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Mini Reviews in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28443521/synthesis-anticancer-screening-and-molecular-docking-studies-of-new-heterocycles-with-trimethoxyphenyl-scaffold-as-combretastatin-analogues
#1
Korany A Ali, Naglaa A Abdel Hafez, Mohamed A Elsayed, Manal M Elshahawi, Salwa M El-Hallouty, Abd El-Galil E Amr
In this study, synthesis, molecular docking and anticancer screening of new series of substituted heterocycles with trimethoxy phenyl scaffold as Combretastatin analogues were described. Substituted pyridines were synthesized via reaction of (E)-3-(dimethylamino)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (2)with active methylene reagents. Substituted pyrimidines were prepared by the reaction of the enaminone (2) with heterocyclic amines and 6-amino thiouracil. Furthermore, a series of pyrazoles substituted with trimethoxyphenyl scaffold were prepared by reaction of the enaminone 2, with selected examples of hydrazonoyl halides...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28443520/recent-advances-on-3-hydroxyflavone-derivatives-structures-and-properties
#2
Burcu Butun, Gulacti Topcu, Turan Ozturk
Flavonoids are naturally occurring phenolic compounds named as 2-phenyl-1-benzopyran-4-one and classified into several subclasses according to their basic chemical structures such as flavones, flavonols, flavanones, flavanonols, and flavanols. Among them, flavonols (3-hydroxyflavone), containing a 3-hydroxyl group in association with its 4-keto group and double bond between 2- and 3- carbon atoms, have the best electron conjugated skeleton in flavonoid family, providing several resonance structures and chelating ability, through which various pharmacological activities such as antiviral, antitumor, anti-inflammatory, anticholinesterase, cytotoxicity, and particularly high antioxidant activity are demonstrated...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28443519/atranorin-an-interesting-lichen-secondary-metabolite
#3
Elżbieta Studzińska-Sroka, Agnieszka Galanty, Wiesława Bylka
Atranorin, the compound with the depside structure, is one of the most common lichen secondary metabolites, characteristic for numerous lichen families but rarely found in some mosses and higher plants. Over the years various biological properties of atranorin were examined. This review summarises the studies on atranorin, focusing on a number of biological activities in different fields. The literature describes anti-inflammatory, analgesic, as well as wound healing, antibacterial, antifungal, cytotoxic, antioxidant, antiviral, and immunomodulatory activities of the depside...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28443518/limitations-of-current-therapeutic-options-possible-drug-targets-and-scope-of-natural-products-in-control-of-leishmaniasis
#4
Neeraj Tiwari, Mallikarjuna Rao Gedda, Vinod K Tiwari, Surya P Singh, Rakesh K Singh
Soon after the identification of Leishmania parasites,the pentavalent antimony compounds have been the mainstay to treat leishmanial infections, worldwide. These compounds were also considered true antileishmanial but the growing incidences of resistance have forced clinicians to use other options. However, due to unavailability of antileishmanial compounds, few drugs like pentamidine (antimicrobial), amphotericin B (antifungal) or miltefosine (antitumor) agents, which are associated with serious side effects, are currently being used...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28440190/characterization-of-a-novel-polysaccharide-iron-iii-complex-and-its-anti-anemia-and-nonspecific-immune-regulating-activities
#5
Yun Zhang, Fanyi Ma, Jinhua Zhu, Zuliang Du, Yingyong Zhao, Xiuhua Liu
Dioscorea opposita Thunb. is the famous food and traditional medicine in China and it was rich in polysaccharides. Polysaccharides of D. Opposita Thunb. possess immunoregulatory activity, free radical scavenging activity and anti-diabetic activity. A novel polysaccharide-iron(III) complex (CYPIC) was synthesized by using crude polysaccharide extracted from Dioscorea opposita Thunb. The component, structure, morphology and molecular weights of CYPIC were analysed, and the anti-anemia, acute toxicity and nonspecific immune regulating activities of CYPIC were assayed...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425868/pomegranate-as-a-possible-treatment-in-reducing-risk-of-developing-wound-healing-obesity-neurodegenerative-disorders-and-diabetes-mellitus
#6
Manaf AlMatar, Md Rashedul Islam, Othman Albari, Işıl Var, Fatih Köksal
Four distinguished although overlying stages make up the methodical procedure of wound healing, which are hemostasis, inflammation, proliferation and remodelling. Multiple sclerosis (MS) comprises a persistent inflammatory infection of the central nervous system, and is related to demyelination, neurodegeneration, as well as susceptibility to oxidative pressure. Obesity signifies a swiftly developing danger to the wellbeing of populations in a rising number of nations. Usually called diabetes mellitus (DM) by medical practitioners, diabetes details a collection of metabolic diseases within which the individual has raised blood glucose, either due to an insufficiency of insulin generation, or the lack of suitable response by the body to insulin, or both...
April 19, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425867/chemokines-and-relevant-micrornas-in-the-atherogenic-process
#7
Dimitry A Chistiakov, Alexander N Orekhov, Yuri V Bobryshev
Chemokines play a significant role in initial and advanced steps of atherogenesis. In early steps, chemokines control the adhesion of leukocytes to endothelial cells (ECs) followed by transmigration of monocytes and their deposition in the intima where they differentiate to proinflammatory macrophages. Except proinflammatory activity, chemokines are responsible for homeostasis and homing of progenitor cells. Recently, microRNAs (miRs) were found to control expression and activity of chemokines in ECs, vascular smooth muscle cells (VSMCs), and macrophages at different steps of atherogenesis...
April 19, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425866/recent-development-of-oridonin-derivatives-with-diverse-pharmacological-activities
#8
Weiyan Cheng, Chuanhui Huang, Weifeng Ma, Xin Tian, Xiaojian Zhang
Oridonin is one of the major components isolated from Isodon rubescens, a traditional Chinese medicine, and it has been confirmed to exhibit many kinds of biological activities including anticancer, anti-inflammation, antibacterial and so on. However, the poor pharmaceutical property limits the clinical applications of oridonin. So many strategies have been explored in the purpose of improving the potencies of oridonin, and structure modification is one thus way. This review outlines the landscape of recent development of oridonin derivatives with diverse pharmacological activities, mainly focusing on the biological properties, structure-activity relationships, and mechanism of actions...
April 17, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403794/ultrasound-assisted-synthesis-of-quinoline-derivatives-in-the-presence-of-sncl2%C3%A2-2h2o-as-a-precatalyst-in-water-evaluation-of-their-antibacterial-activities
#9
A S G Prasad, T Bhaskara Rao, D Rambabu, Mandava V Basaveswara Rao, Manojit Pal
SnCl2•2H2O has been used as a convenient precatalyst for the one-pot and rapid synthesis of 2-substituted quinolines under ultrasound irradiation in water. The reaction involved a 3-component reaction of aniline, aldehydes and ethyl 3,3-diethoxypropionate in the presence of aerial oxygen to give the desired products in good yields. Several of these compounds showed antibacterial activities when tested against gram-positive and gram-negative species. One compound i.e. 4b showed promising activities across both the species...
April 12, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28325147/berberine-derivatives-with-different-pharmacological-activities-via-structural-modifications
#10
Daipeng Xiao, Zhenbao Liu, Shanshan Zhang, Mi Zhou, Fen He, Ming Zou, Junying Peng, Xiong Xie, Yanfei Liu, Dongming Peng
Berberine, a quaternary ammonium protoberberine alkaloid with an isoquinoline scaffold isolated from medicinal herbs, exhibits a wide spectrum of pharmacological activities. Berberine has been used in traditional Chinese medicine and Ayurvedic medicine. However, it has poor bioavailability, which seriously limits its application and development. The chemical transformation of natural products is an effective method to improve pharmacological activities. Researches have been carried out on the modification of berberine to obtain better pharmacological properties...
March 21, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28302042/natural-anti-cancer-agents-implications-in-gemcitabine-resistant-pancreatic-cancer-treatment
#11
Bishal Marasini, Ravi P Sahu
Pancreatic cancer is one of the most lethal malignancy accounting for the fourth leading cause of cancer-related deaths in the United States. Among several explored anti-cancer agents, Gemcitabine, a nucleoside analogue remained a front line chemotherapeutic agent for the treatment of pancreatic cancer. However, gemcitabine exerts a low response rate with limited progression free survival in cancer patients due to cellular resistance of pancreatic tumors to this therapy. Several chemotherapeutic agents have been explored in combination with gemcitabine against pancreatic cancer with overall mixed responses and survival rates...
March 15, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28302041/promises-of-machine-learning-approaches-in-prediction-of-absorption-of-compounds
#12
Rajnish Kumar, Anju Sharma, Mohammed Haris Siddiqui, Rajesh Kumar Tiwari
The Machine Learning (ML) is one of the fastest developing techniques in prediction and evaluation of important pharmacokinetic properties such as absorption, distribution, metabolism and excretion. The availability of large number of robust validation techniques for prediction models devoted to pharmacokinetics have significantly enhanced the trust and authenticity in ML approaches. There are series of prediction models generated and used for rapid screening of compounds on the basis of absorption in last one decade...
March 15, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28302040/trypanothione-reductase-a-target-for-the-development-of-anti-trypanosoma-cruzi-drugs
#13
Karina Vázquez, Margot Paulino, Cristian O Salas, Juan J Zarate-Ramos, Brenda Vera, Gildardo Rivera
Chagas disease or American trypanosomiasis is a major parasitic disease in Latin America with treatment available via two drugs: nifurtimox and benznidazole. These two treatments are ineffective in the chronic phase of the disease. Therefore, there is a need for the development of new, efficient and safe drugs for the treatment of these diseases. With this goal, one of the promising targets proposed is the trypanothione reductase (TR), a key enzyme important in the metabolism of Trypanosoma cruzi. In this review, we analyze the importance of TR as a drug target, as well as their compounds inhibitors reported in the last decade as potential therapeutic agents for Chagas disease...
March 15, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28302039/bone-degeneration-inflammation-and-secondary-complications-of-arthritis-potential-targets-and-their-natural-inhibitors
#14
Mahadevappa Hemshekhar, Ram M Thushara, Somanatahpura K NaveenKumar, Paul Manoj, Mahalingam S Sundaram, Kempaiah Kemparaju, Kesturu S Girish
Arthritis is marked with joint deterioration that affects articular cartilage and subchondral bone. Though cartilage degradation is a major damage during arthritis, the subsequent bone loss cannot be neglected. Progress in the arthritis research has identified clinical importance of bone erosion in destructive arthritis. Studies have showed the key role played by osteoclasts and receptor activator of nuclear factor kappaB ligand (RANKL) signaling in bone erosion. Cathepsins and tartrate resistant acid phosphatase (TRAP) are considered key enzymatic factors contributing to bone erosion...
March 15, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28302038/current-application-of-quantum-dots-qd-in-cancer-therapy-a-review
#15
Lavanya Thilak Babu, Priyankar Paira
Semiconductor quantum dots proved themselves as an efficient fluorescent probes in cancer detection and treatment. Their size, high stability, non-photobleaching and water solubility made them a unique fluorophore in place of conventional organic dyes. Newly emerged theranoistic drug delivery system using quantum dots helped us in better understanding of the drug delivery mechanism inside the cells. Surface modified Quantum dots and their applications became wide in bioimaging, immunohistochemistry, tracking intracellular drug and intracellular molecules target...
March 15, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28302037/recent-advances-in-the-catalytic-one-pot-synthesis-of-flavonoids-and-chromones
#16
Manijeh Mohadeszadeh, Mehrdad Iranshahi
Flavonoids and chromones are two important classes of natural products that have various biological properties. During the past 10 years, there has been a significant increase in studies on the one-pot synthesis of flavonoids and chromones as medicinal scaffolds in drug discovery. This review describes the scope, mechanistic properties and regio- and chemo-selectivity features of several recently developed one-pot procedures for the synthesis of substituted chromones and flavonoids that have recently been published...
March 15, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28271816/an-overview-on-application-of-natural-substances-incorporated-with-electrospun-nanofibrous-scaffolds-to-development-of-innovative-wound-dressings
#17
Nosratollah Zarghami, Roghayeh Sheervalilou, Amir Fattahi, Abbas Mohajeri, Mehdi Dadashpour, Younes Pilehvar-Soltanahmadi
Conventional dressings are cost-effective and highly absorbent, but not effectual enough to promote hemostasis, adherence and in holding a moist wound bed. Thanks to the developments in the field of nanotechnology and bioengineering, one of the promising current trends is to move progress of innovative wound dressings, merging the application of traditional healing agents and modern products/practices, such as hydrocolloids, hydrogels, films and nanofibers. The electrospun nanofibers webs can provide the essential parameters require for wound dressing to heal wounds including absorptivity, oxygen permeability, and non-adherence to the healing tissue, barrier to bacteria, bioactivity and occlusivity...
March 8, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28245783/advance-in-anti-tumor-mechanisms-of-shikonin-alkannin-and-their-derivatives
#18
Xu Zhang, Jia-Hua Cui, Qing-Qing Meng, Shao-Shun Li, Wen Zhou, Sui Xiao
Shikonin, alkannin and their derivatives, the main ingredient of Lithospermum erythrorhizon native to Inner Mongolian and Northwest of China, displayed good antitumor effects via multiple-target mechanisms. This review focus on their antitumor mechanisms from the direct reaction and the indirect reaction aspects, and expounded the death of tumor cells caused by shkionin, akannin and derivatives, which are involved in the ROS-mediated mechanisms and direct interaction with DNA and protein.
February 28, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28245782/reactive-oxygen-and-nitrogen-species-in-carcinogenesis-implications-of-oxidative-stress-on-the-progression-and-development-of-several-cancer-types
#19
Joanna Kruk, Hassan Y Aboul-Enein
BACKGROUND: The body of evidence available from published literature during the past three decades indicates that reactive oxygen species and reactive nitrogen species can induce, promote and modulate carcinogenesis. OBJECTIVE: The purpose of this review was to present current status of knowledge on the possible role of oxidative/nitrosative stress in the development and progression of several human cancers. Moreover, we discuss briefly the formation and decomposition of oxygen and nitrogen species within cells and their physiological and damaging influences...
February 28, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28245781/endogenous-and-exogenous-natural-adjuvants-for-vaccine-development
#20
Azam Bolhassani, Somayeh Talebi, Ali Anvar
Various adjuvants are usually co-injected with an antigen for stimulation of effective immune responses. Their mechanisms of action in vaccine development include: a) enhancement of the total antibody titers; b) reduction of the antigen dose; c) induction of potent cell-mediated immunity; d) increase in the speed and duration of the protective response; e) stimulation of mucosal immunity; and f) cross-protection. Up to now, different exogenous adjuvants have been identified to boost immune responses including inorganic compounds (e...
February 28, 2017: Mini Reviews in Medicinal Chemistry
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