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Furkan Özen, Aslıhan Günel, Arif Baran
In this study, two novel phthalocyanine complexes were synthesized using their corresponding metal salts and 4-(4-(3-(2,4,5-trimethoxyphenyl)acryloyl)phenoxy)phthalo-nitrile as chalcone ligand (4), which was prepared from the reaction of 4-nitrophthalonitrile with 4-hydroxyphenyl-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one (3). These metallophthalocyanines showed good solubility in organic solvents such as CDCl3 , DCM, THF, DMF, and DMSO. The novel phthalocyanine compounds 4a (Pc-Zn) and 4b (Pc-Co) were characterized using their UV-vis, FT-IR, 1 H NMR, 13 C NMR, and MALDI-TOF mass spectra and elemental analysis...
August 4, 2018: Bioorganic Chemistry
Gabriel Silva, Mozart Marins, Nadda Chaichanasak, Yongdae Yoon, Ana Lúcia Fachin, Vitor Caressato Pinhanelli, Luis Octávio Regasini, Mariana Bastos Dos Santos, Gabriela Miranda Ayusso, Beatriz de Carvalho Marques, Wells W Wu, Je-Nie Phue, Rong-Fong Shen, Seung Joon Baek
Naturally-occurring chalcones and synthetic chalcone analogues have been demonstrated to have many biological effects, including anti-inflammatory, anti-malarial, anti-fungal, and anti-oxidant/anti-cancerous activities. Compared to other chalcones, trans-chalcone exhibits superior inhibitory activity in cancer cell growth as shown via in vitro assays, and exerts anti-cancerous effects via the activation of the p53 tumor suppressor protein. Thus, characterization of the specific mechanisms, by which trans-chalcone activates p53, can aid development of new chemotherapeutic drugs that can be used individually or synergistically with other drugs...
2018: PloS One
T N Sanjeeva Murthy, S Naveen, C S Chidan Kumar, M K Veeraiah, Ching Kheng Quah, B P Siddaraju, Ismail Warad
In the title chalcone-thio-phene derivative, C13 H6 Cl3 FOS, the aromatic rings are inclined to one another by 12.9 (2)°, and the thio-phene ring is affected by π-conjugation. In the crystal, mol-ecules are linked by C-H⋯F hydrogen bonds, forming an R 2 2 (8) ring motif. A Hirshfeld surface analysis was conducted to verify the contribution of the different inter-molecular inter-actions. The shape-index surface clearly shows that the two sides of the mol-ecules are involved in the same contacts with neighbouring mol-ecules and the curvedness plots show flat surface patches characteristic of planar stacking...
August 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
Dian Alwani Zainuri, Ibrahim Abdul Razak, Suhana Arshad
The title compounds, C24 H18 O2 and C24 H17 FO2 , were synthesized using the Claisen-Schmidt condensation method and characterized by UV-Vis spectroscopy. Weak inter-molecular C-H⋯O, C-H⋯π and π-π hydrogen-bonding inter-actions help to stabilize the crystal structures of both compounds. The geometrical parameters obtained from the mol-ecular structure were optimized using density functional theory (DFT) calculations at the B3LYP/6-311++G(d,p) level, showing a good correlation with the experimental results...
August 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
Thaís C Muradás, Bruno L Abbadi, Anne D Villela, Fernanda S Macchi, Pedro F Bergo, Talita F de Freitas, Nathalia D M Sperotto, Luis F S M Timmers, Osmar Norberto de Souza, Jaqueline N Picada, Jean Fachini, Juliana Bondan da Silva, Nayara C P de Albuquerque, Maísa D Habenschus, Daniel B Carrão, Bruno A Rocha, Fernando Barbosa Junior, Anderson R M de Oliveira, Alessandra Mascarello, Patrícia Neuenfeldf, Ricardo J Nunes, Héctor R Morbidoni, Maria M Campos, Luiz A Basso, Valnês S Rodrigues-Junior
New effective compounds for tuberculosis treatment are needed. This study evaluated the effects of a series of quinoxaline-derived chalcones against laboratorial strains and clinical isolates of M. tuberculosis. Six molecules, namely N5, N9, N10, N15, N16, and N23 inhibited the growth of the M. tuberculosis H37Rv laboratorial strain. The three compounds (N9, N15 and N23) with the lowest MIC values were further tested against clinical isolates and laboratory strains with mutations in katG or inhA genes. From these data, N9 was selected as the lead compound for further investigation...
2018: PloS One
Yi-Tzu Kuo, Ya-Ting Chao, Wan-Chieh Chen, Ming-Che Shih, Song-Bin Chang
Background and Aims: Orchidaceae is a large plant family, and its extraordinary adaptations may have guaranteed its evolutionary success. Flavonoids are a group of secondary metabolites that mediate plant acclimation to challenge environments. Chalcone synthase (CHS) catalyses the initial step in the flavonoid biosynthetic pathway. This is the first chromosome-level investigation of the CHS gene family in Phalaenopsis aphrodite and was conducted to elucidate if divergence of this gene family is associated with chromosome evolution...
August 2, 2018: Annals of Botany
Yun-Liang Hou, Mei Han, Li-Min Yang, Lin Cheng, Yan Luo
The study is aimed to explore the effect of different temperature on the content of baicalin and gene expression in the growth of Scutellaria baicalensis. Four culture temperatures were used to establish the callus culture of S. baicalensis under dark conditions for 40 days and once every 5 days. The growth and baicalin contents were determined. 18S RNA was used as a reference gene to analyze the five key factors in baicalin biosynthesis pathway (PAL), cinnamic acid 4-hydroxylase (C4H), chalcone synthase (CHS), β-glucuronidase (GUS), baicalein-7- O -glucuronosyltransferase (UBGAT) gene expression levels...
July 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Jianhua Li, Ridao Chen, Ruishan Wang, Xiao Liu, Kebo Xie, Dawei Chen, Jungui Dai
Prenylflavonoids are valuable natural products that have diverse biological properties, and are usually generated biologically by multiple metabolic enzymes in nature. In this study, structurally diverse prenylflavonoids were conveniently synthesized by enzymatic catalysis by combining GuILDT, a regiospecific chalcone prenyltransferase, and GuCHI, a stereospecific chalcone isomerase that has promiscuous activity for both chalcones and prenylchalcones as substrates. Our findings provided a new approach for the synthesis of natural/unnatural bioactive prenylflavonoids, including prenylchalcones and optical prenylflavanones with chalcone origins...
July 2018: Acta Pharmaceutica Sinica. B
Zubair Shanib Bhat, Hafiz Ul Lah, Muzafar Ahmad Rather, Mubashir Maqbool, Tabassum Ara, Zahoor Ahmad, Syed Khalid Yousuf
Tuberculosis is an ever-evolving infectious disease that urgently needs new drugs. In the search for new antituberculosis agents, a library of 3-cinnamoyl-4-hydroxy-6-methyl-2 H -pyran-2-ones (CHPs) ( 2a-2y ) was synthesized and evaluated against a standard virulent laboratory strain of Mycobacterium tuberculosis H37Rv. Out of 25 compounds, 11 , 5 , 7 and 2 ( 2a and 2u ) showed least, moderate, good and appreciable activities, respectively, based on minimum inhibitory concentrations (MICs). Both 2a and 2u exhibited an MIC value of 4 μg ml-1 , which was close to those of standard antituberculosis drugs ethambutol, streptomycin and levofloxacin...
January 1, 2018: MedChemComm
Chandrakant Bagul, Garikapati Koteswara Rao, Venkata Krishna Kanth Makani, Jaki R Tamboli, Manika Pal-Bhadra, Ahmed Kamal
A series of pyrazolo[1,5- a ]pyrimidines substituted at C5 with 1-phenylprop-2-en-1-one ( 6a-q ) and 3-phenylprop-2-en-1-one ( 7a-k ) was synthesized and evaluated for antiproliferative activity. Among them, 6h was found to be the most active compound against the MDA-MB-231 cell line with an IC50 of 2.6 μM . The antiproliferative activity of this series of compounds ranged from 2.6 to 34.9 μM against A549 (lung cancer), MDA-MB-231 (breast cancer) and DU-145 (prostate cancer) cell lines. FACS analysis revealed that these hybrids arrest the cell cycle at the subG1 phase...
September 1, 2017: MedChemComm
Aijaz Ahmad, Mohmmad Younus Wani, Mrudula Patel, Abilio J F N Sobral, Adriano G Duse, Faisal Mohammed Aqlan, Abdullah Saad Al-Bogami
The occurrence of invasive fungal diseases, particularly in immunocompromised patients, is life-threatening and increases the economic burden. The rising problem of multi-drug resistance is becoming a major concern for clinicians. In addition, a repertoire of antifungal agents is far less in number than antibacterial drugs. To combat these problems, combination therapy has gained a lot of interest. We previously reported the synergistic interaction of some mono- and bis-dihydropyrimidinone and thione derivatives with fluconazole and amphotericin B for combination antifungal therapy...
December 1, 2017: MedChemComm
Pierre Regenass, Dayana Abboud, François Daubeuf, Christine Lehalle, Patrick Gizzi, Stéphanie Riché, Muriel Hachet-Haas, François Rohmer, Vincent Gasparik, Damien Boeglin, Jacques Haiech, Tim Knehans, Didier Rognan, Denis Heissler, Claire Marsol, Pascal Villa, Jean-Luc Galzi, Marcel Hibert, Nelly Frossard, Dominique Bonnet
We previously reported small molecules that bind the chemokine CXCL12, not its cognate receptors CXCR4 or CXCR7, and neutralize its biological activity. These neutraligands encompass a chalcone chemotype, and suffer from limitations such as poor chemical stability, solubility and oral activity. Herein, we report a systematic structure-activity relationship study around the first neutraligand of CXCL12, Chalcone 4 (1) resulting in the discovery of pyrimidinone 57 (LIT-927), a novel neutraligand of CXCL12 which displays a higher solubility than 1...
August 14, 2018: Journal of Medicinal Chemistry
Tatiana Takahasi Komoto, Tayná Minervina Bernardes, Thaís Balthazar Mesquita, Luis Felipe Buso Bortolotto, Gabriel Silva, Tamires Aparecida Bitencourt, Seung Joon Baek, Mozart Marins, Ana Lúcia Fachin
In the present investigation, trans -chalcone and licochalcone A were tested against MCF-7 and BT-20 breast cancer cell lines for anti-tumor activity. We found that both chalcones down regulated important genes associated to cancer development and inhibited cell migration of metastatic cells (BT-20). Finally, we observed that licochalcone A reduces the MDR-1 protein, while both chalcones suppress the AURKA protein in a dose-dependent manner. In conclusion, we observed the trans -chalcone and licochalcone A affected the cell viability of breast cancer cell lines MCF-7 and BT-20 and presents anti-metastatic and anti-resistance potential, by the repression of AUKA and MDR-1 proteins...
August 13, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Manh Tuan Ha, Su Hui Seong, Tien Dat Nguyen, Won-Kyung Cho, Kim Jeong Ah, Jin Yeul Ma, Mi Hee Woo, Jae Sue Choi, Byung Sun Min
As part of our continuing research to obtain pharmacologically active compounds from Morus alba L. (Moraceae), four Diels-Alder type adducts (DAs) [morusalbins A-D], one isoprenylated flavonoid [albanin T], together with twenty-one known phenolic compounds were isolated from its root bark. The chemical structures were established using NMR, MS, and ECD spectra. The DAs including morusalbins A-D, albasin B, macrourin G, yunanensin A, mulberrofuran G and K, and albanol B exhibited strong inhibitory activities against both protein tyrosine phosphatase 1B (PTP1B) (IC50 , 1...
August 10, 2018: Phytochemistry
Xu Deng, Yan Wang, Hong-Hua Wu, Weize Zhang, Xueqi Dong, Zhimei Wang, Yan Zhu, Xiu-Mei Gao, Li Li, Ya-Nan Wang, Yan-Tong Xu
Four sesquiterpenoid-chalcone hybrids (nardochalaristolones A-D, 1-4), a pair of epimeric sesquiterpenoid-flavonone hybrids ((2'S)- and (2'R)-nardoflavaristolone A, 5 and 6), and a sesquiterpenoid dimer (dinardokanshone F, 7), all sharing a kanshone C-derived sesquiterpenoid unit, were isolated from the underground parts of Nardostachys jatamansi (D.Don) DC. Their structures were elucidated by analysis of the extensive spectroscopic data, and the absolute configurations were established by analysis of 2D NMR spectroscopic data including NOESY data, combined with comparisons of experimental and calculated electronic circular dichroism spectra...
August 2, 2018: Bioorganic Chemistry
Xiaoning Li, Sijia Wang, Yanhua Lu, Huanhuan Yin, Junhua Xiao, Kai Li, Lei Ma, Yuxun Zhou
Kisspeptin is a multifunctional peptide encoded by the Kiss1 gene that plays critical roles in mammalian puberty onset modulation and fertility maintenance in the hypothalamus. Understanding how Kiss1 expression is regulated is essential for elucidating the molecular mechanisms responsible for these reproductive events. In this study, we constructed an in vitro dual fluorescence reporter system to facilitate high throughput screening of effectors influencing the expression of Kiss1 . In GT1-7 cells, an enhanced GFP gene was placed under the control of the Kiss1 gene regulatory elements and translated together with this gene...
August 2018: FEBS Open Bio
Pouran Makhdoumi, Afshin Zarghi, Bahram Daraei, Gholamreza Karimi
Objectives: Study of the mechanisms involved in cancer progression suggests that cyclooxygenase enzymes play an important role in the induction of inflammation, tumor formation, and metastasis of cancer cells. Thus, cyclooxygenase enzymes could be considered for cancer chemotherapy. Among these enzymes, cyclooxygenase 2 (COX-2) is associated with liver carcinogenesis. Various COX-2 inhibitors cause growth inhibition of human hepatocellular carcinoma cells, but many of them act in the COX-2 independent mechanism...
September 2017: Journal of Pharmacopuncture
Gurupada Hazra, Shiv Pratap, Prasanta Ghorai
An efficient method for the construction of chiral C-P bond via an enantioselective 1,2-hydrophosphenylation followed by an oxa-Michael addition cascade of ortho-formyl chalcones has been developed. This provides the diastereoenriched (cis) 1,3-dihydroisobenzofuryl phosphonates with excel-lent enantioselectivities (up to >99%). The origin of enantio- and diastereoselectivity is induced by using a chiral bifunctional organocatalysts. Further, functionalization to highly enantioselective 3-substituted phthalides has also been demonstrated...
August 7, 2018: Journal of Organic Chemistry
Leydi M Moreno, Jairo Quiroga, Rodrigo Abonia, Jonathan Ramírez-Prada, Braulio Insuasty
A new series of 1,3,5-triazine-containing 2-pyrazoline derivatives ( 8 ⁻ 11 ) a ⁻ g was synthesized by cyclocondensation reactions of [(4,6-bis((2-hydroxyethyl)amino)-1,3,5-triazin-2-yl)amine]chalcones 7a ⁻ g with hydrazine hydrate and derivatives. Chalcones 7a ⁻ g were obtained by Claisen-Schmidt condensation between aromatic aldehydes and triazinic derivative 5 , which was synthesized in high yield by a microwave-assisted reaction. Seventeen of the synthesized compounds were selected and tested by the US National Cancer Institute (NCI) for their anticancer activity against 58 different human tumor cell lines...
August 6, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Olívia Pontes, Marta Costa, Filipa Santos, Belém Sampaio-Marques, Tatiana Dias, Paula Ludovico, Fátima Baltazar, Fernanda Proença
Chalcone and chromene derivatives were synthesized in good yield through simple and effective reactions using innocuous solvents such as water and ethanol and high yielding aldol condensations. Generally, the reactions were performed at room temperature, leading to the isolation of highly pure compounds. These compounds were tested on breast cancer cells (MCF-7 and Hs578T) and breast non-neoplastic cells (MCF-10A). After determination of IC50 value, specific assays were performed to analyze the potential of these compounds, and those bearing halogenated substituents presented enhanced activity comparing to methoxyl or methyl groups...
July 26, 2018: European Journal of Medicinal Chemistry
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