Advancements in folate receptor targeting for anti-cancer therapy: A small molecule-drug conjugate approach.

Targeted delivery combined with controlled release of drugs has a crucial role in future of personalized medicine. The majority of cancer drugs are intended to interfere with one or more cellular events. Anticancer agents can also be toxic to healthy cells, as healthy cells may also need to proliferate and avoid apoptosis. The focus of this review covers the principles, advantages, drawbacks and summarize criteria that must be met for design of small molecule-drug conjugates (SMDCs) to achieve the desired therapeutic potency with minimal toxicity. SMDCs are composed of a targeting ligand, a releasable bridge, a spacer, and a therapeutic payload. We summarize the criteria for the effective design that influences the selection of tumor specific receptor and optimum elements in the design of SMDCs. We also discuss the criteria for selecting the optimal therapeutic drug payload, spacer and linker. The linker chemistries and cleavage strategies are also discussed. Finally, we review the folate receptor targeting SMDCs that are in preclinical development and in clinical trials.

Auto-Optimized Electro-Flow Reactor Platform for the in-situ Reduction of P(V) Oxide to P(III) and Their Application.

Trivalent phosphine catalysis is mostly utilized to activate the carbon-carbon multiple bonds to form carbanion intermediate species and is highly sensitive to certain variables. Random manual multi-variables are critical for understanding the batch disabled regeneration of trivalent phosphine chemistry. We need the artificial intelligence-based system which can change the variable based on previously conducted failed experiment. Herein, we report an auto-optimized electro-micro-flow reactor platform for the in-situ reduction of stable P(V) oxide to sensitive P(III) and further utilized the method for Corey-Fuchs reaction.

"Smart" drug delivery: A window to future of translational medicine.

Chemotherapy is the mainstay of cancer treatment today. Chemotherapeutic drugs are non-selective and can harm both cancer and healthy cells, causing a variety of adverse effects such as lack of specificity, cytotoxicity, short half-life, poor solubility, multidrug resistance, and acquiring cancer stem-like characteristics. There is a paradigm shift in drug delivery systems (DDS) with the advent of smarter ways of targeted cancer treatment. Smart Drug Delivery Systems (SDDSs) are stimuli responsive and can be modified in chemical structure in response to light, pH, redox, magnetic fields, and enzyme degradation can be future of translational medicine. Therefore, SDDSs have the potential to be used as a viable cancer treatment alternative to traditional chemotherapy. This review focuses mostly on stimuli responsive drug delivery, inorganic nanocarriers (Carbon nanotubes, gold nanoparticles, Meso-porous silica nanoparticles, quantum dots etc.), organic nanocarriers (Dendrimers, liposomes, micelles), antibody-drug conjugates (ADC) and small molecule drug conjugates (SMDC) based SDDSs for targeted cancer therapy and strategies of targeted drug delivery systems in cancer cells.

Recent efforts for drug identification from phytochemicals against SARS-CoV-2: Exploration of the chemical space to identify druggable leads.

Nature, which remains a central drug discovery pool, is always looked upon to find a putative druggable lead. The natural products and phytochemical derived from plants are essential during a global health crisis. This class represents one of the most practical and promising approaches to decrease pandemic's intensity owing to their therapeutic potential. The present manuscript is therefore kept forth to give the researchers updated information on undergoing research in allied areas of natural product-based drug discovery, particularly for Covid-19 disease. The study briefly shreds evidence from in vitro and in silico researches done so far to find a lead molecule against Covid-19. Following this, we exhaustively explored the concept of chemical space and molecular similarity parameters for the drug discovery about the lead(s) generated from in silico-based studies. The comparison was drawn using FDA-approved anti-infective agents during 2015-2020 using key descriptors to evaluate druglike properties. The outcomes of results were further corroborated using Molecular Dynamics studies which suggested the outcomes in alignment with chemical space ranking. In a nutshell, current research work aims to provide a holistic strategic approach to drug design, keeping in view the identified phytochemicals against Covid-19.

Essential Oils: An Impending Substitute of Synthetic Antimicrobial Agents to Overcome Antimicrobial Resistance.

Antimicrobial resistance (AMR) is an emerging problem in the world that has a significant impact on our society. AMR made conventional drugs futile against microorganisms and diseases untreatable. Plant-derived medicines are considered to be safe alternatives as compared to synthetic drugs. Active ingredients and the mixtures of these natural medicines have been used for centuries, due to their easy availability, low cost, and negligible side effects. Essential oils (EOs) are the secondary metabolites that are produced by aromatic plants to protect them from microorganisms. However, these EOs and their constituents have shown good fighting potential against drug-resistant pathogens. These oils have been proved extremely effective antimicrobial agents in comparison to antibiotics. Also, the combination of synthetic drugs with EOs or their components improve their efficacy. So, EOs can be established as an alternative to synthetic antimicrobial agents to eradicate tough form of infectious microorganisms. EO's can interact with multiple target sites, like the destruction of cytoplasm membrane or inhibition of protein synthesis and efflux pump, etc. The purpose of this review is to provide information about the antimicrobial activity of EOs attained from different plants, their combination with synthetic antimicrobials. In addition, mechanism of antimicrobial activity of several EOs and their constituents was reported.