Innovative materials against tumour to decrease remarkably the number of persons died by cancer are desired eagerly. To innovate in the medical technologies, tumour accumulative sugar dendritic Gd-DTPA complex MRI contrast agent (DEN-OH) and IER5/Cdc25B targeted novel phospha sugar antitumour agents (TBMPP) were prepared and evaluated preclinically. These novel medicinal materials were revealed to exert excellent characteristics against tumour cells. DEN-OH was prepared by introduction of protected sugar dendritic parts to the ligand of diethylenetriamine pentaacetic acid (DTPA) and the successive complex formation with Gd (III) and hydrolysis. The prepared DEN-OH for MRI contrast agent with the less concentration (10% Gd concentration of Gd-DTPA complex) showed quite clearer images of quite early stage cancer. Phospha sugar derivatives were prepared by new synthetic pathway to construct the compound library. Deoxybromophospha sugar derivatives such as TBMPP (Tribromophospha sugar derivative) prepared from phospholene derivative were first found to exert quite strong and wide spectral antitumor activities by in vitro evaluation against various kinds of leukemia cells such as K562, U937, etc. cell lines as well as solid cancer cells. Mechanistic studies with TBMPP against leukemia cells by Western blotting showed that the phospha sugar enhanced the expression of IER5, suppressed the expression of Cdc25B against tumour cells selectively and specifically, and then induced apoptosis at the mitosis step of the tumour cell cycle. Invivo evaluation for TBMPP was successfully performed by using a nude mouse transplanted by K562 cells on the skin.
Larisa Klapshina received her PhD from Razuvaev Institute of Organometallic Chemistry of Russian Academy of Sciences, IOMC RAS Nizhny Novgorod, Russia. Currently she is a senior researcher at IOOMC RAS and at the Laboratory of Optical Theranostics in Nizhny Novgorod State University. She and her group work in organic, organometallic synthesis and functional materials in bio-photonics and biomedicine. She is author of about 100 articles.
For a long time the idea of separated diagnostic and therapeutic approaches was predominant in the development of new drugs in medicine. However, recently a significant increase has been observed in the trend to create drugs which effectively combine diagnostic and therapeutic approaches. Such the drugs termed the agents of theranostics allow to determine the tumor localization in the body and to provide a therapeutic effect on it. Furthermore, in some cases theranostic agent allows to provide the real time monitoring of individual therapeutic response to the treatment procedure. Recently we reported on the preparation and studies of the photophysical properties of new fluorescent porphyrazine pigments which have been found to be an excellent platform for drugs with the unique combination of various biomedical functions: Bimodal (fluorescent/ MRI) diagnostic agents, sensitive optical sensors of intracellular viscosity and highly efficient photosensitizers in photodynamic therapy. Here we report the new series of aryl-cyano porphyrazine pigments containing n-donor oxygen atoms in the aromatic groups of peripheral frame of tetrapyrrol macrocycle. They demonstrate significantly improved photocytoxic properties and the potential for biomedical application as photosensitizers in PDT in comparison with previously reported aryl-cyano porphyrazine Pz1. Moreover, this series of tetrapyrrols the structural feature of which is the alternation of strongly electron withdrawing CN and Pi-donor aryl groups in the peripheral frame of macrocycle have been found to be novel fluorescent molecular rotor type dyes with the desirable feature of intense absorption and emission of red light that can be useful in vivo to enable deep tissue penetration in the tissue optical window. High efficacy of all the series as the fluorescent sensors of local viscosity in a wide viscosity range, had been demonstrated. Furthermore, we first proposed semi-empirical model describing photophysical behavior of novel porphyrazine series. The model was verified with fluorescence decay investigations for all the porphyrazine series, T.
Marine benthic invertebretes (Sponges and soft corals etc.) are widely distributed in the coral reefs of the world oceans. Of them, the animals belonging to the genus Sarcophyton (phylum Cnidaria, class Anthozoa, subclass Octocorallia, order Alcyonaceae, family Alcyoniidae) are very prolific and are the intense research subjects for marine natural product chemists. Literature checking revealed that Sarcophyton animals can produce different structural classes of secondary metabolites exhibiting various interesting biological activities ranging from antifouling, anti-inflammatory to cytotoxic activities. Among the metabolites reported, cembrane-type diterpenes are the most frequently encountered. Moreover, biscembranoids, characterized by the complex and highly oxygeneted macrocyclic frameworks, which are formally synthesized from two different cembranoid units via a probable [4+2] Diels-Alder cyclic addition, are unique and typical natural products from soft corals of the genera Sarcophyton. Due to the flexible nature of the macrocycles accompanying with the highly diverse substitution patterns, it has been being a challenging task for their structural, in particular, the absolute stereochemistry, determination by natural product chemists. In this presentation, I’ll present the latest chemical studies and promising bioactivity results on the sarcophyton corals and sponge spongia officinalis collected from South China Sea. All work has been performed in close collaboration with marine biologists and with pharmacologists.
Host-guest inclusion of two drugs, phenylephrine hydrochloride and synephrine with α and β-cyclodextrins and their applications in biological Sciences have been investigated by physicochemical and microbiological approach. Phenylephrine hydrochloride (PEH) is a selective α1-adrenergic receptor agonist of the phenethylamine class used primarily in cold and flu conditions as an antipyretic, analgesic drug to relief pain. Alkaloid synephrine (SNP) was first extracted as a natural product from the leaves of various citrus trees is used as bronchial muscle reluctant, increases blood pressure in the patients suffering from low blood pressure. Formation of Host Guest Inclusion complexes of PEH and SNP with the CDs have increased the activities of the drugs concerned and controlled the dose for regulatory dischargement i.e. the drugs can be released as per requirement of the patient to avoid the side effects which have been explored in this research paper.
Bahman Ebrahimi Saatloo was born in Urmia (Iran) in 1979. He received his B.Sc in Applied Chemistry (2007) from the Urmia University. He will receive his Ph.D. degree in Organic Chemistry from the Urmia University (Iran) in 2017 after completing his research in the Study of Synthesis of Polyazadodecahedrone and Synthesis of Spirooxindole Compounds of 1,2,3,4- Tetrahydroqunoline by Base, Acid and Nano Catalysts under the guidance of Professor Mohammad Mehdi baradarani. His current research interest focuses on the synthesis of Spirooxindole and supramolecular in heterocyclic for organic synthesis.
Green synthesis of spiropyrazolo-1,4-dihydropyridine has been reported via one-pot four-component reaction in EtOH/H2O (1:9) in the presence of p-TSA as a catalyst.
Spirooxindoles are classified as an important structural motif due to their distribution in diverse natural products, biologically and pharmaceutical activities such as the influenza virus [1], as inhibitors of the dengue virus and anti-cancer agents [2]. Therefore, we conducted a series of examination the chemistry of 5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolone-1,2-dione, in which the reactivity of the ketone carbonyl group of the 2-keto-amide unit was utilized. Thus, we were able to construct various spiro [3,3’-oxindoles] via three and four component combination [3]. Amongst, Spiropyrazole-1,4-dihydropyridine moieties have shown important biological and medicinal activities.
As a part of our ongoing interest in this context, we reported a simple and facile synthesis of a new type of spiropyrazolo-1,4-dihydropyridines (5) in the presence of p-TSA as a catalyst (scheme 1) from starting materials phenyl hydrazine hydrochloride derivatives (3), 3-aminobut-2-enenitrile (2), 3-oxo-3-phenyl propanenitrile (4) and 5,6-dihydro-1H-pyrrolo[3,2,1-ij]quinolone 1,2(4H)-dione (1) in environmentally friendly solvent, EtOH/H2O.
Shizuoka University, Japan
Sofia Konstantinidou is currently a PhD student at the Medical School, National and Kapodistrian Uninersity of Athens. She is a recipient of an Onassis Foundation Scholarship (G ZO 011-1/2018-2019) in Clinical Pharmacology-Oncology. She has participated in various conferences worldwide. She has published five articles in peer reviewed journals and one book chapter.
Biological products contain active substances coming from living cells and are usually large, complex proteins. They are used to treat many diseases such as cancer, rheumatoid arthritis, anaemia, renal failure and autoimmune diseases. However, due to their high cost, patient access is restricted, thus biosimilars came to the market. A biosimilar is defined by the United States Food and Drug Administration (FDA) as ‘biological product that is highly similar to and has no clinically meaningful differences from an existing FDA-approved reference product in terms of safety, purity and potency1’. They increase treatment options, decrease healthcare costs and improve patients’ access to very expensive therapies. Studies have proven that biosimilars offer significant cost savings to governments, which are greatly needed in the healthcare sectors. Only minor differences are acceptable between biologics and their respective biosimilars. Currently, there are few biosimilars approved for cancer treatment, but as the patents of many biologics are expiring, many more are coming to the market. These include rituximab, bevacizumab, trastuzumab, marketed for indications such as lymphomas, leukaemia, lung or breast cancer. Erythropoiesis-Stimulating agents (ESAs) are widely used for chemotherapy-induced anaemia2 and filgrastims for neutropenia respectively. Progression-free survival (PFS) and overall survival (OS) are usually used to measure the efficacy of biosimilars used in oncology3. The aim of this study is to provide a brief review of biosimilars, their perspectives in medical oncology and the current status of some clinical trials.
Miroslaw Kwiatkowski in 2004 obtained PhD degree at the AGH University of Science and Technology in Krakow (Poland). His published work includes more than 45 papers in reputable international journals and 80 conference proceedings. Miroslaw Kwiatkowski is the editor in chief of The International Journal of System Modeling and Simulation (United Arab Emirates), an associate editor of Micro & Nano Letters Journal (United Kingdom) and a member of the many editorial board of internationals journals.
Adsorption processes are among the widespread applications of Metal-Organic Frameworks (MOFs), which found employment in removal of harmful substances such as heavy metals from liquid and gaseous streams, storage and sequestration of gases such as carbon dioxide, methane and hydrogen as well as in separation and purification of gases products, catalytic processes and others. The performance and applicability of MOFs in mentioned processes among others depend on the high specific surface area and adsorption capacity. In this work adsorption properties of CO2 and CH4 on Basosiv M050 sample were determined by a volumetric method. The adsorbed volume values with respect to relative pressure were obtained for all of the gases. The nitrogen adsorption isotherms were studied at 77 K, and CO2 and CH4 isotherms were studied at 273 K. The BET and Langmuir surface areas of the samples were determined using N2 adsorption isotherms. Adsorption capacities for CO2 and CH4 are also calculated from their isotherm analysis. Additionally, the new numerical method with the unique fast multivariant identification procedure was employed for the analysis of the adsorption process on a specific type of a MOF sample. The proposed tools permit the gathering of a broader spectrum of information on the analysed structure of MOFs materials and the adsorption processes taking place on their surface as compared with the others methods. Additionally the proposed method with unique numerical procedure can be a good starting point for the development of more advanced tools.
Ilyes Safir has completed his PhD at the age of 33 years from Geneva University. Ilyes Safir is having international experience of performing research in materials science, nanosurface, nanotechnology, analytical chemistry. Skilled in preparing accurate nano-layers of thin polymer films, analysis with Atomic Force Microscope (AFM). Performed novel bio-nanostructured micelles/vesicles for drug delivery system.
Combination of straight biochemical and organic routes to graft nucleotide sequences to a chitosan backbone. The resulting chitosan-g-ssDNA hybrid self-assembles into submicrometer size structures in dilute aqueous solution as assessed by atomic force and electron microscopy imaging. The hypothesis of self-assembly driven by chemical incompatibility between the amphiphilic chitosan and nucleic acid grafts is supported further by stability of the self-assembly against ionic strength and pH variations.
Ahmed Abdelrahman Daoud has completed his PhD in Medical parasitology at the faculty of medicine Tanta University 1980 and another PhD in Microbiology and Immunology in 1992 at Cairo Military Medical Academy.
Kafa Khalaf Hammud has completed her BSC, MSC, and PhD from Department of Chemistry, College of Science, Baghdad University, Iraq. She works at Directorate of Materials Research, Ministry of Science & Technology. She has published several scientific articles and has been serving as an editorial board member. Her main concern related to chemistry subjects such as synthesis, characterization and application.
This paper gave a mini review about pharmaceutical chemistry that started from lab experiments and end at publication stage but not at industry stage. There are many scientific paper that deal with new organic or organometallic compounds with good biological activities. These compounds are differing in their structures and methods of preparation beside the prior biological activities. The biological applications are mostly limited as antibacterial or antifungal agents at agar plates and may be solely increased to mice tests. These preparation and biological steps were dependant on the presence of functional groups or heteroatoms. So, Iraqi researchers as students or supervisors synthesized and characterized a large number of derivatives with no happy ending as a drug or treatment. This problem is present in medicinal herbs plant in Iraq. Many research papers about herbal extracts end at bacterial or fungal tests and may moved another step with cancer cell line then nothing more. In Iraq, there are the state company for drugs industry in Samarra (SDI) and other state in Nineveh (NDI). Both states are authorized for production of specific drugs such as antibiotics but not for new synthesized compounds might be a promising therapy. The Iraqi private drugs companies are limited in their choices and do not support such issue. For this case, I do think that solutions for this issue are related to main drug and disease relationship. In another words, we want a drug to treat a disease and industry need scientific documentations describes all pharmaceutical requirements and solution begins by supporting known companies searching of truth in facilitated labs.
Bahman Ebrahimi Saatloo was born in Urmia (Iran) in 1979. He received his B.Sc in Applied Chemistry (2007) from the Urmia University. He will receive his Ph.D degree in Organic Chemistry from the Urmia University (Iran) in 2017 after completing his research in the Study of Synthesis of Polyazadodecahedrone and Synthesis of Spirooxindole Compounds of 1,2,3,4- Tetrahydroqunoline by Base, Acid and Nano Catalysts under the guidance of Professor Mohammad Mehdi baradarani. His current research interest focuses on the synthesis of Spirooxindole and supramolecular in heterocyclic for organic synthesis.
Green synthesis of spiropyrazolo-1,4-dihydropyridine has been reported via one-pot four-component reaction in EtOH/H2O (1:9) in the presence of p-TSA as a catalyst. Spirooxindoles are classified as an important structural motif due to their distribution in diverse natural products, biologically and pharmaceutical activities such as the influenza virus, as inhibitors of the dengue virus and anti-cancer agents. Therefore, we conducted a series of examination the chemistry of 5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolone-1,2-dione, in which the reactivity of the ketone carbonyl group of the 2-keto-amide unit was utilized. Thus, we were able to construct various spiro [3,3’-oxindoles] via three and four component combination. Amongst, Spiropyrazole-1,4-dihydropyridine moieties have shown important biological and medicinal activities. As a part of our ongoing interest in this context, we reported a simple and facile synthesis of a new type of spiropyrazolo-1,4-dihydropyridines (5) in the presence of p-TSA as a catalyst from starting materials phenyl hydrazine hydrochloride derivatives (3), 3-aminobut-2-enenitrile (2), 3-oxo-3-phenyl propanenitrile (4) and 5,6-dihydro-1H-pyrrolo[3,2,1-ij]quinolone 1,2(4H)-dione (1) in environmentally friendly solvent, EtOH/H2O.
University of Michigan, USA