SCI时时刷

search
+
Dual site reactivity of indole-3-Schiff bases with S/Se/Cl substituted ketenes for stereoselective C-4 substituted indole-β-lactams, biological evaluations, magic chloro effect and molecular docking studies
Dual site reactivity of indole-3-Schiff bases with S/Se/Cl substituted ketenes for stereoselective C-4 substituted indole-β-lactams, biological evaluations, magic chloro effect and molecular docking studies
The landscape of medicinal chemistry in drug discovery has witnessed significant transformations [1]. An era of drug disco...
The novel small molecule E0924G dually regulates bone formation and bone resorption through activating the PPARδ signaling pathway to prevent bone loss in ovariectomized rats and senile mice
The novel small molecule E0924G dually regulates bone formation and bone resorption through activating the PPARδ signaling pathway to prevent bone loss in ovariectomized rats and senile mice
Osteoporosis is a systemic skeletal disease that is particularly prevalent among postmenopausal women and elderly people [...
Inhibition of TGF-β1/Smad3 signaling by compound 5aa: A potential treatment for idiopathic pulmonary fibrosis
Inhibition of TGF-β1/Smad3 signaling by compound 5aa: A potential treatment for idiopathic pulmonary fibrosis
Idiopathic pulmonary fibrosis (IPF) is a progressive interstitial lung disease characterized by widespread scar tissue for...
Non-peptidic inhibitors targeting SARS-CoV-2 main protease: A review
Non-peptidic inhibitors targeting SARS-CoV-2 main protease: A review
The outbreak of coronavirus disease 2019 (COVID-19) signified the commencement of a global health crisis [1], [2]. Origina...
Design, synthesis, docking, and antiviral evaluation of some novel pyrimidinone-based α-aminophosphonates as potent H1N1 and HCoV-229E inhibitors
Design, synthesis, docking, and antiviral evaluation of some novel pyrimidinone-based α-aminophosphonates as potent H1N1 and HCoV-229E inhibitors
Global health concerns are increasingly focused on the emergence of controversial pandemics caused by the viruses of the c...
Peroxynitrite-activated fluorescent probe with two reaction triggers for pathological diagnosis and therapeutic evaluation of inflammation
Peroxynitrite-activated fluorescent probe with two reaction triggers for pathological diagnosis and therapeutic evaluation of inflammation
Inflammation is an innate protective response to pathological signs arising from tissue injury or pathogen-associated infe...
Design, synthesis, and biological evaluation of cathepsin B cleavage albumin-binding SN38 prodrug in breast cancer
Design, synthesis, and biological evaluation of cathepsin B cleavage albumin-binding SN38 prodrug in breast cancer
Albumin stands as a crucial and abundantly present plasma protein, pivotal in various physiological functions [1], [2]. It...
Discovery of novel thiophene-3-carboxamide derivatives as potential VEGFR-2 inhibitors with anti-angiogenic properties
Discovery of novel thiophene-3-carboxamide derivatives as potential VEGFR-2 inhibitors with anti-angiogenic properties
Angiogenesis is a crucial factor in tumor proliferation and metastasis [1], [2]. Among the various participants involved i...
13-Oxyingenol-dodecanoate inhibits the growth of non-small cell lung cancer cells by targeting ULK1
13-Oxyingenol-dodecanoate inhibits the growth of non-small cell lung cancer cells by targeting ULK1
According to the World Health Organization's 2020 publication of global lung cancer incidence and mortality rates, lung ca...
Synthesis, structural, multitargeted molecular docking analysis of anti-cancer, anti-tubercular, DNA interactions of benzotriazole based macrocyclic ligand
Synthesis, structural, multitargeted molecular docking analysis of anti-cancer, anti-tubercular, DNA interactions of benzotriazole based macrocyclic ligand
Macrocyclic molecules are molecules bearing at least 12 atoms with a cyclic skeleton, and they have unique spatial structu...
Rapid identifying of COX-2 inhibitors from turmeric (Curcuma longa) by bioaffinity ultrafiltration coupled with UPLC-Q Exactive-Orbitrap-MS and zebrafish-based in vivo validation
Rapid identifying of COX-2 inhibitors from turmeric (Curcuma longa) by bioaffinity ultrafiltration coupled with UPLC-Q Exactive-Orbitrap-MS and zebrafish-based in vivo validation
Inflammation is associated with nearly all major human diseases [1]. Besides causing discomfort such as redness, swelling,...
Discovery of two non-UDP-mimic inhibitors of O-GlcNAc transferase by screening a DNA-encoded library
Discovery of two non-UDP-mimic inhibitors of O-GlcNAc transferase by screening a DNA-encoded library
Volume 147, June 2024, 107321Author links open overlay panel, , , , , , , , Highlights•Screening of a DNA-encoded library ...
Development of D-π-A organic dyes for discriminating HSA from BSA and study on dye-HSA interaction
Development of D-π-A organic dyes for discriminating HSA from BSA and study on dye-HSA interaction
Enzymes are biomacromolecules for biological processes in a living being, assisting organisms in controlling physiological...
New meroterpenoids and polyketides from the endophytic fungus Paraphaeosphaeria sp. C-XB-J-1 and their anti-inflammatory and SARS-CoV-2 Mpro inhibitory activities
New meroterpenoids and polyketides from the endophytic fungus Paraphaeosphaeria sp. C-XB-J-1 and their anti-inflammatory and SARS-CoV-2 Mpro inhibitory activities
Meroterpenoids were a class of natural secondary metabolites which structural moieties partially derive from terpenoid met...
Chaetoxylariones A–G: undescribed chromone-derived polyketides from co-culture of Chaetomium virescens and Xylaria grammica enabled via the molecular networking strategy
Chaetoxylariones A–G: undescribed chromone-derived polyketides from co-culture of Chaetomium virescens and Xylaria grammica enabled via the molecular networking strategy
Smilax glabra Roxb. (SGB), which belongs to the Smilacaceae family, is the dry rhizome of the Sarsaparilla plant known as ...
Discovery of a new class of potent pyrrolo[3,4-c]quinoline-1,3-diones based inhibitors of human dihydroorotate dehydrogenase: Synthesis, pharmacological and toxicological evaluation
Discovery of a new class of potent pyrrolo[3,4-c]quinoline-1,3-diones based inhibitors of human dihydroorotate dehydrogenase: Synthesis, pharmacological and toxicological evaluation
Pyrimidine nucleotides play crucial roles in the biosynthesis of DNA, RNA, glycoproteins and membrane lipids [1]. Human di...
Synthesis, physicochemical characterization, and investigation of anti-inflammatory activity of water-soluble PEGylated 1,2,4-Triazoles
Synthesis, physicochemical characterization, and investigation of anti-inflammatory activity of water-soluble PEGylated 1,2,4-Triazoles
Inflammation is a process mediated by activated macrophages and pro-inflammatory cytokines, resulting in the accumulation ...
Design, selective synthesis and biological activities evaluation of novel thiazol-2-ylbenzamide and thiazole-2-ylbenzimidoyl chloride derivatives
Design, selective synthesis and biological activities evaluation of novel thiazol-2-ylbenzamide and thiazole-2-ylbenzimidoyl chloride derivatives
Chemical fungicides play a vital role in protecting plants and are considered one of the most cost-effective and efficient...
d-type peptides based fluorescent probes for “turn on” sensing of heparin
d-type peptides based fluorescent probes for “turn on” sensing of heparin
Heparin is a highly sulfated linear polysaccharide, mainly composed of different sulfated disaccharide units such as iduro...
Corrigendum to “A novel Cereblon E3 ligase modulator with antitumor activity in gastrointestinal cancer” [Bioorgan. Chem. 119 (2022) 105505]
Corrigendum to “A novel Cereblon E3 ligase modulator with antitumor activity in gastrointestinal cancer” [Bioorgan. Chem. 119 (2022) 105505]
Volume 146, May 2024, 107248Author links open overlay panelSvenja Lier a 1, Andreas Sellmer b 1, Felix Orben a, Stephanie ...
Structure-guided design of novel biphenyl-quinazoline derivatives as potent non-nucleoside reverse transcriptase inhibitors featuring improved anti-resistance, selectivity, and solubility
Structure-guided design of novel biphenyl-quinazoline derivatives as potent non-nucleoside reverse transcriptase inhibitors featuring improved anti-resistance, selectivity, and solubility
The global prevalence of acquired immunodeficiency syndrome (AIDS) has posed a significant threat to human over the past f...
Discovery of novel co-degradation CK1α and CDK7/9 PROTACs with p53 activation for treating acute myeloid leukemia
Discovery of novel co-degradation CK1α and CDK7/9 PROTACs with p53 activation for treating acute myeloid leukemia
TP53 is a tumor suppressor gene that encodes for the transcription factor p53. It plays important functions throughout hum...
Design, synthesis, in silico and biological evaluation of new indole based oxadiazole derivatives targeting estrogen receptor alpha
Design, synthesis, in silico and biological evaluation of new indole based oxadiazole derivatives targeting estrogen receptor alpha
Breast cancer (BC) is a multifactorial disease that poses a significant threat to women’s health [1]. In 2023, an estimate...
N-Containing triterpenoid saponins from Mussaenda densiflora and identification of heinsiagenin A as a potent immunosuppressant
N-Containing triterpenoid saponins from Mussaenda densiflora and identification of heinsiagenin A as a potent immunosuppressant
Immune-mediated inflammatory diseases (IMIDs), which are characterized by heightened and unregulated inflammation, coupled...
Discovery of PXR agonists from Hypericum japonicum: A class of novel nonaromatic acylphloroglucinol-terpenoid adducts
Discovery of PXR agonists from Hypericum japonicum: A class of novel nonaromatic acylphloroglucinol-terpenoid adducts
Cholestasis is characterized by a disturbance of bile acids (BAs) formation and/or secretion leading to the intrahepatic a...
Bioisosteric replacement strategy leads to novel DNA gyrase B inhibitors with improved potencies and properties
Bioisosteric replacement strategy leads to novel DNA gyrase B inhibitors with improved potencies and properties
Bacterial infection poses a serious threat to human life due to its rapidly growing resistance to antibacterial drugs, whi...
Dual inhibition of oxidative phosphorylation and glycolysis to enhance cancer therapy
Dual inhibition of oxidative phosphorylation and glycolysis to enhance cancer therapy
Cancer cells require plentiful energy to keep up with the increasing demands for proliferation and division [1], thus, mit...
Targeted genetic and small molecule disruption of N-Ras CaaX cleavage alters its localization and oncogenic potential
Targeted genetic and small molecule disruption of N-Ras CaaX cleavage alters its localization and oncogenic potential
Volume 147, June 2024, 107316Author links open overlay panel, , , , , , , , , Highlights•N-Ras is mislocalized when its Ca...
PI3Kδ and mTOR dual inhibitors: Design, synthesis and anticancer evaluation of 3-substituted aminomethylquinoline analogues
PI3Kδ and mTOR dual inhibitors: Design, synthesis and anticancer evaluation of 3-substituted aminomethylquinoline analogues
The PI3K/Akt/mammalian target of rapamycin (PI3K/Akt/mTOR, PAM) pathway has drawn significant pharmacological investment i...
Design and synthesis of novel imidazole-chalcone derivatives as microtubule protein polymerization inhibitors to treat cervical cancer and reverse cisplatin resistance
Design and synthesis of novel imidazole-chalcone derivatives as microtubule protein polymerization inhibitors to treat cervical cancer and reverse cisplatin resistance
Cervical cancer is one of the most common malignant tumors in women worldwide [1]. Human papillomavirus (HPV) is the main ...
阅读更多
format_indent_increase