32884-52-9Relevant academic research and scientific papers
Synthesis, Antiproliferative and Cytotoxic Activities, DNA Binding Features and Molecular Docking Study of Novel Enamine Derivatives
Burcu Gürdere, Meliha,Aydin, Ali,Yencilek, Belk?z,Ertürk, Fatih,?zbek, O?uz,Erkan, Sultan,Budak, Yakup,Ceylan, Mustafa
, (2020)
Novel enamine derivatives were synthesized from the reaction of lactone and chalcones and their antiproliferative and cytotoxic activities against six cancer cell lines (e. g., HeLa, HT29, A549, MCF7, PC3 and Hep3B) and one normal cell lines (e. g., FL) were investigated along with their mode of interactions with CT-DNA. Most of the enamine derivatives with IC50 values of 86–168 μM demonstrated much stronger antiproliferative activity than the starting molecules against the cancer cells. While, among the enamine derivatives, four compounds displayed higher cytotoxic potency than the control drugs (5-fluorouracil and cisplatin) against the Hep3B cell lines, these compounds did not exhibit any significant toxicity against normal cells, FL. The UV/VIS spectral data suggest that eight compounds cause hypochromism with a slight bathochromic shift (~6 nm), indicating that they bind to the DNA by way of an intercalative or minor groove binding mode. The binding constants of the compounds are in the range of 0.1×103 M?1–2.3×104 M?1. The antiproliferative activity of studied enamine derivatives could possibly be due to their DNA binding as well as their cytotoxic properties. In addition to these assays, the chalcones and enamine derivatives were investigated by molecular docking to calculate the synergistic effect of antiproliferative activities against six human cancer cell lines.
Synthesis and antimicrobial activity of azetidin-2-one containing pyrazoline derivatives
Shah, Shailesh H.,Patel, Pankqj S.
, p. 863 - 866 (2013/08/23)
Pyrazolines are well-known and important nitrogen containing 5-membered heterocyclic compounds and various methods have been worked out for their synthesis. A new series of 3-chloro-1-(4-[5-(substituted phenyl)-4,5-dihydro- pyrazol-3-yl]phenyl)-4-(4-cholo
Design, synthesis and in vitro antimalarial evaluation of new quinolinylhydrazone derivatives
Thuy, Le Thi,Tien, Hoang Xuan,Hoang, Vu Dinh,Vu, Tran Khac
scheme or table, p. 163 - 168 (2012/07/17)
A series of novel quinolinylhydrazones (5a-f) was synthesized by the condensation reaction of 2,6-diaryl-substituted piperidin-4-ones (4a-f) with 7-chloro-4-hydrazinoquinoline (2). Novel quinolinylhydrazones containing Shiff bases 8a-f and 11a-f were obta
Determination of latent transition temperatures of nonmesomorphs by extrapolation method in binary systems
Doshi,Bhoya,Travadi
body text, p. 10 - 15 (2012/05/04)
Eight binary systems consisting of mesomorphs and nonmesomorphs (A 1 or A2 + B1 B2, B7, B8) were studied with a view to determine the latent transition temperature (LTT) for the nonmesomorp
Chemoselectivity in reactions of an α-diazo-β-diketone with some conjugative double-bond systems
Xu,Zhang,Chen,Chen
, p. 2266 - 2268 (2007/10/03)
Reactions of 2-diazo-1,3-diphenylpropane-1,3-dione with α,β-unsaturated aldehydes and ketones, and keto-imines, in refluxing anhydrous toluene indicate that benzoyl(phenyl)ketene, which is generated by the thermal Wolff rearrangement of 2-diazo-1,3-diphen
Studies on Mixed Liquid Crystal. Part-I. Nemetic Mesophase induced by Mixing Two Non-liquid Crystalline Components and Determination of Latent Transition Temperature
Doshi, A.V.,Joshi, N.N.
, p. 807 - 810 (2007/10/02)
Eight binary systems consisting of both non-liquid crystalline components, viz. p-methoxyphenyl-p''-methoxy benzoate and Schiff base have been studied.One of the eight binary systems involving Schiff base p-tolual-p-phenetidine was found to give monotropi
Synthesis of Some New &β-Lactams, 4-Thiazolidinones and Pyrazolines
Fahmy, A. M.,Hassan, Kh. M.,Khalaf, A. A.,Ahmed, R. A.
, p. 884 - 887 (2007/10/02)
N-Arylidene-p-aminoacetophenone (I) and N-arylidene-4'-aminochalcones (V) have been converted into a series of substituted β-lactams (III) and 4-thiazolidinones (IV), and pyrazolines (VI, VII) respectively. p-Chloroacetamidoacetophenone (II) has also been converted into series of substituted 4'-piperidino/morpholinoacetoamidochalcones (X) which undergo cyclization on treatment with hydrazine, phenylhydrazine or thiourea to pyrazolines (XI, XII) and pyrimidine-2-thiones (XIII) respectively.The antibacterial and antifungal activities of the compounds have been determined.
