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Rania Hamdy, Noha I Ziedan, Samia Ali, Cinzia Bordoni, Mohamed El-Sadek, Elsaid Lashin, Andrea Brancale, Arwyn T Jones, Andrew D Westwell
A series of 5-(1H-indol-3-yl)-N-aryl-1,3,4-oxadiazol-2-amines 8a-j has been designed, synthesized and tested in vitro as potential pro-apoptotic Bcl-2-inhibitory anticancer agents based on our previous lead compound 8a. Synthesis of the target compounds was readily accomplished through a cyclisation reaction between indole-3-carboxylic acid hydrazide (5) and substituted isothiocyanates 6a-j, followed by oxidative cyclodesulfurization of the corresponding thiosemicarbazide 7a-j using 1,3-dibromo-5,5-dimethylhydantoin...
December 27, 2016: Bioorganic & Medicinal Chemistry Letters
(no author information available yet)
The Administrator of the Drug Enforcement Administration is issuing this notice of intent to temporarily schedule six synthetic cannabinoids: methyl 2-(1-(5-fluoropentyl)-1H-indazole-3-carboxamido)-3,3-dimethylbutanoate [5F-ADB; 5F-MDMB-PINACA]; methyl 2-(1-(5-fluoropentyl)-1H-indazole-3-carboxamido)-3-methylbutanoate [5F-AMB]; N-(adamantan-1-yl)-1-(5-fluoropentyl)-1H-indazole-3-carboxamide [5F-APINACA, 5F-AKB48]; N-(1-amino-3,3-dimethyl-1-oxobutan-2-yl)-1-(4-fluorobenzyl)-1H-indazole-3-carboxamide [ADB-FUBINACA]; methyl 2-(1-(cyclohexylmethyl)-1H-indole-3-carboxamido)-3,3-dimethylbutanoate [MDMB-CHMICA, MMB-CHMINACA] and methyl 2-(1-(4-fluorobenzyl)-1H-indazole-3-carboxamido)-3,3-dimethylbutanoate [MDMB-FUBINACA], into schedule I pursuant to the temporary scheduling provisions of the Controlled Substances Act (CSA)...
21, 2016: Federal Register
Noha I Ziedan, Rania Hamdy, Alessandra Cavaliere, Malamati Kourti, Filippo Prencipe, Andrea Brancale, Arwyn T Jones, Andrew D Westwell
A new series of oxadiazoles were designed to act as inhibitors of the anti-apoptotic Bcl-2 protein. Virtual screening led to the discovery of new hits that interact with Bcl-2 at the BH3 binding pocket. Further study of the structure-activity relationship of the most active compound of the first series, compound 1, led to the discovery of a novel oxadiazole analogue, compound 16j, that was a more potent small molecule inhibitor of Bcl-2. 16j had good in vitro inhibitory activity with sub-micromolar IC50 values in a metastatic human breast cancer cell line (MDA-MB-231) and a human cervical cancer cell line (HeLa)...
January 9, 2017: Chemical Biology & Drug Design
Anjali Chauhan, Shiwani Guleria, Praveen P Balgir, Abhishek Walia, Rishi Mahajan, Preeti Mehta, Chand Karan Shirkot
Aneurinibacillus aneurinilyticus strain CKMV1 was isolated from rhizosphere of Valeriana jatamansi and possessed multiple plant growth promoting traits like production of phosphate solubilization (260mg/L), nitrogen fixation (202.91nmolethylenemL(-1)h(-1)), indole-3-acetic acid (IAA) (8.1μg/mL), siderophores (61.60%), HCN (hydrogen cyanide) production and antifungal activity. We investigated the ability of isolate CKMV1 to solubilize insoluble P via mechanism of organic acid production. High-performance liquid chromatography (HPLC) study showed that isolate CKMV1 produced mainly gluconic (1...
December 24, 2016: Brazilian Journal of Microbiology: [publication of the Brazilian Society for Microbiology]
Chelladurai Chellamboli, Muthiah Perumalsamy
  This study states an integrated approach to grow Scenedesmus abundans in the presence of biostimulants as a robust flourishing organism pertaining to attain the maximum yield of the biodiesel through transesterification. These assessments are especially targeted to achieve the appreciable profit on biodiesel using three biostimulants such as, Indole 3-acetic acid (3 IAA), 6-Benzylaminopurine (6 BAP), and Gibberellic acid (GA) hormones. The proposed schema proved a rise in biomass; as well as lipid content, compared with an alga grown in the absence of hormones...
December 1, 2016: Water Environment Research: a Research Publication of the Water Environment Federation
Rareş-Petru Moldovan, Winnie Deuther-Conrad, Andrew G Horti, Peter Brust
A small series of indol-3-yl-oxoacetamides was synthesized starting from the literature known N-(adamantan-1-yl)-2-(5-(furan-2-yl)-1-pentyl-1H-indol-3-yl)-2-oxoacetamide (5) by substituting the 1-pentyl-1H-indole subunit. Our preliminary biological evaluation showed that the fluorinated derivative 8 is a potent and selective CB₂ ligand with Ki = 6.2 nM.
January 4, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Jakkapan Sakpirom, Duangporn Kantachote, Tomorn Nunkaew, Eakalak Khan
This study was aimed at selecting purple non-sulfur bacteria (PNSB) isolated from various paddy fields, including Cd- and Zn-contaminated paddy fields, based on their biofertilizer properties. Among 235 PNSB isolates, strain TN110 was most effective in plant growth-promoting substance (PGPS) production, releasing 3.2 mg/L of [Formula: see text] , 4.11 mg/L of 5-aminolevulinic acid (ALA) and 3.62 mg/L of indole-3-acetic acid (IAA), and reducing methane emission up to 80%. This strain had nifH, vnfG and anfG, which are the Mo, V and Fe nitrogenase genes encoded for key enzymes in nitrogen fixation under different conditions...
December 28, 2016: Research in Microbiology
Qing Wang, Wen-Jing Cai, Lei Yu, Jun Ding, Yu-Qi Feng
Honey exhibits various nutritional and medicinal functions, which are highly related to the active components, thus the exploration of new compounds in honey is of great importance. As honey is a by-product of flower nectar, which is rich in phytohormones, the existence of phytohormones in honeys is anticipated. In this research, a method for comprehensive profiling of 49 phytohormones in honey was developed by sequential liquid-liquid extraction (LLE) coupled with liquid chromatography-tandem mass spectrometry (LC-MS/MS)...
December 29, 2016: Journal of Agricultural and Food Chemistry
Tushar S Basu Baul, Pelesakuo Kehie, Andrew Duthie, Nikhil Guchhait, Nune Raviprakash, Raveendra B Mokhamatam, Sunil K Manna, Nerina Armata, Michelangelo Scopelliti, Ruimin Wang, Ulli Englert
Five new organotin(IV) complexes of compositions [Me2SnL(1)] (1), [Me2SnL(2)]n (2), [Me2SnL(3)] (3), [Ph3SnL(1)H]n (4) and [Ph3SnL(3)H] (5) (where L(1)=(2S)-2-((E)-((Z)-4-hydroxypent-3-en-2-ylidene)amino)-3-(1H-indol-3-yl)propanoate, L(2)=(2S)-(E)-2-((2-hydroxybenzylidene)amino)-3-(1H-indol-3-yl)propanoate and L(3)=(2S)-(E)-2-((1-(2-hydroxyphenyl)ethylidene)amino)-3-(1H-indol-3-yl)propanoate were synthesized and spectroscopically characterized. The crystal structures of 1-4 were determined. For the dimethyltin derivative 2, a polymeric chain structure was observed as a result of a long Sn∙∙∙O contact involving the exocyclic carbonyl oxygen-atom from the tridentate ligand of a neighboring Sn-complex unit...
December 16, 2016: Journal of Inorganic Biochemistry
Suleman M Inamdar, Rajesh G Gonnade, Nitin T Patil
A general method to access annulated bis-indoles from (1H-indol-3-yl)(aryl)methanols and 2-(arylethynyl)-1H-indoles under the catalysis of the Ph3PAuOTf/Brønsted acid binary catalyst system has been developed. The reaction was found to proceed in a highly efficient manner and benefit from easy-to-make starting materials, broad substrate scope and operational simplicity. The potential of this method has also been exemplified for the synthesis of pyrrole-annulated indoles using 2-(phenylethynyl)-1H-indoles and phenyl(1H-pyrrol-2-yl)methanols...
December 23, 2016: Organic & Biomolecular Chemistry
Oksana O Kolachevskaya, Lidiya I Sergeeva, Kristyna Floková, Irina A Getman, Sergey N Lomin, Valeriya V Alekseeva, Elena B Rukavtsova, Yaroslav I Buryanov, Georgy A Romanov
Ectopic auxin overproduction in transgenic potato leads to enhanced productivity accompanied with concerted and occasional changes in hormonal status, and causing altered response of transformants to exogenous auxin or cytokinin. Previously, we generated potato transformants expressing Agrobacterium-derived auxin synthesis gene tms1 driven by tuber-specific patatin gene promoter (B33-promoter). Here, we studied the endogenous hormonal status and the response to exogenous phytohormones in tms1 transformants cultured in vitro...
December 20, 2016: Plant Cell Reports
Angela K Spartz, Vai S Lor, Hong Ren, Neil E Olszewski, Nathan D Miller, Guosheng Wu, Edgar P Spalding, William M Gray
The plant hormone indole-3-acetic acid (IAA or auxin) mediates the elongation growth of shoot tissues by promoting cell expansion. According to the acid growth theory proposed in the 1970s, auxin activates plasma membrane H+-ATPases (PM H+-ATPases) to facilitate cell expansion by both loosening the cell wall through acidification and promoting solute uptake. Mechanistically, however, this process is poorly understood. Recent findings in Arabidopsis have demonstrated that auxin-induced SMALL AUXIN UP RNA (SAUR) genes promote elongation growth and play a key role in PM H+-ATPase activation by inhibiting PP2C...
December 20, 2016: Plant Physiology
Xiumei Yu, Yangxin Li, Yongliang Cui, Ricong Liu, Yanmei Li, Qiang Chen, Yunfu Gu, Ke Zhao, Quanju Xiang, Kaiwei Xu, Xiaoping Zhang
AIMS: To analyze whether some secreting indoleacetic acid (IAA) PGPB can alleviate Cd stress or not, the role of an Ochrobactrum sp. MGJ11 from rhizosphere of soybean in promoting plant growth and counteracting Cd effects on soybean was evaluated. METHODS AND RESULTS: Ochrobactrum sp. MGJ11 produced 121.2 mg l(-1) of indole-3-acetic acid (IAA). MGJ11 increased soybean root length, shoot length and biomass by 30.1%, 30.8% and 13.4%, respectively. In liquid medium, no IAA production was detected in Cd concentration of 100 mg l(-1) ...
December 20, 2016: Journal of Applied Microbiology
Ye Jin Kim, Jae Sung Pyo, Young-Suk Jung, Jae-Hwan Kwak
A series of novel 1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-3-carboxamide analogs were designed and synthesized for developing pyrazinoindolone scaffolds as anti-breast cancer agents. Compounds 1h and 1i, having a furan-2-yl-methylamide and benzylamide group, respectively, exhibited more potent cytotoxicity in MDA-MB-468 triple-negative breast cancer (TNBC) cells than compounds possessing aliphatic groups. Compounds 2a and 2b, as (R)-enantiomers of 1h and 1i, also had inhibitory activity against MDA-MB-468 cells...
December 5, 2016: Bioorganic & Medicinal Chemistry Letters
Tristan A Reekie, Shane M Wilkinson, Vivian Law, David E Hibbs, Jennifer A Ong, Michael Kassiou
Preparation of N-(indol-2-yl)amides and N-(indol-3-yl)amides are scarce in the scientific literature due to unstable intermediates impeding current reported syntheses. We have employed cheap and readily available substrates in the Curtius rearrangement of indole-3-carboxazide to afford N-(indol-3-yl)amides. The reaction is observed for alkyl and aryl carboxylic acids and both N-substituted or 1H-indole derivatives are tolerated. This approach was extended to the preparation of N-(indol-2-yl)amides from the corresponding indole-2-carboxazides...
December 19, 2016: Organic & Biomolecular Chemistry
Catherine W Bogner, Ramsay S T Kamdem, Gisela Sichtermann, Christian Matthäus, Dirk Hölscher, Jürgen Popp, Peter Proksch, Florian M W Grundler, Alexander Schouten
In order to replace particularly biohazardous nematocides, there is a strong drive to finding natural product-based alternatives with the aim of containing nematode pests in agriculture. The metabolites produced by the fungal endophyte Fusarium oxysporum 162 when cultivated on rice media were isolated and their structures elucidated. Eleven compounds were obtained, of which six were isolated from a Fusarium spp. for the first time. The three most potent nematode-antagonistic compounds, 4-hydroxybenzoic acid, indole-3-acetic acid (IAA) and gibepyrone D had LC50 values of 104, 117 and 134 μg ml(-1) , respectively, after 72 h...
December 19, 2016: Microbial Biotechnology
Scott Hayes, Ashutosh Sharma, Donald P Fraser, Martine Trevisan, C Kester Cragg-Barber, Eleni Tavridou, Christian Fankhauser, Gareth I Jenkins, Keara A Franklin
Small increases in ambient temperature can elicit striking effects on plant architecture, collectively termed thermomorphogenesis [1]. In Arabidopsis thaliana, these include marked stem elongation and leaf elevation, responses that have been predicted to enhance leaf cooling [2-5]. Thermomorphogenesis requires increased auxin biosynthesis, mediated by the bHLH transcription factor PHYTOCHROME-INTERACTING FACTOR 4 (PIF4) [6-8], and enhanced stability of the auxin co-receptor TIR1, involving HEAT SHOCK PROTEIN 90 (HSP90) [9]...
January 9, 2017: Current Biology: CB
Gholamreza Khaksar, Chairat Treesubsuntorn, Paitip Thiravetyan
Better understanding of plant-bacteria interactions under stress is of the prime importance for enhancing airborne pollutant phytoremediation. No studies have investigated plant-epiphyte interactions compared to plant-endophyte interactions under airborne formaldehyde stress in terms of plant Indole-3-acetic acid (IAA), ethylene, reactive oxygen species (ROS) levels and pollutant removal efficiency. Euphorbia milii was inoculated with native plant growth-promoting (PGP) endophytic and epiphytic isolates individually to investigate plant-endophyte compared to plant-epiphyte interactions under continuous formaldehyde fumigation...
December 8, 2016: Plant Physiology and Biochemistry: PPB
Rino Ishikawa, Ryosuke Iwasawa, Yuichiro Takiyama, Tomokazu Yamauchi, Tetsuo Iwanaga, Makoto Takezaki, Motonori Watanabe, Naozumi Teramoto, Toshiaki Shimasaki, Mitsuhiro Shibata
New π-conjugated 1,2-bis(2-aryl-1H-indol-3-yl)ethynes 1a-j having various substituents on the two aryl groups were efficiently synthesized via unusual 5-exo-digonal double isocyanide-acetylene cyclization reactions of 1,4-bis(2-isocyanophenyl)buta-1,3-diyne 3 and aryl Grignard reagents (R-MgBr, R = C6H5 (1a), 4-H3CC6H4 (1b), 2-H3CC6H4 (1c), 3-MeOC6H4 (1d), 3-(CH3)2NC6H4 (1e), 4-F3CC6H4 (1f), 4-FC6H4 (1g), 3-FC6H4 (1h), 4-PhOC6H4 (1i), and 2-Naph (1j)) in 19-85% yields. The UV-vis spectra were rationalized in detail using time-dependent DFT and single point calculations...
December 16, 2016: Journal of Organic Chemistry
Xiu-Rong Hu, Jia-Li Ye, Jian-Ming Gu
In the title compound, C26H28N5O2(+)·Cl(-)·CH3OH {systematic name: 4-(2-carbamoyl-1-benzo-furan-5-yl)-1-[4-(5-cyano-1H-indol-3-yl)but-yl]piperazin-1-ium chloride methanol monosolvate}, the protonated piperazine ring adopts a chair conformation. The indole ring plane is nearly perpendicular to the benzo-furan ring system, with a dihedral angle of 85.77 (2)°. In the crystal, the organic cations, Cl(-) anions and methanol solvent mol-ecules are linked by classical N-H⋯O and N-H⋯Cl hydrogen bonds, and weak C-H⋯O and C-H⋯π inter-actions into a three-dimensional supra-molecular architecture...
December 1, 2016: Acta Crystallographica. Section E, Crystallographic Communications
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