Breast Cancer Drug Repurposing a Tool for a Challenging Disease

Drug repurposing is one of the best strategy for drug discovery. There are several examples where drug repurposing has revolutionized the drug development process, such as metformin developed for diabetes and is now employed in polycystic ovarian syndrome. Drug repurposing against breast cancer is currently a hot topic to look upon. With the continued rise in breast cancer cases, there is a dire need for new therapies that can tackle it in a better way. There is a rise of resistance to current therapies, so drug repurposing might produce some lead candidates that may be promising to treat breast cancer. We will highlight the breast cancer molecular targets, currently available drugs, problems with current therapy, and some examples that might be promising to treat it.

Challenges and Tools for In Vitro Leishmania Exploratory Screening in the Drug Development Process: An Updated Review

Leishmaniases are a group of vector-borne diseases caused by infection with the protozoan parasites Leishmania spp. Some of them, such as Mediterranean visceral leishmaniasis, are zoonotic diseases transmitted from vertebrate to vertebrate by a hematophagous insect, the sand fly. As there is an endemic in more than 90 countries worldwide, this complex and major health problem has different clinical forms depending on the parasite species involved, with the visceral form being the most worrying since it is fatal when left untreated. Nevertheless, currently available antileishmanial therapies are significantly limited (low efficacy, toxicity, adverse side effects, drug-resistance, length of treatment, and cost), so there is an urgent need to discover new compounds with antileishmanial activity, which are ideally inexpensive and orally administrable with few side effects and a novel mechanism of action. Therefore, various powerful approaches were recently applied in many interesting antileishmanial drug development programs. The objective of this review is to focus on the very first step in developing a potential drug and to identify the exploratory methods currently used to screen in vitro hit compounds and the challenges involved, particularly in terms of harmonizing the results of work carried out by different research teams. This review also aims to identify innovative screening tools and methods for more extensive use in the drug development process.

Synthesis and Evaluation of Trypanocidal Activity of Chromane-Type Compounds and Acetophenones

American trypanosomiasis (Chagas disease) caused by the Trypanosoma cruzi parasite, is a severe health problem in different regions of Latin America and is currently reported to be spreading to Europe, North America, Japan, and Australia, due to the migration of populations from South and Central America. At present, there is no vaccine available and chemotherapeutic options are reduced to nifurtimox and benznidazole. Therefore, the discovery of new molecules is urgently needed to initiate the drug development process. Some acetophenones and chalcones, as well as chromane-type substances, such as chromones and flavones, are natural products that have been studied as trypanocides, but the relationships between structure and activity are not yet fully understood. In this work, 26 compounds were synthesized to determine the effect of hydroxyl and isoprenyl substituents on trypanocide activity. One of the compounds showed interesting activity against a resistant strain of T. cruzi, with a half effective concentration of 18.3 µM ± 1.1 and an index of selectivity > 10.9.

Significant role of chemistry in drug development: a systematic journey from traditional to modern approaches with anti-HIV/AIDS drugs as examples

Background: Traditionally, various plant extracts having interesting biological properties were the main source of new drugs. In the last 30 years, the role of chemistry in combination with new technologies, like various computational techniques in chemistry, has witnessed a major upsurge in drug discovery and targeted drug delivery. Objective: This article provides a succinct overview of recent techniques of chemistry that have a great impact on the drug development process in general and also against HIV/AIDS. It focuses on new methods employed for drug development with an emphasis on in silico studies, including identifying drug targets, especially the proteins associated with specific diseases. Methods: The rational drug development process starts with the identification of a drug target as the first phase, which helps in the computer-assisted design of new drug molecules. Synthetic chemistry has a major impact on the drug development process because it provides new molecules for future study. Natural products based semisynthesis or microwave assisted synthesis is also involved in developing newly designed drug molecules. Further, the role of analytical chemistry involves extraction, fractionation, isolation and characterization of newly synthesized molecules. Results: Chemistry plays a key role in drug discovery and delivery by natural process or with the help of synthetic nanoparticles or nanomedicines. So, nanochemistry is also deeply involved in the development of new drugs and their applications. Conclusion: The previous era of drug discovery was dominated only by chemistry, but the modern approaches involve a comprehensive knowledge of synthetic chemistry, medicinal chemistry, computational chemistry and the concerned biological phenomenon.

Traditional Approach to Cure Shingles Using Medicinal Plants in Eastern Nepal

Oral Collection and documentation of indigenous knowledge of local people have an important role in scientific research, biodiversity conservation, and the drug development process. A study was carried out to document the medicinal plants that have been used by the local folk healer to treat Shingles in Ilam district, Eastern Nepal. A renowned folk healer who was involved in curing Shingles for decades and 30 key informants were selected for the interview to know the methods of curing Shingles. Altogether six plants viz: Oroxylum indicum, Cynodon dactylon, Centella asiatica, Drymaria cordata, Sesamum indicum, and Lygodium japonicum were found to be used against the disease. The traditional method of preparing medicine from these plants was found to be highly effective. The finding provides a clue for further extensive lab-based research to isolate the specific compounds that are effective against the disease.

AI in drug development: a multidisciplinary perspective

The introduction of a new drug to the commercial market follows a complex and long process that typically spans over several years and entails large monetary costs due to a high attrition rate. Because of this, there is an urgent need to improve this process using innovative technologies such as artificial intelligence (AI). Different AI tools are being applied to support all four steps of the drug development process (basic research for drug discovery; pre-clinical phase; clinical phase; and postmarketing). Some of the main tasks where AI has proven useful include identifying molecular targets, searching for hit and lead compounds, synthesising drug-like compounds and predicting ADME-Tox. This review, on the one hand, brings in a mathematical vision of some of the key AI methods used in drug development closer to medicinal chemists and, on the other hand, brings the drug development process and the use of different models closer to mathematicians. Emphasis is placed on two aspects not mentioned in similar surveys, namely, Bayesian approaches and their applications to molecular modelling and the eventual final use of the methods to actually support decisions. Graphic abstract Promoting a perfect synergy

Biopolymer: A Novel Bioexcipient

Polymers are the key material in design of drug delivery systems. These have been shown as the spine for drug development process. These accept an essential part in rising of novel drug delivery systems to crush different intricacies in drug delivery. These are used for controlling the appearance of the drug in needed manner. The hydrophilic and lipophilic polymers are the most ideal choice for getting the ideal conveyance in controlled, manner at the target sites. Isolated of this, these fabricated and semisynthetic polymers are made by different chemical reactions and purification measures. Since these are prepared by different unit operations which are costly. By and by days different investigates are being examined for avoiding the characteristic, physiological and reasonable issues related with the synthetic and semisynthetic polymers. So an alternative rather than synthetic and semisynthetic polymers are being investigated having interest, probability, and any leftover benefits with least troublesome ramifications for environment and physiology of the people. One of the alternatives as opposed to designed and semisynthetic polymers is biopolymers which have pulled in the thought of researchers by using an economical procedures. Biopolymers are novel, adroit and sharp polymers which have been confined from various basic sources. Biopolymers isolated from natural sources might be utilized as novel excipients having a polymeric nature. These isolated biopolymers have superb bioretardant, bio stabilizer, and mucoadhesive properties. These have the brilliant film-framing capacity and biocompatibility properties. The isolated bio-polymers have great drug release rate controlling capacities. Since these are biodegradable and might be utilized as an option in contrast to standard manufactured synthetic and semisynthetic polymers. The isolated biopolymer shows critical biodegradable, mucoadhesive, filmability, and retardability properties which are like properties of standard polymers, may be the alternative in design of novel drug delivery system design.