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Palbociclib-derived multifunctional molecules for lysosomal targeting and diagnostic-therapeutic integration
Palbociclib-derived multifunctional molecules for lysosomal targeting and diagnostic-therapeutic integration
Aim: Lysosomal pH changes are associated with drug resistance, cell growth and invasion of tumors, but effective and speci...
Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights
Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights
Aim: Synthesis of novel bis-Schiff bases having potent inhibitory activity against phosphodiesterase (PDE-1 and -3) enzyme...
Cu-promoted synthesis of triclosan-Mannich and Glaser adducts: anti-mycobacterial evaluation with in silico validations
Cu-promoted synthesis of triclosan-Mannich and Glaser adducts: anti-mycobacterial evaluation with in silico validations
Aim: The WHO, Global tuberculosis report 2022 estimated number of tuberculosis (TB) cases reached 10.6 million in 2021, re...
Thiazolation of phenylthiosemicarbazone to access new thiazoles: anticancer activity and molecular docking
Thiazolation of phenylthiosemicarbazone to access new thiazoles: anticancer activity and molecular docking
Aim: Novel thiazole hybrids were synthesized via thiazolation of 4-phenylthiosemicarbazone (4). Materials & methods: T...
Design, synthesis and biological evaluation of 1-aryldonepezil analogues as anti-Alzheimer's disease agents
Design, synthesis and biological evaluation of 1-aryldonepezil analogues as anti-Alzheimer's disease agents
Aim: To design and synthesize a novel series of 1-aryldonepezil analogues. Materials & methods: The 1-aryldonepezil an...
Exploring the current advancements of quercetin nanoformulations alleviating respiratory diseases
Exploring the current advancements of quercetin nanoformulations alleviating respiratory diseases
The authors have no competing interests or relevant affiliations with any organization or entity with the subject matter o...
Synthesis, anti-diabetic profiling and molecular docking studies of 2-(2-arylidenehydrazinyl)thiazol-4(5H)-ones
Synthesis, anti-diabetic profiling and molecular docking studies of 2-(2-arylidenehydrazinyl)thiazol-4(5H)-ones
Aim: To synthesize novel more potent anti-diabetic agents. Methodology: A simple cost effective Hantzsch's synthetic strat...
Anti-proliferation evaluation of new derivatives of indole-6-carboxylate ester as receptor tyrosine kinase inhibitors
Anti-proliferation evaluation of new derivatives of indole-6-carboxylate ester as receptor tyrosine kinase inhibitors
Aim: The main goal was to create two new groups of indole derivatives, hydrazine-1-carbothioamide (4a and 4b) and oxadiazo...
Design, synthesis and biological evaluation of sulfamethazine derivatives as potent neuraminidase inhibitors
Design, synthesis and biological evaluation of sulfamethazine derivatives as potent neuraminidase inhibitors
Aim: The purpose of this study is to design and synthesize a new series of sulfamethazine derivatives as potent neuraminid...
Harnessing molecular hybridization approach to discover novel quinoline EGFR-TK inhibitors for cancer treatment
Harnessing molecular hybridization approach to discover novel quinoline EGFR-TK inhibitors for cancer treatment
Aim: Using molecular hybridization approach, novel 18 quinoline derivatives (6a–11) were designed and synthesized as EGFR-...
Synthesis and interest in medicinal chemistry of β-phenylalanine derivatives (β-PAD): an update (2010–2022)
Synthesis and interest in medicinal chemistry of β-phenylalanine derivatives (β-PAD): an update (2010–2022)
β-Phenylalanine derivatives (β-PAD) represent a structural family of therapeutic interest, either as components of drugs o...
Synthesis and antiproliferative evaluation of novel 3,5,8-trisubstituted coumarins against breast cancer
Synthesis and antiproliferative evaluation of novel 3,5,8-trisubstituted coumarins against breast cancer
Aim: This study focused on designing and synthesizing novel derivatives of 3,5,8-trisubstituted coumarin. Results: The syn...
Quinazoline sulfonamide derivatives targeting MicroRNA-34a/MDM4/p53 apoptotic axis with radiosensitizing activity
Quinazoline sulfonamide derivatives targeting MicroRNA-34a/MDM4/p53 apoptotic axis with radiosensitizing activity
Aim: New quinazoline benzenesulfonamide hybrids 4a–n were synthesized to determine their cytotoxicity and effect on the mi...
Application of parallel artificial membrane permeability assay technique and chemometric modeling for blood–brain barrier permeability prediction of protein kinase inhibitors
Application of parallel artificial membrane permeability assay technique and chemometric modeling for blood–brain barrier permeability prediction of protein kinase inhibitors
Aim: This study aims to investigate the passive diffusion of protein kinase inhibitors through the blood–brain barrier (BB...
Exploring of novel oxazolones and imidazolones as anti-inflammatory and analgesic candidates with cyclooxygenase inhibitory action
Exploring of novel oxazolones and imidazolones as anti-inflammatory and analgesic candidates with cyclooxygenase inhibitory action
Aim: Over the last few decades, therapeutic needs have led to a search for safer COX-2 inhibitors with potential anti-infl...
Insight on novel oxindole conjugates adopting different anti-inflammatory investigations and quantitative evaluation
Insight on novel oxindole conjugates adopting different anti-inflammatory investigations and quantitative evaluation
Background: A dual COX/5-LOX strategy was adopted to develop new oxindole derivatives with superior anti-inflammatory acti...
Key structural requirements of benzamide derivatives for histone deacetylase inhibition: design, synthesis and biological evaluation
Key structural requirements of benzamide derivatives for histone deacetylase inhibition: design, synthesis and biological evaluation
Background: Histone deacetylase inhibitors (HDACIs) are important as anticancer agents. Objective: This study aimed to inv...
The anticancer therapeutic potential of pyrimidine–sulfonamide hybrids
The anticancer therapeutic potential of pyrimidine–sulfonamide hybrids
Cancer as a devastating malignancy, seriously threatens human life and health, but most chemotherapeutics have long been c...
Synthesis, in vitro and in silico anticancer evaluation of novel pyridin-2-yl estra-1,3,5(10)-triene derivatives
Synthesis, in vitro and in silico anticancer evaluation of novel pyridin-2-yl estra-1,3,5(10)-triene derivatives
Aim: The aim of this study was the synthesis of steroid compounds with heterocyclic rings and good anticancer properties. ...
Design, synthesis and biological evaluation of novel 3C-like protease inhibitors as lead compounds against SARS-CoV-2
Design, synthesis and biological evaluation of novel 3C-like protease inhibitors as lead compounds against SARS-CoV-2
Background: The epidemic caused by SARS-CoV-2 swept the world in 2019. The 3C-like protease (3CLpro) of SARS-CoV-2 plays a...
ProHES: hydroxyethyl starch's transformative role in anticancer drug delivery
ProHES: hydroxyethyl starch's transformative role in anticancer drug delivery
The authors have no financial involvement with any organization or entity with a financial interest in or financial confli...
Design and synthesis of novel coumarin–benzimidazole hybrids as human galectin-1 inhibitors
Design and synthesis of novel coumarin–benzimidazole hybrids as human galectin-1 inhibitors
Aim: To develop novel non-carbohydrate inhibitors of human galectin-1 (GAL-1), we have designed a series of coumarin–benzi...
PTSA-induced synthesis, in silico and nano study of novel ethylquinolin–thiazolo–triazole in cervical cancer
PTSA-induced synthesis, in silico and nano study of novel ethylquinolin–thiazolo–triazole in cervical cancer
Aim: p-Toluenesulfonic acid-(PTSA) and grinding-induced novel synthesis of ethylquinolin–thiazolo–triazole derivatives was...
Design, synthesis and evaluation of new thiazolidin-4-ones as LPA1 receptor antagonists for breast cancer therapy
Design, synthesis and evaluation of new thiazolidin-4-ones as LPA1 receptor antagonists for breast cancer therapy
Aim: Breast cancer has been a leading cause of mortality among women worldwide in recent years. Targeting the lysophosphat...
Novel 1,2,4-triazoles as selective carbonic anhydrase inhibitors showing ancillary anticathepsin B activity
Novel 1,2,4-triazoles as selective carbonic anhydrase inhibitors showing ancillary anticathepsin B activity
Background: Exploration of the multi-target approach considering both human carbonic anhydrase (hCA) IX and XII and cathep...
The contemplation of amylose for the delivery of ulcerogenic nonsteroidal anti-inflammatory drugs
The contemplation of amylose for the delivery of ulcerogenic nonsteroidal anti-inflammatory drugs
This manuscript proposes an innovative approach to mitigate the gastrointestinal adversities linked with nonsteroidal anti...
One-step synthesis of diaryloxadiazoles as potent inhibitors of BCRP
One-step synthesis of diaryloxadiazoles as potent inhibitors of BCRP
Aim: BCRP plays a major role in the efflux of cytotoxic molecules, limiting their antiproliferative activity. We aimed to ...
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...
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