84023-76-7Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of new series of pyrrol-2(3H)-one and pyridazin-3(2H)-one derivatives as tubulin polymerization inhibitors
Abdelbaset, Mahmoud S.,Abdelrahman, Mostafa H.,Bukhari, Syed Nasir Abbas,Gouda, Ahmed M.,Youssif, Bahaa G.M.,Abdel-Aziz, Mohamed,Abuo-Rahma, Gamal El-Din A.
, (2020/12/21)
A potential microtubule destabilizing series of new thirty-five Pyrrol-2-one, Pyridazin-3(2H)-one and Pyridazin-3(2H)-one/oxime derivatives has been synthesized and tested for their antiproliferative activity against a panel of 60 human cancer cell lines. Compounds IVc, IVg and IVf showed a broad spectrum of growth inhibitory activity against cancer cell lines representing renal, cancer of lung, colon, central nervous system, ovary, and kidney. Among them, compound IVg was found to have broad spectrum anti-tumor activity against the tested nine tumor subpanels with selectivity ratios ranging between 0.21 and 3.77 at the GI50 level. In vitro assaying revealed tubulin polymerization inhibition by all active compounds IVc, IVg and IVf. The results of the docking study revealed nice fitting of compounds IVc, IVf, and IVg into CA-4 binding site in tubulin. The three compounds exhibited high binding affinities (ΔGb = ?12.49 to ?12.99 kcal/mol) toward tubulin compared to CA-4 (?8.87 kcal/mol). Investigation of the binding modes of the three compounds IVc, IVf, and IVg revealed that they interacted mainly hydrophobically with tubulin and similar binding orientations to that of CA-4. These observations suggest that tubulin is a possible target for these compounds.
Microwave assisted Perkin reaction for the synthesis of α-arylidine-γ-phenyl-Δ, β, γ-butenolides
Deo, Sujata,Chaudhari, Tanishq,Inam, Farhin
, p. 363 - 367 (2014/05/06)
Perkin condensation with subsequent intramolecular lactonisation as one pot synthesis of α-arylidine-γ-phenyl-Δ,β,γ- butenolides have been studied under microwave irradiation. The butenolides are cleaved to give keto acids, which are the precursors of pericarbonyl lactone lignans possessing variety of biological activities. Syntheses of butenolides have been carried out using pyridine as a catalyst under microwave conditions. The generality of this protocol has been demonstrated by synthesizing a variety of substituted butenolides in excellent yields, short reaction time and with good purity compared to those under classical thermal conditions. All the products have been characterized by their IR, 1H NMR and UV spectral values.
Synthesis of 1-phenyl naphthalene and pericarbonyl lignans
Deo, Sujata,Inam, Farhin,Mahashabde,Jadhav
experimental part, p. 3362 - 3368 (2010/11/16)
The approach towards synthesis of 1-phenyl naphthalene and pericarbonyl lactone by cyclization of Perkin condensation product, ∝- arylidene β-benzoyl propionic acid with polyphosphoric acid and concentrated sulphuric acid can be achieved in one step.
