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Mini Reviews in Medicinal Chemistry

Tian-Jun Ma, Jie Gao, Yan Liu, Jian-Hua Zhuang, Chuan Yin, Peng Li, Lei Mao, Jin Xu, Yi-Xin Xu, Yan-Peng Li, Zhong-Xin Zhao, You Yin
Background Alzheimer's disease (AD) is one of the most devastating diseases worldwide. The current drugs for AD can only ameliorate the symptoms rather than reverse or prevent the progress of AD. On the other hand, blood-brain barrier (BBB), as a natural barrier, significantly impedes drug delivery from the blood circulation into the brain. Nanomedicine can be a safe, effective and promising approach to treat AD. Objective This review summarizes the recent nanomedicine research in this area, including the use of liposomes and nanoparticles (NPs), to provide new approach for targeted treatment of AD...
December 15, 2017: Mini Reviews in Medicinal Chemistry
Sarita Sarkar, Kakali Bhadra
BACKGROUND: Harmalol, a beta carboline alkaloid, shows remarkable importance in the contemporary biomedical research and drug discovery programs. With time, there is growing interest in search for anti-cancer drugs of plant origin with high efficacy, low toxicity and minimum side effects. Most of the chemotherapeutic agents due to their non-selective nature and dose limiting toxicity, use is often restricted, necessitating search for newer drugs having greater potentiality. OBJECTIVE: The review highlighted the interaction of harmalol with nucleic acids of different motifs as sole target biomolecules and in vitro cytotoxicity of the alkaloid in human cancer cell lines with special emphasis on its apoptotic induction ability...
December 11, 2017: Mini Reviews in Medicinal Chemistry
Yang Liu, Gangliang Huang
Polysaccharides are a kind of biological macromolecules with immune regulation, anti-tumor, anti-radiation, anti-inflammation, anti-fatigue and anti-aging effects. These effects are related to their antioxidant properties. The action mechanisms of antioxidation and scavenging free radicals for polysaccharides were reviewed. The polysaccharides contain plant polysaccharides, animal polysaccharides and microbial polysaccharides. The recent research progresses and our work on antioxidant properties of polysaccharides and their derivatives were summarized...
December 7, 2017: Mini Reviews in Medicinal Chemistry
Salwa F Mohamed, Eman M H Abbas, Hemat S Khalaf, Thoraya A Farghaly, Dina N Abd El-Shafy
Merged pyrimidine derivatives were designed by one pot synthesis of pyrimidinethione derivative with halogenated compounds. The structure of all prepared compounds was characterized by their spectroscopic data and also, their ability to inhibit the in vitro replication of HSV-1 was estimated. Amongst the tested compounds 2-acetyl-3-methyl-5-(p-tolyl)indeno[1,2-d]thiazolo[3,2-a]pyrimidin-6(5H)-one (9b) and ethyl 3-methyl-6-oxo-5-(p-tolyl)-5,6-dihydroindeno[1,2-d]thiazolo[3,2-a]pyrimidine-2-carboxylate (9c), caused viral inhibition over 90%...
December 7, 2017: Mini Reviews in Medicinal Chemistry
Rakesh Gupta, Hardik Joshi, C S Ramaa
Thiazolidine-2,4-dione (TZD), one of the most frequently encountered heterocyclic ring which has been implicated in design and synthesis of entities for various pathogenic conditions including cancer. Since its discoveryvarious substitutions at 5th position has been carried out and reviewed. Various substitutions at 5th position has led to generation of glitazones, whose target peroxisome proliferating activated receptor γ (PPARγ) was found decade after their discovery.Acidichydrogen (-NH) of TZD is prime pharmacophoric requirement for activation of PPARγ...
November 29, 2017: Mini Reviews in Medicinal Chemistry
Qian-Qian Xu, Kui-Wu Wang
Withanolides are a group of highly oxygenated steroids derived from a C28 ergostane skeleton, and have attracted significant scientific interest due to their complex structural features and multiple bioactivities. More than 170 new natural withanolides were isolated and identified in the last 5 years. This review provides a comprehensive summary of the structural, biological and pharmacological activities and distribution of these new compounds.
November 29, 2017: Mini Reviews in Medicinal Chemistry
Bidisha Sarkar, Priyankar Paira
Theranostic agents or theranostic imaging as its name suggests is a combination of two terms-'diagnosis' & 'therapy'. Efforts are being made to combine both the terms into clinical formulations. This theranostic imaging is found to be very much significant to complex diseases like cancer and proliferative tumors specially now that protionic and genomic profiling can provide an accurate 'fingerprint' of each tumor, with all such kinds of informations theranostic agents can be designed in such a way that it is specific in its action and selective towards the cancer cells only, without causing any adverse effects on the normal tissue cells...
November 29, 2017: Mini Reviews in Medicinal Chemistry
George Perry
No abstract text is available yet for this article.
2018: Mini Reviews in Medicinal Chemistry
Jian Tang, Aun Raza, Jian Chen, Huaxi Xu
Sinomenine is one of the most widely known alkaloids owing to different therapeutic properties including anti-inflammatory and immunosuppressive activities, as well as the potency in neurodegenerative disorders, such as Alzheimer's disease and Parkinson's disease. Sinomenine has being studied as a potential anti-inflammatory agent through appropriate structural modifications. Recently, a number of such approaches have been attempted in various laboratories with great success. Several series of derivatives have been synthesized with changes at rings A, B, C and D...
November 23, 2017: Mini Reviews in Medicinal Chemistry
Shweta Jain, Satyanarayan Pattnaik, Kamla Pathak, Sushant Kumar, Devender Pathak, Surendra Jain, Ankur Vaidya
Thiazole nucleus is one of the most important and well-known heterocyclic nuclei that possesses almost all types of biological activities. Thiazole compounds play an important role in anticancer drug development as they have shown excellent results through different mechanism of action. A number of thiazole derivatives have been reported till date for their anticancer activity. The present review is complementary to earlier reviews and aims to review the work reported on the anticancer activity of thiazole derivatives from year 2000 to the beginning of 2016...
November 23, 2017: Mini Reviews in Medicinal Chemistry
Muhammad Hassan Safdar, Humna Hasan, Sajal Afzal, Zahid Hussain
BACKGROUND: The immune system is an intricate and coordinated nexus serving as a natural defense to preclude internal and external pathogenic insults. The deregulation in the natural balance of immunological functions, as a consequence of either over expression or under expression of immune cells may cause development of numerous immune disorders. Chalcone moieties (1,3-diphenyl-2-propen-1-one) have been well-documented as ideal lead compounds or precursors to design wide range of pharmacologically active agents to down-regulate various immune disorders...
November 23, 2017: Mini Reviews in Medicinal Chemistry
Qu Renyu, Liu Yuchao, W M Wishwajith W Kandegama, Chen Qiong, Yang Guangfu
The triazolopyrimidine ring is a ubiquitous structural feature of many active compounds with diversified pharmacology efficacy. These structures have aroused our / researchers interests in the development of novel compounds with anticancer, anti-inflammatory, antibacterial, antifungal, and other activities. A large number of published literatures were reviewed during the last few decades. This review contains various pharmacological and agrochemical activities of triazolopyrimidine and it may be regarded as the lead compound for the new research towards future medicinal and agrochemical development...
November 1, 2017: Mini Reviews in Medicinal Chemistry
Leilei Shi, Wei Hu, Jifeng Wu, Huaiyu Zhou, Hua Zhou, Xun Li
Among the family of nitrogen-containing heterocycles, quinoxalinone (or quinoxalin-2-one) core, characterized by pyrazin-2(1H)-one fused to benzene ring at two adjacent carbon atoms, has been frequently found in a variety of pharmacologically active compounds with biological or pharmaceutical applications. It was gratifying that a larger part of these bioactive quinoxalinone-based derivatives have entered various clinical trials, which in turn hastens the synthetic versatility and also initiates various derivatization of quinoxalinone scaffold...
November 1, 2017: Mini Reviews in Medicinal Chemistry
Yogita Bansal, Manjinder Kaur, Gulshan Bansal
Structural resemblance of benzimidazole nucleus with purine nucleus in nucleotides makes benzimidazole derivatives attractive ligands to interact with biopolymers of a living system. The most prominent benzimidazole compound in nature is N-ribosyldimethylbenzimidazole, which serves as an axial ligand for cobalt in vitamin B12. This structural similarity prompted medicinal chemists across the globe to synthesize a variety of benzimidazole derivatives and to screen those for various biological activities, such as anticancer, hormone antagonist, antiviral, anti-HIV, anthelmintic, antiprotozoal, antimicrobial, antihypertensive, anti-inflammatory, analgesic, anxiolytic, antiallergic, coagulant, anticoagulant, antioxidant and antidiabetic activities...
October 31, 2017: Mini Reviews in Medicinal Chemistry
Stephen Paul Avvaru, Malleshappa N Noolvi, Tejraj M Aminabhavia, Sudipta Chakraborty
Aromatase inhibitors are class of drugs that inhibit aromatase, a rate limiting enzyme in the biosynthesis of estrogens from their corresponding androgens. Estrogens play a vital role in the development and growth of breast tumors especially in postmenopausal women apart from their important functions in cell homeostasis. The reduction of estrogen physiological concentration through aromatase inhibition is one of the most important therapeutic strategies against this cancer type. The third-generation aromatase inhibitors are now used as first-line therapy in the treatment of early and metastatic breast cancer in postmenopausal women...
October 31, 2017: Mini Reviews in Medicinal Chemistry
Shaoyong Ke
Steroid and its derivatives have been proved to have important and diverse biological functions, which present the wide spectrum of biological activities such as antitumor, antiviral, antibacterial, antimicrobial, antifungal, antioxidant, insecticidal, aromatase inhibitors, 5α-reductase inhibitors and neuromuscular blocking agents et c. Versatile features of steroid-derived compounds have emerged, so the aim of the present paper was to review the recent advances of steroid-based derivatives mainly focused on their structures and biological properties...
October 3, 2017: Mini Reviews in Medicinal Chemistry
Roberta Napolitano, Serena De Matteis, Alessandro Lucchesi, Silvia Carloni, Delia Cangini, Gerardo Musuraca, Eliana Valentina Liardo, Marianna Norata, Pier Paolo Fattori
Background Chronic lymphocytic leukemia (CLL) is an indolent B-lineage neoplasm, characterized by clonal expansion of CD5 positive B cells with constitutive activation of survival pathways including NF-kB. Pentoxifylline, a xanthine-derivative compound indicated for the treatment of microvascular disturbancies, has been suggested to have anti-proliferative and anti-metastatic activities in various types of cancer. In the present study we extend these data showing one of the potential molecular mechanisms through which Pentoxifylline may promote apoptosis in CLL clonal lymphocytes...
October 2, 2017: Mini Reviews in Medicinal Chemistry
Michela I Simone, Laura Mares, Clothilde Eveleens, Adam McCluskey, Brighid B Pappin, Milton J Kiefel, Todd A Houston
Glycosidases have important anti-cancer, anti-viral and anti-diabetic properties. This review covers the literature in the past 15 years since our initial review in this journal on "neutral" glycosidase inhibitors lacking a basic nitrogen found in iminosugars and azasugars or inhibitors that are neutral by virtue of being "charge-balanced" (zwitterionic). These structurally diverse inhibitors include lactones, lactams, epoxides such as cyclophellitol, and sulfonium ion derivatives of the natural product salacinol...
October 2, 2017: Mini Reviews in Medicinal Chemistry
Weibin Li, Meng Zhao, Kaiyu Wang, Huihui Yan, XIaopeng Lan
Aptamers are single-stranded DNA or RNA oligonucleotides generated by a novel in vitro selection technique termed Systematic Evolution of Ligands by Exponential Enrichment (SELEX). During the past two decades, various aptamer drugs have been developed and many of them have entered into clinical trials. In the present review, we focus on aptamers as potential therapeutics for hematological diseases, including anemia of chronic inflammation (ACI) and anemia of chronic disease (ACD), hemophilia, thrombotic thrombocytopenic purpura (TTP) or VWD type-2B, and sickle cell disease (SCD), in particular, those that have entered into clinical trials...
October 2, 2017: Mini Reviews in Medicinal Chemistry
Adali Pecci, Lautaro D Alvarez, Diego M Presman, Gerardo Burton
Glucocorticoids are steroid hormones that exert most of their effects through their binding to the glucocorticoid receptor (GR), a ligand regulated transcription factor. Although glucocorticoids are widely used in the clinic, their usage in chronic therapies provokes severe adverse reactions. In the quest for safer glucocorticoids a dissociated model was established that proposes a disconnection between GR activated pathways responsible of desired pharmacological effects and pathways involved in adverse GR reactions...
October 2, 2017: Mini Reviews in Medicinal Chemistry
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