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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
David Young, Manoharan K Pillai, Mohamed Majid
The plant Alpinia officinarum of the ginger family originated in China and is used throughout South and South-East Asian countries to flavour food and as a traditional medicine to treat a variety of diseases. This review summarizes the biological, pharmacological and phytochemical properties of extracts and subsequently isolated compounds from A. officinarum. In vitro and in vivo studies of both extracts and pure compounds indicate a wide variety of potent bioactivities including anti-inflammatory, antibacterial, antioxidant, antiobesity, anticancer, enzyme inhibitory and remarkable antiviral properties...
October 2, 2017: Mini Reviews in Medicinal Chemistry
Burak Yulug, Lütfü Hanoglu, Elmir Ksanmemmedov, Ozge Arıcı Düz, Burcu Polat, Taha Hanoglu, Mehmet Yalçin Günal, Ertugrul Kilic
There are limited studies in the literature evaluating region specific neuroprotective effects of repetitive transcranial magnetic stimulation (rTMS) in Alzheimer's Disease. Here, we aimed to review the neurochemical correlates of the hippocampal neuroprotective effect of rTMS in various preclinical and clinical studies. Our findings indicate that rTMS may exert a significant neuroprotective effect through acting on the hippocampal Brain Derived Growth Factor (BDNF) levels which may, in turn, slow the progression of Alzheimer's Disease...
September 27, 2017: Mini Reviews in Medicinal Chemistry
Jaya Dwivedi, Swapnil Sharma, Sonika Jain, Aarti Singh
Pyrazole nucleus is a unique structural scaffold which acts as an interesting template for combinatorial as well as medicinal chemistry. This review presents a detailed overview on the synthesis, QSAR and pharmacological applications of pyrazole. In addition, it covers most recent reports on structural modifications on pyrazole illustrating vital structural activity relationship.
September 27, 2017: Mini Reviews in Medicinal Chemistry
Mona O Sarhan, Mohamed A Motaleb, Ismail T Ibrahim, Wafaa A Zaghary, Manal M Anwar
1,3,5-Triazine-based compounds form a privileged class of compounds in the medicinal chemistry field as they are versatile synthetic scaffolds possessing wide spectra of biological effects including potential anticancer activity. 1,3,5-Triazine compounds explored for anticancer activities have been reported to act by various mechanisms on several molecular targets in human cells such as methyltransferase (DNMT), heat shock protein 90 (Hsp90) and phosphoinositide 3-kinase (PI3K). This review focuses on the synthetic strategies for current developments of 1,3,5-triazine-based anticancer agents and discuses the docking studies that confirm their unique binding modes in the targeted receptors active sites...
September 27, 2017: Mini Reviews in Medicinal Chemistry
Farida Hussan, Mohamad Fairuz Yahaya, Seong Lin Teoh, Srijit Das
The incidence of diabetes mellitus (DM) has increased globally. Various complications such as blindness, nephropathy leading to renal failure, neuropathy, foot ulceration, amputation, and disturbance in autonomic nervous system have been reported. Although, allopathy treatment still remains the treatment of choice, there is a need to look at the easy availability, patient compliance and cheaper cost of the drugs used in day-day practice. In this regard, complementary and alternative medicine has a greater role to play...
September 27, 2017: Mini Reviews in Medicinal Chemistry
Alla P Toropova, Andrey A Toropov
The applications of optimal molecular descriptors as a tool to predict endpoints related to medicinal chemistry are listed. The general scheme of building up of the optimal descriptors is represented in detail. Simplified molecular input-line entry system (SMILES) is using to represent the molecular architecture. The optimal descriptor is the sum of correlation weights of molecular fragments extracted from SMILES. The numerical data on the correlation weights are calculated by the Monte Carlo method. The data should provide maximal correlation coefficient between experimental values of endpoint and corresponding values of the optimal descriptor...
September 27, 2017: Mini Reviews in Medicinal Chemistry
Jignesh Lunagariya, Poonam Bhadja, Shenghui Zhong, Rohit Vekariya, Shihai Xu
Marine bis-indole alkaloids comprise a large and increasingly growing class of secondary metabolites, and continue to deliver a great variety of structural templates. The alkaloids derived from marine resources play a crucial role in medicinal chemistry and as chemical agents. In particular, bis-indole alkaloid caulerpin isolated from marine green algae Caulerpa and a red algae Chondria armata at various places around the world, and tested against several therapeutic areas such as anti-diabetic, antinociceptive, anti-inflammatory, anti-tumor, anti-larvicidal, anti-herpes, anti-tubercular, anti-microbial and immunostimulating activity as well as means of other chemical agents...
September 27, 2017: Mini Reviews in Medicinal Chemistry
Mateus Feitosa Alves, Diogo Vilar da Fonsec, Sílvia Adelaide Linhares de Melo, Marcus Tullius Scotti, Luciana Scotti, Sócrates Golzio Dos Santos, Margareth de Fátima Formiga Melo Diniz
Asthma is an inflammatory disease which affects millions of people worldwide. Therefore, it is necessary search for new sources of therapies for the treatment of these patients in order to improve their quality of life. From content analysis of new therapeutic targets literature, there are various targets and drugs reported as promising for treatment asthma. Interleukins involved in inflammatory processes are often presented as candidate targets for new drugs. The action of such therapeutics would not only affect interleukins, but also in their receptors...
September 27, 2017: Mini Reviews in Medicinal Chemistry
Diksha Sharma, Virendra Pratap Singh, Narendra Kumar Singh
Mushrooms have an established history of use in traditional oriental medicine. Higher Basidiomycetes mushrooms contain biologically active compounds in fruit bodies, cultured mycelium, and cultured broth. Medicinal mushrooms possess medicinal properties such as anti-tumor, immunomodulating, antioxidant, cardiovascular, anti-hypercholesterolemic, anti-viral, anti-bacterial, anti-parasitic, anti-fungal, detoxification, hepatoprotective, and anti-diabetic effects. Several compounds isolated from medicinal mushrooms have been subjected to Phase-I, II, and III clinical trials, and are used extensively to treat various diseases including cancer...
September 27, 2017: Mini Reviews in Medicinal Chemistry
Letitia Meiring, Jacobus P Petzer, Anél Petzer
The 3,4-dihydro-2(1H)-quinolinone moiety is present in a number of pharmacologically active compounds. These include registered drugs such as cilostazol, carteolol and aripiprazole as well as numerous experimental compounds. Compounds containing the 3,4-dihydro-2(1H)-quinolinone moiety also exhibit a variety of activities in both the peripheral en central tissues, which includes phosphodiesterase inhibition, blocking of β-adrenergic receptors, antagonism of vasopressin receptors and interaction with serotonin and dopamine receptors...
September 27, 2017: Mini Reviews in Medicinal Chemistry
Priyanshu R Rai, Rakesh R Somani, Pooja S Kandpile
Ornithine decarboxylase is the first enzyme in the polyamine biosynthetic pathway. It is the rate-limiting enzyme which is included in the change of ornithine to putrescine which is the first polyamine. Polyamines (putrescine, spermidine, spermine) are natural and synthetic compounds which contains two or more amino group. Polyamines are highly implicated in cellular functions such as cell-growth & multiplication, DNA stabilization, gene transcription and translation, ion-channel activity, etc. Elevated levels of polyamines were found in highly proliferating tumour cells...
September 27, 2017: Mini Reviews in Medicinal Chemistry
Tingting Li, Ting Ding, Jianrong Li
The environment of marine occupies about 95% biosphere of the world and can be a critical source of bioactive compounds for human to be explored. Special environment such as high salt, high pressure, low temperature, low nutrition and no light, etc. has created the particularity of marine organisms, to make them produce bioactive substances different from terrestrial organisms. Natural ingredients secreted by marine-derived bacteria, fungi, actinomycetes, cyanobacteria and other organisms have been separated as actively pharmacophores...
September 26, 2017: Mini Reviews in Medicinal Chemistry
Jie-Bin Zhou, Rong Luo, Ying-Lin Zheng, Ji-Yan Pang
Numerous studies have indicated that marine natural products are one of the most important sources of the lead compounds in drug discovery for their unique structures, various bioactivities and less side effects. In this review, the marine natural products with cardiovascular pharmacological effects reported after 2000 will be presented. Their structural types, relevant biological activities, origin of isolation and information of strain species will be discussed in detail. Finally, by describing our studies as an example, we also discuss the chances and challenges for translating marine-derived compounds into preclinical or clinical trials...
September 26, 2017: Mini Reviews in Medicinal Chemistry
Ajita Bhatt, Ekta Gurnany, Anuj Modi, Arvind Gulbake, Aviral Jain
Cancer is one of the most important causes of morbidity and mortality all across the world. On an average, every year approximately 238,000 new cases of brain and other central nervous system tumors are diagnosed around the world. Amongst all, tumors of brain account for nearly 85% to 90% of all primary central nervous system (CNS) tumors. Regardless of tremendous scientific efforts to develop newer diagnostic techniques and latest therapy, the management of brain cancer is still challenge in neuro-oncology...
September 26, 2017: Mini Reviews in Medicinal Chemistry
Andrea Rague, Kevin Joseph Tidgewell
The serotonin system exerts its effects on the CNS and many peripheral systems. Of the 14 serotonin receptors, the 5-HT7 receptor is the most recently discovered. The 5-HT7 receptor has been shown to be involved in stress reduction, depression, and nociceptive control. Despite the 20 years since the discovery of 5-HT7R, there are still few truly selective ligands. Two of the common scaffolds for 5-HT7R ligands are long chain arylpiperazines (LCAPs) and sulfonamide containing compounds. This review focuses on recently developed (2014-2016) 5-HT7R ligands, their selectivity for the receptor, and suggests possible new pharmacophore models for these ligands...
September 12, 2017: Mini Reviews in Medicinal Chemistry
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