Aims & Scope | Letters in Drug Design & Discovery




Letters in Drug Design & Discovery publishes letters, full-length/mini-reviews, highlights and guest edited thematic issues in all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis is on publishing quality papers very rapidly by taking full advantage of latest Internet technology for both submission and review of manuscripts. The online journal is an essential reading to all pharmaceutical scientists involved in research in drug design and discovery.

Open Access Articles | Synthesis and Biological Evaluation of Some Novel Thiophene-bearing Quinazoline Derivatives as EGFR Inhibitors

Author(s): Min Zou, Bo Jin, Yanrong Liu, Huiping Chen, Zhuangli Zhang, Changzheng Zhang, Zhihong Zhao, Liyun Zheng*.

With the approval of gefitinib, erlotinib, afatinib, and osimertinib for clinical use, targeting Epidermal Growth Factor Receptor (EGFR) has been intensively pursued. Similar to most therapies, challenges related to the treatment resistance against these drugs have emerged over time, so new EGFR Tyrosine Kinase Inhibitors (TKIs) need to be developed. This study aimed to investigate the potential use of a series of thiophene-bearing quinazoline derivatives as EGFR inhibitors. We designed and synthesized nine quinazolin derivatives, among which five compounds (5e, 5f, 5g, 5h, and 5i) were reported for the first time. Read out full article here:


Open acces

Contributions by Japanese authors in Bentham Science journal ‘Current Organic Synthesis’

Synthesis of Asymmetric Diaryl Sulfides by SNAr Reaction of Substituted Nitrobenzene with Aryl Disulfides

Author(s): Naoki Enjo, Rong Lu and Tetsuo Miyakoshi.

Abstract: A series of sulfides was successfully synthesized from nitroarenes by SNAr reaction via elimination of a nitro or phenylsulfonyl group. The SNAr reaction mechanism is found to depend on the position and type of substituents, and the effect of two-electron withdrawing groups was also examined.

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Two Neglected Multicomponent Reactions: Asinger and Groebke Reaction for Constructing Thiazolines and Imidazolines

Author(s): Zai-Qun Liu.

Abstract: The multicomponent reaction (MCR) is an important research field in the organic synthetic methodology. In 1956, Professor Friedrich Asinger reported a method for synthesizing thiazoline scaffold, in which a ketone was treated by sulfur and ammonia in one-pot operation. In 1998, Professor Katrin Groebke, Hugues Bienayme, and Christopher Blackburn reported a method for preparing imidazo[1,2-a]pyridine, in which an annulation took place among α- aminopyridine, aldehyde, and isocyanide in one-pot operation, and then the reaction was entitled as Groebke reaction. Comparing with the bloom in the research of other MCRs such as Strecker (found in 1850), Hantzsch (1882), Biginelli (1891), Mannich (1912), Passerini (1921) and Ugi (1959) MCR, as newcomers in the family of MCR, Asinger and Groebke reactions are not reported as usually as other MCRs. The aim of the present review is to emphasize the importance of these two MCRs in the synthesis of thiazolines and imidazolines. 

Articles From Bentham Science Impact Factor Journals

Current Nanoscience

Current Nanoscience publishes authoritative reviews, original research and highlights, written by experts in the field on all the most recent advances in nanoscience and nanotechnology. All aspects of the field are represented including nano- structures, nano-bubbles, nano-droplets, nanofluids, synthesis, properties, assembly and devices. Applications of nanoscience in biotechnology, medicine, pharmaceuticals, physics, material science and electronics are also covered. The journal is essential to all involved in nanoscience and its applied areas.

Article: A Short Overview on Light Enhancement in SOI and Void Nanostructures

By: A. Popescu

Affiliation: National Institute of R&D for Optoelectronics – INOE 2000, Bucharest-Magurele, Romania

Article: Analytical Study of Electronic Structure in Archimedean Type-Spiral Zig-Zag Graphene Nanoscroll

By: Razali Ismail

Affiliation: Computational Nanoelectronic Research Group, Faculty of Electrical Engineering, Universiti Teknologi Malaysia, 81310 Johor, Malaysia

Article: Superior Cell Adhesion and Antithrombogenicity Supported by N+-bombarded Carbon Nanotubes

By: D.J. Li

Affiliation: Energy & Materials Engineering Centre, College of Physics and Materials Science, Tianjin Normal University, Tianjin 300387, China

Article: Mono-substituted Molybdenium Preyssler Heteropolyacid: An Ecofriendly Photocatalyst for the Syntheses of Gold Nanoparticles in Solution and Titanium Dioxide Surface with Excellent Photoactivity in Combination with Titanium Dioxide

By: Fatemeh F. Bamoharram

Affiliation: Department of Chemistry, Mashhad Branch, Islamic Azad University, Mashhad, Iran

Article: Microbicidal Tissue Paper Using Green Synthesized Silver Nanoparticles

By: Muthusamy Sivakumar

Affiliation: Division of Nanoscience and Technology, Anna University-Tiruchirappalli, Tiruchirappalli-620024, India

Article: Incorporation of Inorganic Carbon Nanotubes Fillers into the CA Polymeric Matrix for Improvement in CO2/N2 Separation

By: A.L. Ahmad

Affiliation: School of Chemical Engineering, Engineering Campus, Universiti Sains Malaysia, 14300 Nibong Tebal, Penang, Malaysia

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