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Mini Reviews in Medicinal Chemistry

Xun Zhang, Rutao Liu
Bisphenol A (BPA) is an environmental endocrine disruptor widely spreading in life. Its characteristics, including small does, long incubation period, and frequent contact, make it easy to enter human body through drinking water, food, air and other pathways, leading to tumors, infertility, and liver damage. The present review summarizes the underlying mechanism of oxidative stress and its related effects induced by BPA in liver. The progress of research into the mechanism of oxidative stress induced by BPA is summarized, including mitochondrial dysfunction, lipid peroxidation and inflammation reaction, liver dyslipidemia, apoptosis, cell death mechanism...
September 11, 2018: Mini Reviews in Medicinal Chemistry
Nehad E Abo-Elmagd, Riham F George, Manal A Ezzat, Reem K Arafab
A series of thirty-one new 1-phthalazinones was designed and synthesized based on the well-known VEGFR inhibitor vatalanib. The obtained phthalazinones were screened for their cytotoxic activity against DLD-1 and LoVo (colon) and Panc-1, Paca-2 (pancreas) cancer cell lines using MTT assay. The tested compounds revealed exceptionally promising cytotoxic activity against LoVo cell lines with IC50 ranges 0.18-780 nM. Finally, these compounds were also found to be dual inhibitors of VEGFR-2 and EGFR in the in vitro enzyme assay with higher potency against the former (IC50 = 0...
September 3, 2018: Mini Reviews in Medicinal Chemistry
Sumit Tahlan, Balasubramanian Narasimhan, Siong Meng Lim, Kalavathy Ramasamy, Vasudevan Mani, Syed Adnan Ali Shah
Various analogues of benzimidazole are found to be biologically and therapeutically potent against several ailments. Benzimidazole when attached with heterocyclic rings has shown wide range of potential activities. So, from the above provided facts, we altered benzimidazole derivatives so that more potent antagonists could be developed. In the search for a new category of antimicrobial and anticancer agents, novel azomethine of 2-mercaptobenzimidazole derived from 3-(2-(1H-benzo[d]imidazol-2-ylthio)acetamido)benzohydrazide were synthesized...
September 3, 2018: Mini Reviews in Medicinal Chemistry
Julia Krajewska, Adrian Bartoszek, Jakub Fichna
Colorectal cancer (CRC) is one of the most common cancers in both men and women. Approximately one third of patients does not survive five years from diagnosis, which indicates the need for treatment improvement, also through new ways of drug delivery. A possible strategy to increase treatment efficacy is the use of liposomal formulation, which allows to deliver both hydrophobic and hydrophilic compounds with better biocompatibility and reduced side-effects. Liposomal formulations showed better antitumor activity, longer drug accumulation and no cytotoxic effect on normal cells when compared to free drugs...
September 3, 2018: Mini Reviews in Medicinal Chemistry
Sergey S Chuprun, Grigory Kantin, Mikhail Krasavin
The review provides a summary of synthetic approaches to and medicinal applications of N-aryl-C-nitroazoles. This broad chemical family delivered numerous practical applications in the areas other than pharmaceuticals. This is most likely due to a common stigma associated with nitroheterocycles implying their inherent toxicity. Therefore, the research literature appears to be lacking in medicinal chemistry reports related to this class of compounds. However, despite this notion, the nitroheterocycles have enjoyed a marked renaissance in the last years, particularly, in antimicrobial area...
August 30, 2018: Mini Reviews in Medicinal Chemistry
Aurelio Ortiz, Estibaliz Sansinenea
Microorganisms are able to produce hundreds of unique chemical structures that can be effectively used by the human beings on their own benefit using the products in chemical industry. Bacteria belonging to Bacillus genera are very good chemical factories capable to synthetized different compounds with a wide variety of activities. In this review we try to review the compounds with their respective biological activities produced by different species of Bacillus.
August 28, 2018: Mini Reviews in Medicinal Chemistry
Ibrahim F Nassar, Wael A El-Sayed, Tamer I M Ragab, Al Shimaa Gamal Shalaby, Ahmed B M Mehany
New aryl substituted cyclohepta[b]pyridine and cyclohepta[d]pyrimidine derivatives were synthesized. The sugar hydrazones of the synthesized pyridine and pyrimidine compounds were also prepared. In addition, the 1,3,4-oxadiazolyl acyclic C-nucleoside analogues of the pyridine system were prepared. The haemolytic, Prebiotic, anticancer and antimicrobial activities of some of the synthesized compounds were also studied. Compounds 10 and 12 showed high activity against MCF-7, HEPG-2 and HCT-116 cell lines with IC50 ranged from 3...
August 20, 2018: Mini Reviews in Medicinal Chemistry
Swarna Gowri, Santosh L Gaonkar
Thiazole is the versatile heterocyclic compound in heterocyclic chemistry and in drug design. Presence of several reaction sites in the thiazole moiety extends their range of applications and leads to new solutions for challenges in synthetic and medicinal chemistry. Thiazole derivatives are widely used as bioactive agents, liquid crystals, sensors, catalysts, etc. The motivating molecular architecture of 1,3-thiazoles make them suitable moieties for drug development. In this review, our aim is to corroborate the recent data available on various synthetic strategies and biological properties of 1,3-thiazole derivatives...
August 15, 2018: Mini Reviews in Medicinal Chemistry
Canan Kus, Ezgi Ozer, Yesim Korkmaz, Erkan Yurtcu, Rukiye Dagalp
In this ongoing research, it is aimed to investigate the synthesis, structure identification and effects on urokinase-type plasminogen activators (uPA) and its receptor levels of 4-(3H-imidazo[4,5-b]pyridin-2-yl)-N-substituted benzamide and benzamidine derivatives. uPA levels obtained from 4b and 7d administration were similar to 5FU (5-fluorouracil) for colorectal carcinoma cells (p < 0.05). 4b and 7d significantly reduced uPAR (urokinase-type plasminogen activator receptor) levels on both cell lines (p < 0...
August 15, 2018: Mini Reviews in Medicinal Chemistry
Stephanie S Schweiker, Amanda L Tauber, Madeleine E Sherry, Stephan M Levonis
Poly(ADP-ribose)polymerase, member 14 (PARP14) alternatively named ARTD8, BAL2, and COAST6 is an intracellular mono(ADP-ribosyl) transferase. PARP14 transfers a negatively charged ADP-ribose unit from a donor NAD+ molecule onto a target protein, post-translationally. PARP14s domain architecture consists of three macrodomains (Macro1, Macro2 and Macro3), a WWE domain and an ARTD (or catalytic domain). The Macro2 and Macro3 domains bind ADP-ribose (ADPr) with high affinity, whereas the WWE domain stabilizes the protein structure by binding to ADPr derivatives...
August 15, 2018: Mini Reviews in Medicinal Chemistry
Sounak Bagchi, Venkatesan Jayaprakash, Parth Rathee, Sugato Banerjee
Farnesyl Transferase is a hetero-dimer transferase that targets ras proteins and attaches a farnesyl group to it. This ras protein, on localization to the cell membrane has the ability to induce activation of various growth and proliferation pathways of the cell. Over-activation of mutated ras protein may lead to development of cancer. Farnesyl transferase catalyzes the initial step in the post-translational modification of normal as well as mutated ras thus facilitating its tethering to the cell membrane. Inhibition of farnseyl transferase is the main step in restricting the activity of mutant ras protein...
July 31, 2018: Mini Reviews in Medicinal Chemistry
Nagaraju Marepu, Mahes Gosi, Snathoshi Sumana Vedula, Sunandamma Yeturu, Manojit Pal
The 6-substituted indolo[2,3-b]quinolines have been synthesized and explored as potential cytotoxic agents. Ultrasound assisted synthesis of these compounds was carried out by using a method involving two sequential C-N bond forming reactions between 3-(2-bromophenyl)-2-chloroquinoline and amines in a single pot in the presence of Pd(OAc)2 and a ligand (S)-BINAP. The synthesized compounds showed promising growth inhibition when tested against breast adenocarcinoma (MCF7) cancer cell lines and the best compound induced apoptosis in MCF-7 cells...
July 27, 2018: Mini Reviews in Medicinal Chemistry
Yulu Ma, Xi Zheng, Ping Zhu, Bei Liu, Hui Gao, Zewei Mao, Lijun Zhang, Chunping Wan
Resveratrol and chalcones are lead compounds with good biological activities. In this study, a series of novel derivatives (6-38) between resveratrol and chalcone possessing piperazine moiety have been synthesized, and in vitro anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and anti-proliferative effect on a panel of human tumor cell lines (Hela, A549 and SGC7901) by MTT assay were evaluated. The results demonstrated that the substituents of the NH group of piperazine ring had an obvious influence on biological activities...
July 27, 2018: Mini Reviews in Medicinal Chemistry
Oleg A Raevsky, Veniamin Y Grigorev, Daniel E Polianczyk, Olga E Raevskaja, John C Dearden
Detailed critical analysis of publications devoted to QSPR of aqueous solubility is presented in the review with discussion of four types of aqueous solubility (three different thermodynamic solubilities with unknown solute structure, intrinsic solubility, solubility in physiological media at pH=7.4 and kinetic solubility), variety of molecular descriptors (from topological to quantum chemical), traditional statistical and machine learning methods as well as original QSPR models.
July 27, 2018: Mini Reviews in Medicinal Chemistry
Tehreem Tahir, Muhammad Ashfaq, Humna Asghar, Mirza Imran Shahzad, Rukhsana Tabassum, Areeba Ashfaq
In this review, specific therapeutic and medicinal advantages including antiviral, antibacterial, antifungal and antitumor, strategies for drug designing, structure-activity relationship, advances in the syntheses of azo and hippuric acid derivatives of more than 50 compounds have been discussed since 2009-2018. It is found that phenyl-diazenyl azo derivatives and pyridinyl substituted hippuric acid derivatives showed promising antiretroviral potential. The incorporation of azo functionality to the respective quinolones and coumarin moieties and the insertion of thiocarbazone to hippuric acid displayed immense antibacterial activities...
July 27, 2018: Mini Reviews in Medicinal Chemistry
Dengquan Su, Lijian Ding, Shan He
Marine-derived fungi Trichoderma genus are serving as a valuable resource for structurally novel natural products encompassing a variety of chemical substances and diverse pharmacological applications. So far, about 78 metabolites had been structurally documented from the species of marine Trichoderma genus and a large proportion of these metabolites exhibited therapeutic properties with potential application in drug discovery. This mini review focuses on the structures and bioactivities of these secondary metabolites from marine-derived Trichoderma species...
July 27, 2018: Mini Reviews in Medicinal Chemistry
Zeinab A Muhammad, Mohamed A A Radwan, Thoraya A Farghaly, Hatem M Gaber, Mahmuod M Elaasser
BACKGROUND: Several biologically active indole alkaloids have been isolated from marine organisms over the previous few years. Many scientsts interested in synthesis of the marine azepino-indole alkaloids due to their wide range of bioliogical activies. OBJECTIVE: We interested herein to synthesize a new series of some analogues of new naturally occurring azepinoindole alkaloids. METHOD: A novel series of [1,2,4,5]tetrazepino[6,7-b]indoles, Marine natural product Hyrtioreticuline C and D analogues, were synthesized via the reaction of 3-hydrazonoindolin-2-one with hydrzaonoyl chlorides in basic medium...
July 23, 2018: Mini Reviews in Medicinal Chemistry
Mubarak H Shaikh, Dnyaneshwar D Subhedar, Laxman Nawale, Dhiman Sarkar, Firoz A Kalam Khan, Jaiprakash Sangshetti, Bapurao B Shingate
Novel 1,2,3-triazole based benzylidenehydrazide derivatives were synthesized and evaluated for antitubercular activity against Mycobacterium tuberculosis (MTB) H37Ra, M. bovis BCG and cytotoxic activity. Most of the derivatives exhibited promising in vitro potency against MTB characterized by lower MIC values. Among all the synthesized derivatives, compound 6a and 6j were the most active against active and dormant MTB H37Ra, respectively. Compound 6d was significantly active against dormant and active M. bovis BCG...
July 18, 2018: Mini Reviews in Medicinal Chemistry
Lianghan Zhu, Zhiying Cui, Qihua Zhu, Xiaoming Zha, Yungen Xu
Opioid analgesics, such as morphine, are wildly employed in the treatment of moderate to severe pain. However, they are notorious for abuse liability and respiratory depression. Therefore circumventing the side effects, such as euphoria, addiction, respiratory depression and gastrointestinal adverse reactions, is of extensive importance. Recently, a large number of research results have revealed that such morphine-like side effects are not inevitable, and they focus on the novel approaches to disconnecting the analgesics from adverse effects...
July 16, 2018: Mini Reviews in Medicinal Chemistry
Abbas Ahmadi, Mehrdad Roghani, Sanaz Noori, Babak Nahri-Niknafs, Hengameh Bakhtiar
BACKGROUND: Currently, there is no conclusive cure for Alzheimer's disease (AD) and existing treatments mainly offer symptomatic relief. Dysfunction of the cholinergic system plays an important role in pathogenesis of AD. Tacrine (1, 2, 3, 4-tetrahydroacridin-9-amine, I) was the first approved agent for the palliative therapy of AD but its use is associated with some complications. Development of novel multi target derivatives of Tacrine with lower complications is strongly warranted...
July 16, 2018: Mini Reviews in Medicinal Chemistry
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