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Evaluation of novel synthesized thiazole derivatives as potential aromatase inhibitors against breast cancer
Evaluation of novel synthesized thiazole derivatives as potential aromatase inhibitors against breast cancer
Background: 4-Methylacetophenone is used in the preparation of starting materials, 4-methylphenacyle bromide (2) and 4-met...
Exploring the antimicrobial and cytotoxic potential of novel chloroquine analogues
Exploring the antimicrobial and cytotoxic potential of novel chloroquine analogues
Aim: To synthesize novel chloroquine analogues and evaluate them for antimicrobial and cytotoxic potential. Methods: Novel...
Design, synthesis and mechanistic study of new dual targeting HDAC/tubulin inhibitors
Design, synthesis and mechanistic study of new dual targeting HDAC/tubulin inhibitors
Aim: The purpose of this work is to create and synthesize a new class of chemicals: 3-cyano-2-substituted pyridine compoun...
Synthesis and molecular docking studies of 5-trifluoromethoxy-2-indolinones as cholinesterase dual inhibitors
Synthesis and molecular docking studies of 5-trifluoromethoxy-2-indolinones as cholinesterase dual inhibitors
Background: In Alzheimer’s disease, butyrylcholinesterase (BuChE) activity gradually increases, while acetylcholinesterase...
Drug discovery and development: the role of artificial intelligence in drug repurposing
Drug discovery and development: the role of artificial intelligence in drug repurposing
The authors have no competing interests or relevant affiliations with any organization or entity with the subject matter o...
Discovery of novel covalent inhibitors of DJ-1 through hybrid virtual screening
Discovery of novel covalent inhibitors of DJ-1 through hybrid virtual screening
Background: DJ-1 is a ubiquitously expressed protein with multiple functions. Its overexpression has been associated with ...
Antimicrobial activity of carvacrol and its derivatives on Mycobacterium spp.: systematic review of preclinical studies
Antimicrobial activity of carvacrol and its derivatives on Mycobacterium spp.: systematic review of preclinical studies
Background: The scope of the study was to analyze original preclinical studies on the antimicrobial effects of carvacrol a...
The discovery of a novel IκB kinase β inhibitor based on pharmacophore modeling, virtual screening and biological evaluation
The discovery of a novel IκB kinase β inhibitor based on pharmacophore modeling, virtual screening and biological evaluation
Background: IKKβ plays a pivotal role in the NF-κB signaling pathway and is considered a promising therapeutic target for ...
Chitosan–sulfonic acid-catalyzed green synthesis of naphthalene-based azines as potential anticancer agents
Chitosan–sulfonic acid-catalyzed green synthesis of naphthalene-based azines as potential anticancer agents
Aim: This study focuses on advancing green chemistry in anticancer drug discovery, particularly through the synthesis of a...
Design, synthesis and exploration of novel triazinoindoles as potent quorum-sensing inhibitors and radical quenchers
Design, synthesis and exploration of novel triazinoindoles as potent quorum-sensing inhibitors and radical quenchers
Background: Antimicrobial resistance has become a critical health concern, and quorum-sensing exacerbates the resistance b...
Design, synthesis and evaluation of aminothiazole derivatives as potential anti-Alzheimer’s candidates
Design, synthesis and evaluation of aminothiazole derivatives as potential anti-Alzheimer’s candidates
Aim: The objective of the present study was to design, synthesize and evaluate diverse Schiff bases and thiazolidin-4-one ...
Selenium: the emerging element in the medicinal chemist's toolkit
Selenium: the emerging element in the medicinal chemist's toolkit
The authors have no competing interests or relevant affiliations with any organization or entity with the subject matter o...
NeuroClick: software for mimicking click reaction to generate drug-like molecules permeating the blood–brain barrier
NeuroClick: software for mimicking click reaction to generate drug-like molecules permeating the blood–brain barrier
Background: Traditional methods for chemical library generation in virtual screening often impose limitations on the acces...
Unsymmetrical thiourea derivatives: synthesis and evaluation as promising antioxidant and enzyme inhibitors
Unsymmetrical thiourea derivatives: synthesis and evaluation as promising antioxidant and enzyme inhibitors
Background: Unsymmetrical thioureas 1–20 were synthesized and then characterized by various spectroscopy techniques such a...
BioPrint meets the AI age: development of artificial intelligence-based ADMET models for the drug discovery platform SAFIRE
BioPrint meets the AI age: development of artificial intelligence-based ADMET models for the drug discovery platform SAFIRE
Background: To prioritize compounds with a higher likelihood of success, artificial intelligence models can be used to pre...
Emerging synthetic strategies and pharmacological insights of 1,3,4-thiadiazole derivatives: a comprehensive review
Emerging synthetic strategies and pharmacological insights of 1,3,4-thiadiazole derivatives: a comprehensive review
This review meticulously examines the synthesis techniques for 1,3,4-thiadiazole derivatives, focusing on cyclization, con...
Novel sulfonamide derivatives as a tool to combat methicillin-resistant Staphylococcus aureus
Novel sulfonamide derivatives as a tool to combat methicillin-resistant Staphylococcus aureus
Increasing resistance in Staphylococcus aureus has created a critical need for new drugs, especially those effective again...
Design, synthesis and anticancer evaluation of some novel 7-hydroxy-4-methyl-3-substituted benzopyran-2-one derivatives
Design, synthesis and anticancer evaluation of some novel 7-hydroxy-4-methyl-3-substituted benzopyran-2-one derivatives
Aim: 22 derivatives of 7-hydroxy-4-methyl-3-substituted benzopyran-2-one were designed, synthesized and evaluated for thei...
Synthesis and antimicrobial activity of thiophene-based heterocycles derived from thiophene-2-carbohydrazide
Synthesis and antimicrobial activity of thiophene-based heterocycles derived from thiophene-2-carbohydrazide
Aim: Thiophene-based heterocycles were synthesized and evaluated for their antimicrobial activity against methicillin-resi...
Synthesis, in vitro bio-evaluation and in silico molecular docking studies of thiadiazole-based Schiff base derivatives
Synthesis, in vitro bio-evaluation and in silico molecular docking studies of thiadiazole-based Schiff base derivatives
Aim: Recently, thiadiazole-containing drugs have gained greater clinical relevance and are being explored for the developm...
19 Schiff bases as antimycobacterial agents: synthesis, molecular docking and a plausible mechanism of action
19 Schiff bases as antimycobacterial agents: synthesis, molecular docking and a plausible mechanism of action
Aim: To discover novel anti-Mycobacterium tuberculosis (Mtb) drugs, 19 compounds were synthesized; their anti-Mtb effects ...
Investigations of new N1-substituted pyrazoles as anti-inflammatory and analgesic agents having COX inhibitory activity
Investigations of new N1-substituted pyrazoles as anti-inflammatory and analgesic agents having COX inhibitory activity
Background: The search is ongoing for ideal anti-inflammatory and analgesic agents with promising potency and reasonable s...
Novel 2-indolinone derivatives as promising agents against respiratory syncytial and yellow fever viruses
Novel 2-indolinone derivatives as promising agents against respiratory syncytial and yellow fever viruses
Background: A vaccine or antiviral drug for respiratory syncytial virus (RSV) infections and a specific antiviral drug for...
Molecules inducing specific cyclin-dependent kinase degradation and their possible use in cancer therapy
Molecules inducing specific cyclin-dependent kinase degradation and their possible use in cancer therapy
Cyclin-dependent kinases (CDKs) play an important role in the regulation of cell proliferation, and many CDK inhibitors we...
Exploring new imines as anti-inflammatory COX and 5-LOX inhibitors with an improved pharmacokinetic profile
Exploring new imines as anti-inflammatory COX and 5-LOX inhibitors with an improved pharmacokinetic profile
Background: Dual COX/5-LOX inhibition is a bright strategy for developing new potent and safe anti-inflammatory agents. Me...
Recent developments of hydroxamic acid hybrids as potential anti-breast cancer agents
Recent developments of hydroxamic acid hybrids as potential anti-breast cancer agents
Histone deacetylase inhibitors not only possess favorable effects on modulating tumor microenvironment and host immune cel...
Synthesis of hydrazinyl–thiazole ester derivatives, in vitro trypanocidal and leishmanicidal activities
Synthesis of hydrazinyl–thiazole ester derivatives, in vitro trypanocidal and leishmanicidal activities
Aim: To synthesize novel more potent trypanocidal and leishmanicidal agents. Methods: Hantzsch’s synthetic strategy was us...
Emerging therapeutic approaches of SHP2-targeted modulators
Emerging therapeutic approaches of SHP2-targeted modulators
Tweetable abstract Monotherapy and combination therapy of SHP2 regulator for cancer treatment.
Recent advances in the synthesis and medicinal perspective of pyrazole-based α-amylase inhibitors as antidiabetic agents
Recent advances in the synthesis and medicinal perspective of pyrazole-based α-amylase inhibitors as antidiabetic agents
Diabetes is a serious health threat across the globe, claiming millions of lives worldwide. Among the various strategies e...