Kinesin-5 inhibitörü olan Monastrol bileşiğinin sentezi ve yük transferi kompleks etkileşmelerinin incelenmesi [PDF]
Kinesin-5 inhibitörü olarak kullanılan Monastrol, çözücüsüz ortamda alümina sülfonik asit (ASA) katalizörü varlığında 3-hidroksibenzaldehit, tiyoüre ve etilasetoasetat kullanılarak sentezlenmiştir.
Mustafa Arslan, Nurcan Berber
doaj +3 more sources
Monastrol disrupts KIFC1-ATP dynamics: Towards newer anticancer mechanism
Mitotic kinesins are eukaryotic proteins that play a vital role in cellular mitosis. Their over-expression in malignant rather than normal cells and their specific cellular role made kinesin inhibitors a promising cancer therapeutics.
Musab Ali +2 more
doaj +2 more sources
Catalyzed and non-catalyzed synthesis of bioactive monastrol [PDF]
The bioactive 3,4-dihydropyrimidin-2(1H)-thione derivative known as Monastrol was synthesized under catalyzed and non-catalyzed conditions through the Biginelli multicomponent reaction under solvent-free conditions.
Haline G. O. Alvim +4 more
doaj +2 more sources
Monastrol derivatives: in silico and in vitro cytotoxicity assessments [PDF]
Background and purpose: Cancer is the leading cause of death in today’s world, therefore the efforts to achieve anticancer drugs with higher potency and fewer side effects have always been conducted by researchers in the field of pharmaceutical chemistry.
Zahra Bidram +6 more
doaj +2 more sources
In this paper, we describe a practical route for the synthesis of Biginelli compounds using In(OTf)3. To study the generality of this catalyst, several examples using aromatic aldehydes, 1,3-dicarbonyl compounds, urea, and thiourea were investigated. The
Marla N. Godoi +5 more
doaj +2 more sources
Multigram-Scale Organic Synthesis by Resonant Acoustic Mixing: Application to the Sustainable Preparation of Active Pharmaceutical Ingredients. [PDF]
Knoevenagel condensation, Biginelli three‐component reaction and benzylic rearrangement are investigated at multi‐gram scale, by resonance acoustic mixing (RAM), to prepare biologically active molecules, also including the marketed Phenytoin (antiepileptic drug). Chem21 and DOZN 3.0 tools were used to assess the greenness of the RAM‐assisted syntheses,
Chatzigiannis CM +3 more
europepmc +2 more sources
PB2382: EFFECTS OF ANTIFASCIN COMPOUNDS AGAINST LYMPHOMA CELLS IN VITRO [PDF]
HemaSphere, Volume 7, Issue S3, August 2023.
María Hurtado López A +10 more
europepmc +2 more sources
Morphological Profiling Identifies the Motor Protein Eg5 as Cellular Target of Spirooxindoles
Functional group‐controlled, RhIII‐catalyzed scaffold‐divergent synthesis of spirooxindole–isooxindoles and spirooxindole–oxindoles in combination with unbiased morphological bioactivity profiling reveal a unique Eg5 inhibitor chemotype. Abstract Oxindoles and iso‐oxindoles are natural product‐derived scaffolds that provide inspiration for the design ...
Jie Liu +13 more
wiley +2 more sources
Tetraploidy‐linked sensitization to CENP‐E inhibition in human cells
Tetraploidy arising through whole‐genome duplication is a cancer hallmark. Inhibitors of a mitotic kinesin CENP‐E preferentially suppress tetraploid cells over diploid counterparts with superior generality across different cellular backgrounds. Comparative imaging reveals tetraploidy‐linked aggravation of chromosome misalignment, mitotic delay ...
Koya Yoshizawa +14 more
wiley +1 more source
Hypoxia‐Induced FUS–circTBC1D14 Stress Granules Promote Autophagy in TNBC
FUS‐circTBC1D14‐associated stress granules (SGs) are transferred to the cytoplasm after being modified by PRMT1 and circTBC1D14 increases the stability of PRMT1 by inhibiting its K48‐regulated polyubiquitination. Then FUS‐circTBC1D14 can initiate a cascade of SGs‐linked proteins to control the elimination of SGs by recruiting LAMP1. The findings reveal
Ying Liu +13 more
wiley +1 more source

