Letters in Drug Design & Discovery - Volume 15, Issue 2, 2018

Background: In this study, we reported the in vitro cytotoxicity activities of a series of N-(2-(arylmethylimino)ethyl)-7-chloroquinolin-4-amine derivatives against four human cancer cell lines. Methods: Good activities were obtained for compounds having aryl groups = 2-hydroxyphenyl, pyridinyl, 5-nitrofuran-2-yl and 5-nitrothiophen-2-yl. Results and Conclusion: The results indicate that this group of compounds is a good Read More

Background: Antioxidants are proficient of stabilizing agents in the target cells and biological systems. The homeostatic equilibrium between the reactive oxygen species and endogenous antioxidants is important in maintaining healthy tissues. As some antioxidant agent's show improved resistance, it is necessary to design the new heterocyclic molecules to form potent antioxidant agents with promising pharmacological a Read More

Background: Diabetes Mellitus (DM) is a complex metabolic disease illustrated by abnormally high levels of plasma glucose or hyperglycaemia. Accordingly, several α-glucosidase inhibitors have been developed for the treatment of diabetes and other degenerative disorders. While, a coumarin ring has the privilege to represent numerous natural and synthetic compounds with a wide spectrum of biological activities e.g Read More

Background: Calmodulin (CaM) is a ubiquitous, calcium-binding protein that can bind to and regulate a multitude of different protein targets, thereby affecting many different cellular functions. Binding ofsmall, hydrophobic molecules alter its function, as in the case of Phenothiazine (PTZ). PTZ isan organic compound with a history of use as an antihelminth and frequently quoted as a classic example of a pharmaceutical lea Read More

Background: Aroylindole derivatives, the structural analogs of Combretastatin A-4 has been found to possess potent growth inhibitory activity on several cancer cell lines due to its excellent antitumor and antivascular activities. The aim of present research work is to identify lead and establish structure activity correlation of trimethoxyaroylindole derivatives, using integrated ligand and structure based computational approache Read More

Background: Due to multi-drug, extended-drug, and pandrug resistance phenotypes, bacterial resistance to antibiotics and fungal infections are a general health issue. Particulary, increase of fungal infections due to secondary cause of human diseases have been observed. An extensive variety of benzimidazole derivatives have been characterized for their chemotherapeutic significance. Benzimidazole derivatives have received Read More

Background: We report the design, synthesis and evaluation of a series of 4-biaryl substituted 2-amino benzo[h]chromene derivatives as potential cytotoxic agents. Methods: The one-pot synthesis of this class of compounds was carried out under ultrasound irradiation using an MCR involving Pd/C-catalyzed Suzuki-Miyaura coupling as a key step. Result and Conclusion: Several of these compounds showed promising cytotoxiciti Read More

Background: The Janus enzyme family is regulated by various cytokines together with interleukins, interferons, and hormones like glycoprotein, thromboprotein, and hormone. Metamorphosis and translocations in the Janus Kinase genes leading to constitutively active Janus Kinase proteins are associated with a variety of hematopoietic malignancies, comprising the myeloproliferative disorders, acute lymphoblastic leukemia, Read More

Background: In the present study, new triazine derivatives 3, 4, 5, 6, 8 and 10 were synthesized starting from readily available cyanuric chloride 1 via nucleophilic displacement with morpholine followed by Suzuki or Stille coupling reactions and then the thermal displacement of chlorine atom with diverse substituted amines. Methods: All synthesized compounds were screened for their cytotoxic activity against HT-29, MDA-MB- Read More

Background: In medicinal chemistry, thiazoles have gained great importance in antifungal and anticancer drug design and development. Objectives: The aim of this study was to synthesize new quinoline-based thiazolyl hydrazone derivatives and evaluate their anticandidal and anticancer effects. Methods: New thiazolyl hydrazone derivatives were evaluated for their anticandidal effects using disc diffusion metho Read More

Background: Mustard gas or sulfur mustard (dichloro-3-thiapentane-1,5) is a chemical compound consisting of chlorine and sulfur which was used as a chemical weapon in the First World War and during the war between Iran and Iraq. Mustard gas is a lipophilic compound that is highly poisonous and can quickly penetrate into body tissues. Eye is one of the body organs that is quite vulnerable to this compound. The pres Read More

Background: The anti-plasmin activity of Tranexamic Acid (TA) is considered to be the main mechanism of hypopigmentation. Several studies have found TA to be effective for both oral and topical application. When used to lighten stains, TA is effective even at low concentrations, ideally in the range of 2 to 5%. Increasing the duration of treatment is more effective than increasing the concentration of TA: Higher concentrations Read More