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Medicinal Chemistry

Mateusz D Tomczyk, Anna Byczek Wyrostek, Klaudia Strama, Martyna Wawszków, Przemysław Kasprzycki, Krzysztof Z Walczak
1,8-Naphthalimides (benzo[de]isoquinoline-1,3-diones) modified in various positions of chromophore, provided an effective method for enhancing their anticancer activity and reducing undesirable toxic effects. To accomplish this goal, several new 6- and 6,7-substitued 1,8-naphthalimides containing a ω-hydroxylalkylamine side-chains of different length were obtained and evaluated in the report presented. Upon examination, it appeared that the replacement of the nitro groups in the chromophore slightly reduce its anticancer activities, whereas the presence of both nitro groups and ω-hydroxylalkylamine chain resulted in seriously increased anticancer activities...
September 11, 2018: Medicinal Chemistry
Momin Khan, Sehrish Khan, Amir Ul Mulk, Anis Ur Rahman, Abdul Wadood, Sulaiman Shams, Muhammad Ashraf, Jameel Rahman, Abdul Hameed, Zahid Hussain, Abbas Khan, Khair Zaman, Khalid Mohammed Khan, Shahnaz Perveen
BACKGROUND Barbituric acid derivatives are a versatile group of compounds which are identified as potential pharmacophores for the treatment of anxiety, epilepsy and other psychiatric disorders. They are also used as anesthetics and have sound effects on the motor and sensory functions. Barbiturates are malonylurea derivatives with a variety of substituents at C-5 position showing resemblance with nitrogen and sulfur containing compounds like thiouracil which exhibited potent anticancer and antiviral activities...
September 11, 2018: Medicinal Chemistry
Dina H Dawood, Eman M H Abbas, Thoraya A Farghaly, Mamdouh M Ali, Mohammed F Ibrahim
BACKGROUND: Pyrimidines emerged as a remarkable class of heterocyclic compounds that have reinforced the pharmaceutical chemistry with various bioactive antitumor agents. Moreover, pyrimidine scaffold displayed VEGFR-2 inhibitory activity. Also, nano-sized catalysts are used in organic reactions in order to speed up the catalytic process. OBJECTIVE: we interested herein to synthesize a new series of fused pyrimidines using ZnO(NPs) to investigate their antitumor efficiency against breast MCF7 cancer and their VEGFR-2 inhibition properties ...
September 11, 2018: Medicinal Chemistry
Dima A Sabbah, Ameerah Hasan Ibrahim, Wamidh H Talib, Khalid M Alqaisi, Kamal Sweidan, Sanaa K Bardaweel, Ghassan Abu Sheikha, Haizhen A Zhong, Eveen Al-Shalabi, Reema Abu Khalaf, Mohammad S Mubarak
BACKGROUND: Phosphoinositide 3-kinase α (PI3Kα) has emerged as a promising target for anticancer drug design. OBJECTIVES: Target compounds were designed to investigate the effect of the p-OCH3 motifs on ligand/PI3Kα complex interaction and antiproliferative activity. METHODS: Synthesis of the proposed compounds, biological examination tests against human colon adenocarcinoma (HCT-116), breast adenocarcinoma (MCF-7), and breast carcinoma (T47D) cell lines, along with Glide docking studies...
September 11, 2018: Medicinal Chemistry
Saleem Farooq, Javid A Banday, Aashiq Hussain, Momina Nazir, Mushtaq A Qurishi, Abid Hamid, S Koul
Natural product, osthol has been found to have important biological and pharmacological roles. The unmet needs in cancer therapeutics makes its derivatization an important and exciting field of research. Keeping this in view, a whole new series of diverse analogues of osthol (1) were prepared through modification in the lactone ring as well as in the side chain of the osthol molecule. All the newly synthesized compounds were subjected to anti-proliferative screening through 3-(4,5-Dimethylthiazol-yl)-diphenyl tetrazoliumbromide (MTT) against four different human cancers of diverse origins viz...
September 11, 2018: Medicinal Chemistry
Uzma Salar, Khalid Mohammed Khan, Sridevi Chigurupati, Shazia Syed, Shantini Vijayabalan, Abdul Wadood, Muhammad Riaz, Mehreen Ghufran, Shahnaz Perveen
BACKGROUND: Despite of many side effects associated, there are many drugs which are being clinically used for the treatment of type-II diabetes mellitus (DM). In this scenario, there is still need to develop new therapeutic agents with more efficacy and less side effects. By keeping in mind the diverse spectrum of biological potential associated with coumarin and thiazole, a hybrid class based on these two heterocycles was synthesized. METHOD: Hydrazinyl thiazole substituted coumarins 4-20 were synthesized via two step reaction...
September 3, 2018: Medicinal Chemistry
Maria Luisa Teixeira, Silvana Marcussi, Danubia Aparecida de Carvalho Selvati Rezende, Maisa Lamounier Magalhaes, David Lee Nelson, Maria das Gracas Cardoso
BACKGROUND: The search for natural inhibitors of snake venom toxins is essential to supplement or even replace the serum therapy. The aim of this work was to evaluate the pharmacological properties of essential oil from Lippia origanoides Kunth. (Verbenaceae). METHODS: The oil was extracted by hydrodistillation and the constituents were identified and quantified by GC-MS and GC-FID. The essential oil from L. origanoides was evaluated in hemolysis tests, on the activities of phospholipases A2 and serine proteases and in coagulation and thrombolysis induced by different snake venoms...
August 29, 2018: Medicinal Chemistry
Talea Sana, Bina S Siddiqui, Saleem Shahzad, Ahsana D Farooq, Faheema Siddiqui, Samia Sattar, Sabira Begum
BACKGROUND: Endophytic fungi are receiving attention as sources of structurally novel bioactive secondary metabolites towards drug discovery from natural products. This study reports the isolation and characterization of secondary metabolites from an endophytic fungus Aspergillus nidulans, associated with Nyctanthes arbor-tristis Linn., a plant which has a traditional use to cure many ailments including cancer. OBJECTIVE: Objective of this study was to evaluate the antiproliferative activity of the metabolites of A...
August 28, 2018: Medicinal Chemistry
Biao Xiong, Shi Chen, Peng Zhu, Meili Huang, Weijie Gao, Rui Zhu, Jianqiang Qian, Yanfu Peng, Yanan Zhang, Hong Dai, Yong Ling
BACKGROUND: A large number of pyrazole derivatives have different biological activities such as anticancer, antimicrobial, anti-inflammatory, analgesic and antiepileptic activity. Among them, pyrazole oximes have attracted much attention due to their potential pharmacological activities, particularly anticancer activities. OBJECTIVE: Our goal is to synthesize novel thiazolyl substituted bis-pyrazole oxime derivatives with potent antitumor activities by selectively inducing apoptosis and reactive oxygen species (ROS) accumulation in cancer cells...
August 26, 2018: Medicinal Chemistry
Dolores Santa Maria, Rosa M Claramunt, Jose Elguero, Miguel Carda, Eva Falomir, Celia Martin-Beltran
BACKGROUND: A set of 2,5-diaryl-1,2,4-triazol-3-ones was synthesized in two steps and evaluated as regards their activity in some relevant biological targets related with cancer. OBJECTIVE: This study is focused to the synthesis and the biological evaluation of 2,5-diaryl-1,2,4-triazol-3-ones. In this sense, the effect of the synthetic triazolones on the proliferation of HT-29 and A549 cancer cells and on HEK non-cancer cells has been measured. In addition, the effect of triazolones on the expression of hTERT, c-Myc and PD-L1 genes and on the production of c-Myc and PD-L1 proteins have also been evaluated...
August 20, 2018: Medicinal Chemistry
Xinyu Liu, Shengjie Dong, Yuru Ma, Hu Xu, Hongxia Zhao, Qingzhi Gao
BACKGROUND: There is an urgent need to develop novel inhibitors against clinically widespread extended-spectrum β-lactamases (ESBLs) to meet the challenges of the ever-evolving threat of antibiotic resistances. Most existing ESBL inhibitors sharing a common chemical feature of β-lactam ring in their molecule, this structural characteristic makes them intrinsically susceptible to enzymatic breakdown by the resistance mechanisms employed by the bacteria. OBJECTIVE: The aim of this study was to screen and discover novel lead compounds by using L-proline as initial scaffold to create a "non-sulfur, non-β-lactam" new chemotypes for potential ESBL inhibitors...
August 16, 2018: Medicinal Chemistry
Arshia, Almas Jabeen, Aisha Faheem, Khalid Mohammed Khan, Shazia Shah, Shahnaz Perveen
BACKGROUND: Inflammation is a biological rejoinder of vascular tissues against destructive agents e.g. irritants, damaged cell or pathogens. During inflammation respiratory burst occur by activated phagocytes helps to destroy invading pathogens. Phagocytic cells such as neutrophils and macrophages are one of the major sources of reactive oxygen species (ROS) and nitric oxide (NO). Normally the redox environment is maintained by various antioxidant defense systems, however, these reactive oxygen species may be destructive and can lead to various pathological conditions...
August 5, 2018: Medicinal Chemistry
Felipe R S Santos, Jessica T Andrade, Carla D F Sousa, Joice S Fernandes, Lucas F Carmo, Marcelo G F Araujo, Jaqueline M S Ferreira, Jose A F P Villar
BACKGROUND: Microbial infections is a global public health problem. The aim of this work was to synthesize and evaluate the antimicrobial activity of novel triazoles, morpholines and thiosemicarbazones. METHODS: Compounds were synthesized using 2,4-Dihydroxyacetophenone and 4-hydroxybenzaldehyde as starting materials. The antimicrobial activity of these compounds against bacteria and yeast was evaluated by the broth microdilution method. RESULTS: The proposed route for synthesis gave high to moderate yields, moreover these compounds were successfully characterized by ¹H NMR, ¹³C NMR and LC-MS...
July 29, 2018: Medicinal Chemistry
Cigdem Karaaslan, Yalcin Duydu, Aylin Ustundag, Can Ozgur Yalcin, Banu Kaskatepe, Hakan Goker
A series of new 2-(3,4-dimethoxyphenyl)-1H-benz(or pyrido)imidazoles 2, 4-25 were synthesized and evaluated for their anticancer and antimicrobial activities. The NMR assignments of the dimethoxy groups were established by the NOESY spectra. Compound 12 bearing two chlorine atoms at the 5(4) and 7(6) positions of the benzene moiety of benzimidazole was found the most potent analogue, against A549 cells with the GI50 value of 1.5 µg/mL. Moreover, compound 24 showed remarkable cell growth inhibition against MCF-7 and HeLa cells with the GI50 values of 7 and 5...
July 11, 2018: Medicinal Chemistry
Katharigatta N Venugopala, Sandeep Chandrashekharappa, Melendhran Pillay, Subhrajyoti Bhandary, Mahmoud Kandeel, Fawzi M Mahomoodally, Mohamed A Morsy, Deepak Chopra, Bandar E Aldhubiab, Mahesh Attimarad, Osama I Alwassil, Sree Harsha, Koleka Mlisana
BACKGROUND: Benzothiazole derivatives are known for anti-TB properties. Based on the known antiTB benzothiazole pharmacophore, in the present study, we described the synthesis, structural elucidation, and anti-tubercular screening of a series of novel benzothiazole (BNTZ) derivatives (BNTZ 1-7 and BNTZ 8-13). OBJECTIVE: Development of benzothiazole based anti-TB compounds. METHODS: Title compounds are synthesized by microwave method and purified by column chromatography...
July 3, 2018: Medicinal Chemistry
Gopiraja Geethaavacini, Go Poh Poh, Lim Yi Yan, Rajindran Deepashini, Sivadasan Shalini, Rajak Harish, Krishnan Sureshkumar, Veerasamy Ravichandran
BACKGROUND: The development of severe drug resistance caused by the extensive use of anti-HIV agents have resulted in greatly extensive reduction in these drugs efficacy. OBJECTIVES: To identify the important pharmacophoric features and correlate 3Dchemical structure of benzothiazinimines with their anti-HIV potential using 2D, 3D-QSAR and pharmacophore modeling studies. METHODS: QSAR and pharmacophore mapping studies have been used to relate structural features...
May 28, 2018: Medicinal Chemistry
Do Thi Mai Dung, Nguyen Van Huan, Do Manh Cam, Dao Cam Hieu, Pham-The Hai, Le-Thi-Thu Huong, Jisung Kim, Jeong Eun Choi, Jong Soon Kang, Sang-Bae Han, Nguyen-Hai Nam
BACKGROUND: Histone deacetylases (HDAC) enzymes are emerging as potential targets for cancer treatments. In this study several series of novel hydroxamic acids incorporating 1-((1H-1,2,3-triazol-4-yl)methyl)-3-substituted-2-oxoindolines was explored. METHODS: The compounds were designed using Autodock Vina program, then synthesized and evaluated in vitro and in silico for their inhibitory activity against HDACs. The cytotoxicity was measured by SRB method. The enzyme inhibitory effects of the compounds were evaluated by fluorescent assay...
May 27, 2018: Medicinal Chemistry
Zahra Heydari, Maryam Mohammadi-Khanaposhtani, Somaye Imanparast, Mohammad Ali Faramarzi, Mohammad Mahdavi, Parviz Rashidi Ranjbar, Bagher Larijani
BACKGROUND: Pyrano[3,2-c]quinoline derivatives 6a-n were synthesized via simple two-step reactions and evaluated for their in vitro α-glucosidase inhibitory activity. METHODS: Pyrano[3,2-c]quinoline derivatives 6a-n derivatives were prepared from a two-step reaction: cycloaddition reaction between 1-naphthyl amine 1 and malonic acid 2 to obtain benzo[h]quinoline-2(1H)-one 3 and reaction of 3 with aryl aldehydes 4 and Meldrum's acid 5. The anti- α-glucosidase activity and kinetic study of the synthesized compounds were evaluated using α-glucosidase from Saccharomyces cerevisiae and p-nitrophenyl-a-D-glucopyranoside as substrate...
May 27, 2018: Medicinal Chemistry
Fady N Akladios, Scott D Andrew, Samantha J Boog, Carmen de Kock, Richard K Haynes, Christopher J Parkinson
Bis-thiosemicarbazones containing a central pyridyl core display potent antimalarial activity in vitro. The absence of the pyridyl core results in inactive compounds. It is likely that metal ion sequestration and subsequent reactive oxygen generation plays a role in the antimalarial activity of the series, the redox activity of the iron complexes of bis-thiosemicarbazones paralleling antimalarial activity. The activity of this series compares favourably to that of previously reported iron sequestering compounds...
May 25, 2018: Medicinal Chemistry
Shabnam Farzaneh, Soraya Shahhosseini, Hadi Arefi, Bahram Daraei, Marjan Esfahanizadeh, Afshin Zarghi
BACKGROUND: Prostaglandins are a family of eicosanoids biosynthesized from arachidonic acid through cyclooxygenase (COX) pathway. Two isoforms of COX are well established: COX-1, COX-2. Evidence supports the notion that cyclooxygenase-2, plays a crucial role in some pathological conditions such as inflammation and cancer. OBJECTIVE: A new group of 1,3-diphenyl-3-(phenylamino)propan-1-ones was designed and synthesized to investigate for their COX-2 inhibitory activity and inhibition of platelet aggregation...
May 25, 2018: Medicinal Chemistry
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