The versatility of multicomponent Biginelli’s reaction is exploited in the development of proline and cyclized cysteine tethered conjugates of monastrol, a kinesin Eg5 inhibitor.
M Shaheer Malik +2 more
exaly +4 more sources
Kinesin-5 inhibition improves neural regeneration in experimental autoimmune neuritis [PDF]
Background Autoimmune neuropathies can result in long-term disability and incomplete recovery, despite adequate first-line therapy. Kinesin-5 inhibition was shown to accelerate neurite outgrowth in different preclinical studies.
Felix Kohle +9 more
doaj +2 more sources
Mitotic slippage and expression of survivin are linked to differential sensitivity of human cancer cell-lines to the Kinesin-5 inhibitor monastrol. [PDF]
The mitotic Kinesin-5 motor proteins crosslink and slide apart antiparallel spindle microtubules, thus performing essential functions in mitotic spindle dynamics.
Hila Asraf +3 more
doaj +2 more sources
Aryl-Substituted Dihydro-Pyrimidines Effecting Kinesin Eg5 as Novel Approach for Cancer Treatment [PDF]
Cancer is one of the most lethal diseases of this century. Unfortunately, many anticancer agents have harsh side effects or fail to work against cancer any longer due to tolerance.
Dialekti Chlorou, Eleni Pontiki
doaj +2 more sources
The pterocarpan (+)-PTC modulates cytoskeletal proteins and induces apoptosis in metastatic castration-resistant prostate cancer: a proteomic perspective [PDF]
Treatment of metastatic, castration-resistant prostate cancer (mCRPC) remains clinically challenging due to tumor heterogeneity and resistance to standard microtubule-targeting agents, such as docetaxel and cabazitaxel.
José de Brito Vieira Neto +23 more
doaj +2 more sources
Design, synthesis and docking study of 3,4-dihydropyrimidine-2-one derivatives as inhibitors of the Mitotic Kinesin, Eg5 [PDF]
A series of 3,4-dihydropyrimidine-2-one derivatives were designed and synthesized as monastrol analogs by Biginelli cyclocondensation of a β-keto compounds and aromatic aldehyde with urea or thiourea.
Hossein Sadeghpour +4 more
doaj +1 more source
Kinesin-5 motors are required for organization of spindle microtubules in
Background Monastrol, a chemical inhibitor specific to the Kinesin-5 family of motor proteins, was used to examine the functional roles of Kinesin-5 proteins during the first, asymmetric cell division cycle in the brown alga Silvetia compressa.
Kropf Darryl L, Peters Nick T
doaj +1 more source
Breast cancer and gliobalstoma are the most aggressive types of diseases causing serious health issues. Potent anticancer molecules are facing serious side effects which arouse the need for newer molecules with significant clinical efficacy and safety ...
Dhirajkumar Nikam, Anurekha Jain
doaj +1 more source
Recent progress in biological activities of dihydropyrimidine derivatives: An updated mini-review [PDF]
Dihydropyrimidines (DHPMs) are a class of nitrogen-containing heterocycles that have attracted considerable interest due to their great significance in organic and medicinal chemistry.
Ali Elshamsy +3 more
doaj +1 more source
Monastrol Synthesis Using Subcritical EtOH: Response Surface Method for Optimization [PDF]
Monastrol is an Eg5 inhibitor that induces mitotic arrest and apoptosis. The efficiency of the Biginelli reaction for Monastrol synthesis can be enhanced by utilizing a subcritical EtOH.
Yousuf Karimi +3 more
doaj +1 more source

