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Dong-Jun Fu, Jia-Huan Li, Jia-Jia Yang, Ping Li, Yan-Bing Zhang, Simeng Liu, Zhong-Rui Li, Sai-Yang Zhang
Novel chalcone-dithiocarbamate hybrids were designed, synthesized and evaluated for antiproliferative activity against selected cancer cell lines (MGC803, MCF7, and PC3). Among these analogues, (E)-2-oxo-2-((4-(3-(3,4,5-trimethoxyphenyl)acryloyl)phenyl)amino)ethyl-4-(2-hydroxyethyl)piperazine-1-carbodithioate (12d) showed the best inhibitory activity against PC3 cells (IC50  = 1.05 μM). Cellular mechanism studies elucidated 12d could inhibit colony formation, arrest cell cycle at G2/M phase and induce DNA damage against PC3 cells...
January 16, 2019: Bioorganic Chemistry
Li Bai, Hai-Bing Sun, Rui-Ting Liang, Bai-Yan Cai
Soybean ( Glycine max ) is susceptible to root rot when subjected to continuous cropping, and this disease can seriously diminish the crop yield. Proteomics analyses can show the difference of protein expression in different treatment samples. Herein, isobaric tag for relative and absolute quantitation (iTRAQ) labeling and liquid chromatography-tandem mass spectrometry (LC-MS/MS) were employed for proteomic analysis of continuously cropped soybean inoculated with the arbuscular mycorrhizal fungus (AMF) Funneliformis mosseae ...
2019: Frontiers in Microbiology
Suhui Yang, Andrea Shergalis, Dan Lu, Anahita Kyani, Ziwei Lu, Mats Ljungman, Nouri Neamati
Protein disulfide isomerase (PDI) is responsible for nascent protein folding in the endoplasmic reticulum (ER) and is critical for glioblastoma survival. To improve the potency of lead PDI inhibitor BAP2 ((E)-3-(3-(4-hydroxyphenyl)-3-oxoprop-1-en-1-yl)benzonitrile), we designed and synthesized 67 novel analogues. We determined that PDI inhibition relied on the A ring hydroxyl group of the chalcone scaffold and cLogP increase in the sulfonamide chain improved potency. Docking studies revealed that BAP2 and analogues bind to His256 in the b' domain of PDI, and mutation of His256 to Ala abolishes BAP2 analogue activity...
February 13, 2019: Journal of Medicinal Chemistry
Ryosuke Segawa, Mika Shiraki, Shiori Sudo, Kenichi Shigeeda, Taiji Saito, Natsumi Mizuno, Takahiro Moriya, Takayuki Yonezawa, Je-Tae Woo, Masahiro Hiratsuka, Noriyasu Hirasawa
Thymic stromal lymphopoietin (TSLP) is a key epithelial-derived factor that aggravates allergic diseases. Therefore, TSLP inhibitors are candidate compounds for the treatment of allergic diseases. Previously, we reported that KCMH-1, a mouse keratinocyte cell line, constitutively produces TSLP. In this study, we tried to identify inhibitors of TSLP by screening 2169 compounds in KCMH-1 cells and found one such chalcone derivative (code no. 16D10). 16D10 inhibited TSLP expression and TSLP promoter activation in HaCaT cells, a human keratinocyte cell line...
February 9, 2019: European Journal of Pharmacology
Mahmoud S Abdelbaset, Mohamed Abdel-Aziz, Mohamed Ramadan, Mostafa H Abdelrahman, Syed Nasir Abbas Bukhari, Taha F S Ali, Gamal El-Din A Abuo-Rahma
Novel thienoquinoline carboxamide-chalcone derivatives were prepared via the cyclization of acylated chalcones and 2-mercaptoquinoline-3-carbaldehyde in DMF with K2 CO3 . Thienoquinolines 9a-f, h exhibited promising antiproliferative effect against all the tested cell lines and gave a significant activity as EGFR inhibitors, with IC50 values ranging from 0.5 and 3.2 µM, and compounds 9e and 9f being the most active of the series. They also showed better activity than Erlotinib against melanoma cancer cell line A375...
February 5, 2019: Bioorganic & Medicinal Chemistry
Wang Yan, Chen Xiangyu, Li Ya, Wang Yu, Xu Feng
Liver cancer is a kind of high mortality cancer due to the difficulty of early diagnosis. It is necessary to develop the anticancer agents to treat liver cancer. Here, a novel chalcone derivative was synthesized and evaluated for anticancer activity in vitro against liver cancer cell lines (HepG2, SNU-423, SMMC7221, and SNU-398). The chalcone hybrid 9 displayed the antiproliferative effect against HepG2, SNU-423, SMMC7221 and SNU-398 cells with IC50 values of 0.9 μM, 2.7 μM, 6.2 μM and 4.6 μM, respectively...
February 11, 2019: Investigational New Drugs
Seok-Ho Kim, Shin Hee Hong, Young-Joon Park, Jong-Hyuk Sung, Wonhee Suh, Kyeong Won Lee, Kiwon Jung, Changjin Lim, Jin-Hee Kim, Hyoungsu Kim, Kyong Soo Park, Sang Gyu Park
Peroxisome proliferator-activated receptor (PPAR)-α/γ dual agonists have been developed to treat metabolic diseases; however, most of them exhibit side effects such as body weight gain and oedema. Therefore, we developed a novel PPARα/γ dual agonist that modulates glucose and lipid metabolism without adverse effects. We synthesised novel compounds composed of coumarine and chalcone, determined their crystal structures, and then examined their binding affinity toward PPARα/γ. We investigated the expression of PPARα and PPARγ target genes by chemicals in HepG2, differentiated 3T3-L1, and C2C12 cells...
February 7, 2019: Scientific Reports
Caifeng Jiao, Zhenxin Gu
The influences of abscisic acid (ABA)-guanosine 3',5'-cyclic monophosphate (cGMP) on UV-B treatment-stimulated isoflavone synthesis in soybean sprouts was explored. It turned out that ABA, with cGMP, up-regulated gene expression and activity of chalcone synthase (CHS) and isoflavone synthase (IFS), and subsequently induced isoflavone biosynthesis under UV-B treatment. Furthermore, data obtained from the isobaric tags for relative and absolute quantification (iTRAQ) analysis showed that there were two core components in ABA response: SNF1-related protein kinase (SnRK) and type 2C protein phosphatase (PP2C), were up and down regulated after UV-B treatment, respectively...
March 1, 2019: Food Chemistry
Caifeng Jiao, Zhenxin Gu
Abscisic acid (ABA), as a sesquiterpenoid hormone, could regulate lots of physiological processes, especially secondary metabolism in plants. Nevertheless, its mechanism of action, from the perspective of protein expression, remains largely unknown. In the study, isobaric tags for relative and absolute quantitation (iTRAQ) was employed to investigate ABA treatment-induced proteomic changes related to secondary metabolism in soybean sprouts. Among the 3033 proteins identified, compared with the control, ABA treatment up- and down-regulated 350 proteins...
February 2019: Food Research International
Amol Sherikar, Rakesh Dhavale, Manish Bhatia
The main aim of this work is to find out novel chemical moieties with potent anti-inflammatory and vasorelaxant activities with reduced gastric toxicities. For fulfilling the above aim, here we investigated novel chalcones (1, 3-diphenylprop-2-en-1-one derivatives) with nitric oxide (NO) and hydrogen sulfide (H2 S) donating potency for anti-inflammatory activity by carrageenan-induced rat paw edema. These molecules then further evaluated for in-vitro NO-releasing potency and vasorelaxation effect on isolated adult goat aortic tissue...
February 3, 2019: Clinical and Experimental Pharmacology & Physiology
Muhamad Fikri Zaini, Ibrahim Abdul Razak, Mohamad Zahid Anis, Suhana Arshad
The asymmetric unit of the title halogenated chalcone derivative, C15 H10 BrFO, contains two independent mol-ecules, both adopting an s-cis configuration with respect to the C=O and C=C bonds. In the crystal, centrosymmetrically related mol-ecules are linked into dimers via inter-molecular hydrogen bonds, forming rings with R 1 2 (6), R 2 2 (10) and R 2 2 (14) graph-set motifs. The dimers are further connected by C-H⋯O inter-actions into chains parallel to [001]. A Hirshfeld surface analysis suggests that the most significant contribution to the crystal packing is by H⋯H contacts (26...
January 1, 2019: Acta Crystallographica. Section E, Crystallographic Communications
Qin Ai Wong, Tze Shyang Chia, Huey Chong Kwong, C S Chidan Kumar, Ching Kheng Quah, Md Azharul Arafath
The mol-ecular structure of the title chalcone derivative, C15 H10 FNO3 , is nearly planar and the mol-ecule adopts a trans configuration with respect to the C=C double bond. The nitro group is nearly coplanar with the attached benzene ring, which is nearly parallel to the second benzene ring. In the crystal, mol-ecules are connected by pairs of weak inter-molecular C-H⋯O hydrogen bonds into inversion dimers. The dimers are further linked by another C-H⋯O hydrogen bond and a C-H⋯F hydrogen bond into sheets parallel to (104)...
January 1, 2019: Acta Crystallographica. Section E, Crystallographic Communications
Khushboo D Malbari, Anand S Chintakrindi, Lata R Ganji, Devanshi J Gohil, Sweta T Kothari, Mamata V Joshi, Meena A Kanyalkar
The rate of mutability of pathogenic H1N1 influenza virus is a threat. The emergence of drug resistance to the current competitive inhibitors of neuraminidase, such as oseltamivir and zanamivir, attributes to a need for an alternative approach. The design and synthesis of new analogues with alternate approach are particularly important to identify the potential neuraminidase inhibitors which may not only have better anti-influenza activity but also can withstand challenge of resistance. Five series of scaffolds, namely aurones (1a-1e), pyrimidine analogues (2a-2b), cinnamic acid analogues (3a-3k), chalcones (4a-4h) and cinnamic acid linkages (5a-5c), were designed based on virtual screening against pandemic H1N1 virus...
February 1, 2019: Molecular Diversity
Christophe Tratrat, Michelyne Haroun, Iakovos Xenikakis, Evangelia Tsolaki, Phaedra Eleftheriou, Anthi Petrou, Bandar Aldhubiab, Mahesh Attimarad, Katharigatta N Venugopala, Sree Harsha, Heba S Elsewedy, Athina Geronikaki, Marina Soković
BACKGROUND: Thiazole derivates as well as chalcones, are very important scaffold for medicinal chemistry. Literature survey revealed that they possess wide spectrum of biological activities among which are anti-inflammatory and antimicrobial. OBJECTIVES: The current studies describe the synthesis and evaluation of antimicrobial activity of twenty eight novel thiazole-based chalcones. METHODS: The designed compounds were synthesized using classical methods of organic synthesis...
January 29, 2019: Current Topics in Medicinal Chemistry
Bijo Mathew
Due to the structural versatile, chalcones are considered as multi-targeted scaffold for the variety of enzyme targets. The present perspective focused our attention onto the monoamine oxidase inhibitory activity of synthetic chalcones which is synthesized in our lab recently. The studies clearly demonstrated that most of the chalcones showed selective, reversible and potent MAO-B inhibition compared to MAO-A depending upon the substituents bearing around α-β-unsaturated linker of the chalcone scaffold.
January 31, 2019: Central Nervous System Agents in Medicinal Chemistry
Koffi N'Guessan Placide Gabin Allangba, Mélalie Keita, Raymond Kre N'Guessan, Eugene Megnassan, Vladimir Frecer, Stanislav Miertus
We report computer-aided design of new lactone-chalcone and isatin-chalcone (HLCIC) inhibitors of the falcipain-2 (PfFP-2). 3D models of 15 FP-2:HLCIC1-15 complexes with known observed activity (IC50 exp ) were prepared to establish a quantitative structure-activity (QSAR) model and linear correlation between relative Gibbs free energy of enzyme:inhibitor complex formation (ΔΔGcom ) and IC50 exp : pIC50 exp  = -0.0236 × ΔΔGcom +5.082(#); R2  = 0.93. A 3D pharmacophore model (PH4) derived from the QSAR directed our effort to design novel HLCIC analogues...
December 2019: Journal of Enzyme Inhibition and Medicinal Chemistry
Wuttichai Jaidee, Raymond J Andersen, Miguel A G Chavez, Yan A Wang, Brian O Patrick, Stephen G Pyne, Chatchai Muanprasat, Suparerk Borwornpinyo, Surat Laphookhieo
Four new chalcones (1, 10, 13, and 14), a new flavanone, (9), a new amide (8), and 19 known compounds were acquired from Melodorum siamensis. The structures were established by NMR and MS data analyses. Compounds 1 (er 1.4:1) and 2 (er 1.1:1) were scalemic and were resolved to yield (-)-1 and (+)-1 and (-)-2 and (+)-2, respectively. The absolute configurations of these compounds were determined from experimental and calculated ECD data. The structures and configurations of (-)-2 and (+)-8 were identified by single-crystal X-ray diffraction analysis...
January 29, 2019: Journal of Natural Products
Yusuke Ban, Yasumasa Morita, Mika Ogawa, Katsumi Higashi, Takashi Nakatsuka, Masahiro Nishihara, Masayoshi Nakayama
In petals of picotee Petunia cultivars, margin-specific post-transcriptional gene silencing (PTGS) of chalcone synthase A (CHSA) inhibits anthocyanin biosynthesis, resulting in marginal white tissue formation. In this study, we found that a low-molecular-weight compound, fluacrypyrim, inhibits PTGS of CHSA, and we explored the site-specific PTGS operation mechanism. Fluacrypyrim treatment abolished the picotee pattern and eliminated site-specific differences in the levels of anthocyanin-related compounds, CHSA expression, and CHSA small interfering RNA...
January 24, 2019: Journal of Experimental Botany
Beata Żyszka-Haberecht, Anna Poliwoda, Jacek Lipok
Halophilic and freshwater strains of cyanobacteria representing the Oscillatoriales, Nostocales, Chroococcales, and Synechococcales orders of Cyanophyta were examined to determine (i) the resistance of their cultures when suppressed by the presence of exogenous methoxylated and methylated derivatives of 2'-hydroxychalcone, (ii) morphological changes in cells treated with the tested chalcones and, most importantly, (iii) whether these photoautotrophic microorganisms transform chalcone derivatives in a structure- or strain-dependent manner...
January 25, 2019: Journal of Biotechnology
Elvira Escribano-Ferrer, Josep Queralt Regué, Xavier Garcia-Sala, Antoni Boix Montañés, Rosa M Lamuela-Raventos
Flavonoids, found in almost all fruits and vegetables, belong to a class of plant secondary metabolites with a polyphenolic structure and have properties with health-improving potential. However, few experimental studies on the effects of flavonoids have been carried out in vivo after external application and using pure compounds. Aiming to fill this gap, in this study we tested the topical anti-inflammatory and antiallergic activity of three flavonoids of high purity, naringenin, naringenin chalcone, and quercetin, in mouse models...
January 28, 2019: Journal of Natural Products
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