Showing papers in "Bioorganic Chemistry in 2022"

TL;DR: In this paper , a series of new thiazolo-indolin-2-one derivatives were synthesized based on acid and base catalyzed condensation or reaction of thiosemicarbazone 8 with different electrophilic reagents.

TL;DR: In this article , a novel type of coumarin thiazoles as unique multi-targeting antimicrobial agents were developed through four steps including cyclization, nucleophilic substitution and condensation starting from commercial resorcine.

TL;DR: In this paper , a series of 4-methoxyphenyl pyrazole and pyrimidine derivatives were designed and synthesized as dual EGFR/VEGFR-2 inhibitors.

TL;DR: The 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivatives 13-22 have been developed as dual EGFR and BRAFV600E inhibitors as discussed by the authors .

TL;DR: In this paper , the antiviral activity of two compounds, Thymohydroquinone and Dithymoquinone, which are synthesized through simple chemical procedures, deriving from ThymoQuinone, a major compound of Nigella sativa.

TL;DR: In this article , a series of chalcone based coumarin derivatives (23a-h) was designed, subjected to in-silico ADMET prediction, synthesized, characterized by IR, NMR, Mass analytical techniques and evaluated as acetylcholinesterase (AChE) inhibitor for the treatment of Alzheimer's disease (AD).

TL;DR: In this paper , the authors reported the synthesis of a new set of suggested anticancer molecules by joining the 1,2,3-triazole and chalcone privileged fragments in one scaffold to develop novel candidates in leukemia therapy.

TL;DR: In this article , the authors synthesize heterocyclic compounds containing indole, 1,2,4-triazole, and glycosyl or allyl moieties.

TL;DR: In this paper , a series of benzo[b]azonin-2-one derivatives having the same pharmacophoric features as colchicine binding site inhibitors (CBSIs) were synthesized targeting the CBS of β-tubulin.

TL;DR: A recent review as discussed by the authors covers the past decade (2010-2020) research, considering selective as well as potent inhibitors of tumor associated isoforms, hCA IX and hCA XII, which include newer generation inhibitors containing sulfonamides or their bioisosteres, non-classical inhibitors (including carboxylic acid/ester, coumarin and sulfocoumarin classes) and various other novel classes of inhibitors belonging to newly identified chemotypes/scaffolds.

TL;DR: In this paper , an overview of type 2 diabetes; biology of protein tyrosine phosphatase 1B; role of PTP1B in metabolic disorders; and recent updates in the development of PTT1B inhibitors reported in literature since 1994 are discussed.

TL;DR: In this article , the authors reviewed the processes for the initiation of inflammation and the treatment measures, focusing on the cyclooxygenase mediated arachidonic acid metabolic pathways, biochemistry of inflammatory prostaglandins and data corresponding to efficacy, pharmacokinetic profile and the side effects of the available natural and synthetic anti-inflammatory drugs.

TL;DR: A series of chiral and achiral cyclic seleno-and thiourea compounds bearing benzyl groups on N-atoms were prepared from enetetramines and appropriate Group VI elements in good yields as mentioned in this paper .

TL;DR: In this article , a metronidazole-derived three-component hybrid was developed as promising antibacterial therapeutic alternatives to suppress the growth of drug-resistant E. coli (MIC = 0.5 µg/mL).

TL;DR: In this article , a review article on Alzheimer's disease (AD) is presented, which covers all probable mechanisms including lipid dyshomeostasis, pathogenic involvement of P. gingivalis and neurovascular dysfunction, recently reported molecules and drugs under clinical investigations and approved by FDA for AD treatment.

TL;DR: In this paper , the authors reported the discovery of Dacomitinib-based EGFR degraders, which can effectively induce degradation of EGFRdel19 with DC50 value of 3.57 nM in HCC-827 cells, but not to other EGFR mutant, wild-type EGFR protein and the same family receptors.

TL;DR: In this paper , a series of pyrimido[5,4-c]quinoline derivatives variously substituted at positions 2 and 5 have been synthesized, in good to excellent yields, via rapid base-catalyzed cyclization reaction of 2,4dichloroquinoline-3-carbonitrile (5) with guanidine hydrochlorides 6a-c.

TL;DR: In this article , hydrazonoyl-sulfonyl-ethylidene derivatives were designed and synthesized as EGFR inhibitors, which revealed marked inhibitory activity against EGFR kinase having IC50 range from 0.037 to 0.317.

TL;DR: Aloe emodin-conjugated sulfonyl hydrazones (AEBH-5a) was designed and synthesized as novel type of antibacterial modulators as mentioned in this paper .

TL;DR: In this article , a series of pyrazoline compounds were designed and synthesized as antiproliferative agents by VEGFR pathway inhibition, and all synthesized compounds were screened by the National Cancer Institute (NCI), Bethesda, USA for anticancer activity against 60 human cancer cell lines.

TL;DR: Ganoresinoid A showed notably restrained nitric oxide (NO), IL-1β, IL-6 and TNF-α levels in LPS-activated BV-2 microglial cells via suppressing TLR-4/NF-κB and MAPK signaling pathway as discussed by the authors .

TL;DR: In this article , a set of ibuprofen-quinoline conjugates comprising quinolinyl heterocycle and ibuproxen moieties linked by an alkyl chain were synthesized in good yields utilizing an optimized reaction procedure in a molecular hybridization approach to overcome the drawbacks of the current non-steroidal anti-inflammatory drugs.

TL;DR: In this article , the authors reviewed the chemical structures, anti-inflammatory activities, and mechanisms of action of 281 terpenoid natural products reported from 2010 to the present, and both in vitro and in vivo screening models were also surveyed and statistically summarized.

TL;DR: In this paper, a series of pyrazoline compounds were designed and synthesized as antiproliferative agents by VEGFR pathway inhibition, and all synthesized compounds were screened by the National Cancer Institute (NCI), Bethesda, USA for anticancer activity against 60 human cancer cell lines.

TL;DR: In this article, mesoporous silica nanoparticles (MNs) were synthetized and submitted to single and/or dual loading of antibiotics (ofloxacin- OFLO) and anticancer drugs (Doxorubicin- DOX; EpirubicIN- EPI), and investigated regarding their antibacterial activity against Escherichia coli, Staphylococcus aureus, methicillin-resistant S. aUREus (MRSA), Enterococcus faecalis and Pseudomonas aerug

TL;DR: In this paper , the synthesis of novel neolignans-celecoxib hybrids and the evaluation of their biological activity were reported, and the analogs8-13(L13-L18) exhibited anti-inflammatory activity, inhibited glycoprotein expression (P-selectin) related to platelet activation, and were considered non- ulcerogenic in the animal model.

TL;DR: In this paper , small molecule FLT3 degraders based on the proteolysis targeting chimera (PROTAC) were designed, synthesized, and evaluated for FLT 3 degradation.

TL;DR: In this paper , mesoporous silica nanoparticles (MNs) are used for single and/or dual loading of antibiotics (ofloxacin - OFLO) and anticancer drugs (Doxorubicin - DOX; Epirubicincin - EPI) against resistant bacteria with a positive effect even at very low concentrations.

TL;DR: In this article , the spirooxindole scaffold derived from FY-56 was used to design structurally new LSD1 inhibitors for treating human diseases, which showed high selectivity over monoamine oxidases (MAO-A/B).

TL;DR: Proteolysis-targeting chimeras (PROTACs) have been developed to hijack the ubiquitin-proteasome system (UPS) to induce different POIs degradation as mentioned in this paper .