1594880-73-5Relevant academic research and scientific papers
Design, synthesis and drug resistance reversal potential of novel curcumin mimics Van D: Synergy potential of curcumin mimics
Raj Dwivedi, Gaurav,Khwaja, Sadiya,Singh Negi, Arvind,Panda, Swati S.,Swaroop Sanket,Pati, Sanghamitra,Chand Gupta, Amit,Bawankule, Dnyaneshwar Umrao,Chanda, Debabrata,Kant, Rajni,Darokar, Mahendra P.
, (2021)
Being crucial part of plant-based novel discovery of drug from natural resources, a study was done to explore the antibacterial potential of curcumin mimics in combination with antibiotics against multidrug resistant isolates of Pseudomonas aeruginosa. Th
Antiproliferative efficacy of curcumin mimics through microtubule destabilization
Khwaja, Sadiya,Fatima, Kaneez,Hassanain,Behera, Chittaranjan,Kour, Avneet,Singh, Arjun,Luqman, Suaib,Sarkar, Jayanta,Chanda, Debabrata,Shanker, Karuna,Gupta,Mondhe,Negi, Arvind S.
, p. 51 - 61 (2018/04/05)
Curcumin possesses an attractive chemical structure with highly conjugated diferuloylmethane core. Curcumin mimics have been designed and prepared with an additional bridged phenyl ring in conjugation. Fourteen diverse analogues were evaluated against a p
Synthesis, biological evaluation and 3D-QSAR studies of new chalcone derivatives as inhibitors of human P-glycoprotein
Parveen, Zahida,Brunhofer, Gerda,Jabeen, Ishrat,Erker, Thomas,Chiba, Peter,Ecker, Gerhard F.
, p. 2311 - 2319 (2014/04/17)
P-glycoprotein (P-gp) is an ATP-dependent multidrug resistance efflux transporter that plays an important role in anticancer drug resistance and in pharmacokinetics of medicines. Despite a large number of structurally and functionally diverse compounds, also flavonoids and chalcones have been reported as inhibitors of P-gp. The latter share some similarity with the well studied class of propafenones, but do not contain a basic nitrogen atom. Furthermore, due to their rigidity, they are suitable candidates for 3D-QSAR studies. In this study, a set of 22 new chalcone derivatives were synthesized and evaluated in a daunomycin efflux inhibition assay using the CCRF.CEM.VCR1000 cell line. The compound 10 showed the highest activity (IC50 = 42 nM), which is one order of magnitude higher than the activity for an equilipohillic propafenone analogue. 2D- and 3D-QSAR studies indicate the importance of H-bond acceptors, methoxy groups, hydrophobic groups as well as the number of rotatable bonds as pharmacophoric features influencing P-gp inhibitory activity.
