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Design, synthesis and antitumor activity study of tubulin/HDAC6 dual targeting inhibitor
Design, synthesis and antitumor activity study of tubulin/HDAC6 dual targeting inhibitor
Cancer combination therapy is a novel strategy to circumvent drug resistance in highly metastatic and advanced malignancie...
Pharmacological significance of palbociclib and its derivatives in cancer treatment and prevention: an update
Pharmacological significance of palbociclib and its derivatives in cancer treatment and prevention: an update
Palbociclib is a selective cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitor that emerged as a significant therapeutic a...
Exploring putative histone deacetylase inhibitors with antiproliferative activity of chrysin derivatives
Exploring putative histone deacetylase inhibitors with antiproliferative activity of chrysin derivatives
Thirty-three derivatives of chrysin were designed and synthesized to evaluate biological activities. All compounds were ch...
Design and synthesis of novel 1-1,2,3-triazolecarbohydrazides and 1,2,4-triazoloazines based on them for anticancer drug discovery
Design and synthesis of novel 1-1,2,3-triazolecarbohydrazides and 1,2,4-triazoloazines based on them for anticancer drug discovery
The synthesis of (1H-1,2,3-triazol-4-yl)-1,2,4-triazolazine derivatives was achieved via a multi-step synthesis starting f...
Discovery of a novel selenamide derivative as potent activator of aldehyde dehydrogenase 2 for cardioprotective applications
Discovery of a novel selenamide derivative as potent activator of aldehyde dehydrogenase 2 for cardioprotective applications
Aldehyde dehydrogenase 2 (ALDH2), a mitochondrial enzyme, plays a pivotal role in the metabolism of endogenous reactive al...
Benzoxa-[2,1,3]-diazole substituted amino acid hydrazides as therapeutics for drug-resistant
Benzoxa-[2,1,3]-diazole substituted amino acid hydrazides as therapeutics for drug-resistant
The global burden of tuberculosis is on the rise and continues to be alarmingly high, with a notable prevalence of multidr...
Development of novel caffeic acid derivatives as multifunctional agents for the treatment of AD
Development of novel caffeic acid derivatives as multifunctional agents for the treatment of AD
Alzheimer’s disease (AD) is a progressive neurodegenerative disorder for which the multi-target-directed ligand (MTD...
Design and discovery of POLQ helicase domain inhibitors by virtual screening and machine learning
Design and discovery of POLQ helicase domain inhibitors by virtual screening and machine learning
DNA polymerase theta (Polθ or POLQ) is an attractive target for treating BRCA-deficient cancers. In the present work,...
Nanosensing doxorubicin: a new frontier in medicinal chemistry
Nanosensing doxorubicin: a new frontier in medicinal chemistry
The advent of nanosensing technologies marks a significant advancement in medicinal chemistry, particularly in the detecti...
The inhibition of monoamine oxidase by 2-methylbenzo[]oxazole derivatives
The inhibition of monoamine oxidase by 2-methylbenzo[]oxazole derivatives
The monoamine oxidase (MAO) enzymes metabolise neurotransmitter amines and are drug targets for the treatment of neuropsyc...
Inhibition potential against butyrylcholinesterase of stilbenes, bibenzyls, and dihydrophenanthrenes from
Inhibition potential against butyrylcholinesterase of stilbenes, bibenzyls, and dihydrophenanthrenes from
Butyrylcholinesterase (BuChE, EC 3.1.1.8) inhibitors have promising application prospects as they can alleviate cognitive ...
Design, synthesis and biological evaluation of monoglyceride lipase inhibitors guided by dipeptidyl peptidase IV inhibitors
Design, synthesis and biological evaluation of monoglyceride lipase inhibitors guided by dipeptidyl peptidase IV inhibitors
This study aimed to develop inhibitors of monoglyceride lipase, a key enzyme in lipolysis linked to insulin resistance, us...
Prenylated flavonoids icariin and icaritin for drug discovery: structural modifications and bioactivity studies
Prenylated flavonoids icariin and icaritin for drug discovery: structural modifications and bioactivity studies
Prenylated flavonoids icariin and icaritin are the crucial ingredients of traditional Chinese medicinal Herb Epimedii. Ica...
Carbamoyl flavonoids as dual inhibitors of acetylcholinesterase and monoacylglycerol lipase: synthesis, in vitro evaluation, and computational studies
Carbamoyl flavonoids as dual inhibitors of acetylcholinesterase and monoacylglycerol lipase: synthesis, in vitro evaluation, and computational studies
Alzheimer’s disease is a complex neurodegenerative disorder characterized by cognitive decline and memory loss, with...
Synthesis and in vitro study of a novel catechol with a hydantoin core
Synthesis and in vitro study of a novel catechol with a hydantoin core
In this work, stable chemical precursors (3,5-DTBC) and alkylated derivatives were synthesized through strategic modificat...
Phytochemistry and pharmacological activities of genus: An updated review
Phytochemistry and pharmacological activities of genus: An updated review
Plants have played a vital role in medicine from ancient times to the present. Many plant species have been used as medici...
Synthesis, characterization and in vitro antitumor activity of asiatic acid derivatives
Synthesis, characterization and in vitro antitumor activity of asiatic acid derivatives
Twenty-seven asiatic acid derivatives were designed and synthesized in this paper, including twenty-two new compounds. The...
Summary of paeoniflorin derivatives and their biological activities
Summary of paeoniflorin derivatives and their biological activities
Paeoniflorin is one of the active components of the root of peony, which has powerful and diverse pharmacological activiti...
Design and synthesis of formononetin-piperazine hybrids that inhibit the migration and growth of MGC-803 cells
Design and synthesis of formononetin-piperazine hybrids that inhibit the migration and growth of MGC-803 cells
Formononetin, derived from Orostachys japonica (a traditional Chinese medicine), has been reported to have anti-cancer act...
Design, synthesis, molecular docking, and biological activity of pyrazolo[3,4-b]pyridines as promising lead candidates against Mycobacterium tuberculosis
Design, synthesis, molecular docking, and biological activity of pyrazolo[3,4-b]pyridines as promising lead candidates against Mycobacterium tuberculosis
Pyrazolo[3,4-b]pyridine is a medicinally privileged structure. We have achieved a new and facile synthesis of a combinator...
A concise review on anti-breast cancer effectiveness of s-triazines through EGFR kinase inhibition
A concise review on anti-breast cancer effectiveness of s-triazines through EGFR kinase inhibition
Today, one of the most common malignancies in women is breast cancer. Despite the large number of commercially available a...
Unveiling the potential of prodrug and drug-conjugate strategies in treatment of diabetes mellitus and its complications
Unveiling the potential of prodrug and drug-conjugate strategies in treatment of diabetes mellitus and its complications
The 2021 statistics from the International Diabetes Federation reveals that approximately 537 million adults between the a...
Synthesis of adamantane-monoterpene conjugates with 1,3,4-thiadiazol-2(3H)-imine linker and evaluation of their inhibitory activity against TDP1
Synthesis of adamantane-monoterpene conjugates with 1,3,4-thiadiazol-2(3H)-imine linker and evaluation of their inhibitory activity against TDP1
Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a DNA repair enzyme that can reduce the efficacy of some anticancer drugs target...
Self-assembled amphiphilic bipyridine and bisquinoline cisplatin analogues: synthesis and anticancer properties
Self-assembled amphiphilic bipyridine and bisquinoline cisplatin analogues: synthesis and anticancer properties
We report the synthesis and characterisation of two amphiphilic cisplatin analogues derived from bipyridine and bisquinoli...
Increased rigidity and bioisosteric replacement in the design, synthesis and preliminary evaluation of novel, functionalized 3,3-dialkyl-γ-butyrolactones as sigma-2 ligands
Increased rigidity and bioisosteric replacement in the design, synthesis and preliminary evaluation of novel, functionalized 3,3-dialkyl-γ-butyrolactones as sigma-2 ligands
The sigma-2 (σ2) receptor has been linked to several diseases and conditions including cancer, neuropathic drug addic...
Identification of α-mangostin as a potent inhibitor of β-lactamase OXA-48
Identification of α-mangostin as a potent inhibitor of β-lactamase OXA-48
The production of carbapenemases is a significant mechanism contributing to carbapenem resistance in Enterobacteriaceae. A...
Synthesis and pharmacological evaluation of novel coumarin based triazolyl glycoconjugates as potential antibacterial and anti-proliferative agents
Synthesis and pharmacological evaluation of novel coumarin based triazolyl glycoconjugates as potential antibacterial and anti-proliferative agents
A library of novel coumarin-based triazolyl glycoconjugates is prepared and screened for in vitro antibacterial activity a...
Rehmannia glutinosa polysaccharides: a review on structure-activity relationship and biological activity
Rehmannia glutinosa polysaccharides: a review on structure-activity relationship and biological activity
Rehmannia glutinosa has been used historically and is now listed in the 2020 Chinese Pharmacopoeia as a traditional Chines...
Bioactivities and the structural modification of Parthenolide: a review
Bioactivities and the structural modification of Parthenolide: a review
Parthenolide, a sesquiterpene lactone derived from Feverfew (Tanacetum parthenium) buds, has attracted significant attenti...
Research progress on the mechanism of anti-myocardial infarction effect and clinical application of effective components of Salvia miltiorrhiza
Research progress on the mechanism of anti-myocardial infarction effect and clinical application of effective components of Salvia miltiorrhiza
Salvia miltiorrhiza, a plant in the Labiatae family, is a traditional Chinese herb. The small molecular components in S. m...
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