- Peterson, Laura B.,Blagg, Brian S.J.
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scheme or table
p. 3957 - 3960
(2010/09/03)
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- The total synthesis of (±)-11-O-debenzoyltashironin
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The total synthesis of the putative non-peptidyl neurotrophic factor 11-O-debenzoyltashironin has been accomplished. The key transformation involves a biomimetic oxidative dearomatization/transannular Diels-Alder sequence that closes the tetracyclic carbon skeleton present in the natural product. Copyright
- Cook, Silas P.,Polara, Alessandra,Danishefsky, Samuel J.
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p. 16440 - 16441
(2007/10/03)
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- First total synthesis of cichorine and zinnimidine
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The first total synthesis of the phytotoxins cichorine and zinnimidine is described. The synthetic tactics involve the sequential connection of the dense and diverse functionalities on the aromatic nucleus followed by a Parham cyclization process, giving rise to the lactam unit embedded in the title compound framework. The Royal Society of Chemistry 2005.
- Moreau, Anne,Couture, Axel,Deniau, Eric,Grandclaudon, Pierre,Lebrun, Stephane
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p. 2305 - 2309
(2007/10/03)
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- Biologically active 1,3-bis-aromatic-prop-2-en-1-ones, 1,3-bis-aromatic-propan-1-ones, and 1,3-bis-aromatic-prop-2-yn-1-ones
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The invention relates to the use of 1,3-bis-aromatic-prop-2-en-1-ones (chalcones), 1,3-bis-aromatic-propan-1-ones (dihydrochalcones), and 1,3-bis-aromatic-prop-2-yn-1-ones for the preparation of pharmaceutical compositions for the treatment or prophylaxis of a number of serious diseases including i) conditions relating to harmful effects of inflammatory cytokines, ii) conditions involving infection by Helicobacter species, iii) conditions involving infection by viruses, iv) neoplastic disorders, and v) conditions caused by microorganisms or parasites. The invention also relates to novel chalcones and dihydrochalcones (especially alkoxy substituted variants) having advantageous substitution patterns with respect to their effect as drug substances, and to methods of preparing them, as well as to pharmaceutical compositions comprising the novel chalcones. Moreover, the present invention relates to a method for the isolation of Leishmania fumarate reductase, QSAR methodologies for selecting potent compounds for the above-mentioned purposes.
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- Synthesis of isothiochroman 2,2-dioxide and 1,2-benzooxathiin 2,2- dioxide gyrase B inhibitors
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The design, synthesis and in vitro biological evaluation of isothiochroman 2,2-dioxide and 1,2-benzooxathiin 2,2-dioxide analogues of coumarin inhibitors of gyrase B are described. Compared to coumarin derivatives, compounds of the 1,2-benzooxathiin 2,2-dioxide series display improved inhibitory potency in negative supercoiling of relaxed DNA gyrase. (C) 2000 Elsevier Science Ltd.
- Peixoto, Christophe,Laurin, Patrick,Klich, Michel,Dupuis-Hamelin, Claudine,Mauvais, Pascale,Lassaigne, Patrice,Bonnefoy, Alain,Musicki, Branislav
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p. 1741 - 1745
(2007/10/03)
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- Synthesis and biological evaluation of coumarincarboxylic acids as inhibitors of gyrase B. L-rhamnose as an effective substitute for L-noviose
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A series of novobiocin-like coumarincarboxylic acids has been prepared bearing the L-rhamnosyl moiety as the sugar portion of the molecule. The similar DNA gyrase inhibitory activity of the novel class of coumarins to that of novobiocin demonstrates that L-rhamnose can effectively replace L-novoise. Introduction of alkyl side-chains at C-5 of coumarin leads to improved in vitro antibacterial properties in the novel series.
- Ferroud, Didier,Collard, Jeannine,Klich, Michel,Dupuis-Hamelin, Claudine,Mauvais, Pascale,Lassaigne, Patrice,Bonnefoy, Alain,Musicki, Branislav
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p. 2881 - 2886
(2007/10/03)
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- Antileishmaniai chalcones: Statistical design, synthesis, and three- dimensional quantitative structure-activity relationship analysis
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A large number of substituted chalcones have been synthesized and tested for antileishmanial and lymphocyte-suppressing activities. A subset of the chalcones was designed by using statistical methods. 3D-QSAR analyses using 67 (antileishmanial activity) and 63 (lymphocyte-suppressing activity) of the compounds for the training sets and 9 compounds as an external validation set were performed by using the GRID/GOLPE methodology. The Smart Region Definition procedure with subsequent region selection as implemented in GOLPE reduced the number of variables to approximately 1300 yielding 3D-QSAR models of high quality (lymphocyte-suppressing model, R2 = 0.90, Q2 = 0.80; antileishmanial model, R2 = 0.73, Q2 = 0.63). The coefficient plots indicate that steric interactions between the chalcones and the target are of major importance for the potencies of the compounds. A comparison of the coefficient plots for the antileishmanial effect and the lymphocyte- suppressing activity discloses significant differences which should make it possible to design chalcones having a high antileishmanial activity without suppressing the proliferation of lymphocytes.
- Nielsen, Simon Feldb?k,Christensen, S?ren Br?gger,Cruciani, Gabriele,Kharazmi, Arsalan,Liljefors, Tommy
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p. 4819 - 4832
(2007/10/03)
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- Biaryl formation using the Suzuki protocol: Considerations of base, halide, and protecting group
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The generation of aryl anions prior to quenching with a trialkyl berate has been shown to be sensitive to the composition of the aryl substrate. Aryl iodides containing remote benzyl ether substituents undergo trans-metallation with sec-BuLi to cleanly give the desired aryl anions whereas the corresponding bromides afford appreciable quantities of dianionic intermediates. The aryl boronic acids derived from alkylation of these anions subsequently undergo a palladium mediated coupling with aryl halides to provide good yields of the desired biaryls. Copyright (C) 1996 Elsevier Science Ltd.
- Benbow, John W.,Martinez, Bonnie L.
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p. 8829 - 8832
(2007/10/03)
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- Alkynylamino-nucleotides
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Alkynylamino-nucleotides and labeled alkynylaminonucleotides useful, for example, as chain terminating substrates for DNA sequencing are provided along with several key intermediates and processes for their preparation. For some applications, longer, hydrophilic linkers are provided.
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- Method of gene mapping
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The method described characterizes each DNA segment to be mapped by cleaving it to produce DNA fragments which are then end labeled with a reporter(s) specific to the end nucleotides of each fragment. The labeled fragments are again cleaved to produce short fragments which are separated according to size. The short fragments are analyzed as to report identify and size which is indicative of the character of each fragment. By derivatizing the cleaved ends of the primary cleaved fragments, the labeling may be delayed until the second cleavage. Prior to the labeling the derivatized fragments, all underivatized fragments are removed, the derivatized fragments being immobilized.
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- Alkynylamino-nucleotides
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Alkynylamino-nucleotides and labeled alkynylamino-nucleotides useful, for example, as chain terminating substrates for DNA sequencing are provided along with several key intermediates and processes for their preparation.
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- SYNTHESIS OF THREE NATURAL 1,3-DIARYLPROPANES: TWO REVISED STRUCTURES
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1-(2',4'-dihydroxy-3',5'-dimethylphenyl)-3-(2"-hydroxy-4",5"-methylenedioxyphenyl)-Propane, isolated from Iryanthera coriacea and I. laevis, 1-(2'-hydroxy-4'-methoxy-5'-methylphenyl)-3-(2"-hydroxy-4",5"-methylene-dioxyphenyl)-propane, isolated from I. laevis, and 1-(2'-hydroxy-4'-methoxyphenyl)-3-(3"-hydroxy-4"-methoxyphenyl)-propane, isolated from Virola multinervia, were synthesized by processes which involved catalityc hydrogenation of the appropriate chalcones and Clemmensen reduction of dihydrochalcones.Only the structures of 1,3-diarylpropanes isolated from V. multinervia and I. laevis were revised. - Keywords: Virola multinervia; Iryanthera coriaceae; I. laevis; Myristicaceae; 1,3-diarylpropanes; synthesis; reduction of chalcones and dihydrochalcones.
- Morais, Anselmo A.,Fo, Raimundo Braz,Fraiz, Silas V. Jr
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p. 239 - 242
(2007/10/02)
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- The Total Synthesis of some Deuterium Labelled Pentaketide Derivatives of Orsellinic Acid
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The total syntheses of 4,6-dihydroxy-3,5-dimethyl-2-(1-methyl-2-oxopropyl)benzaldehyde and 6,8-dihydroxy-3,4,5,7-tetramethyl-3,4-dihydroisocoumarin, which allow the insertion of specific deuterium labels, are described.
- Barber, Jill,Staunton, James
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p. 1685 - 1689
(2007/10/02)
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