7058-73-3Relevant academic research and scientific papers
Synthesis and biological evaluation of new curcumin analogues as antioxidant and antitumor agents: Molecular modeling study
Bayomi, Said M.,El-Kashef, Hassan A.,El-Ashmawy, Mahmoud B.,Nasr, Magda N.A.,El-Sherbeny, Magda A.,Abdel-Aziz, Naglaa I.,El-Sayed, Magda A.-A.,Suddek, Ghada M.,El-Messery, Shahenda M.,Ghaly, Mariam A.
, p. 584 - 594 (2015)
New curcumin analogues have been synthesized and their antioxidant activities were investigated by measuring their free radical scavenging capacities. The in vitro and in vivo antitumor activities of the synthesized compounds on Ehrlich ascites carcinoma (EAC) cell line were evaluated. 4-(4-Chlorophenyl)-2-(5-ethyl-7-(4-methoxybenzylidene)-3-(4-methoxyphenyl)-3,3a,4,5,6,7-hexahydro-2H-pyrazolo[4,3-c] pyridin-2-yl)thiazole 7h showed excellent antineoplastic activity in both in vitro and in vivo studies more than that of tested compounds and reference drug, cisplatin. Different molecular modeling studies were performed, where docking of compound 7h into telomerase active site suggested that it could exert its antitumor potential by telomerase inhibition.
CURCUMIN ANALOGS AND METHODS OF MAKING AND USING THEREOF
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Page/Page column 65; 75; 76, (2014/02/16)
Compounds having Formula I or II, and methods of making and using thereof, are described herein:
Substituted thiazoles V. Synthesis and antitumor activity of novel thiazolo[2,3-b]quinazoline and pyrido[4,3-d]thiazolo[3,2-a]pyrimidine analogues
Al-Omary, Fatmah A.M.,Hassan, Ghada S.,El-Messery, Shahenda M.,El-Subbagh, Hussein I.
scheme or table, p. 65 - 72 (2012/02/15)
A novel series of thiazolo[2,3-b]quinazoline (14-23, 26 and 27), and pyrido[4,3-d]thiazolo[3,2-a]pyrimidine (34-43, 45 and 46) analogues were designed and synthesized. The obtained compounds were evaluated for their in-vitro antitumor activity at the National Cancer Institute (NCI) 60 cell lines panel assay. Compounds 22, 38, 40 and 41 showed remarkable broad-spectrum antitumor activity. Compounds 22 and 38 are almost nine fold more active than 5-FU, with GI50, TGI, and LC50 values of 2.5, >100, >100; and 2.4, 9.1, 36.2 μM, respectively; while 40 and 41 are almost seven fold more active than 5-FU, with GI50, TGI, and LC50 values of 2.9, 12.4, 46.6 and 3.0, 16.3, 54.0 μM, respectively.
Synthesis of polysubstituted 1,4-diazacycloheptan-5-ones. 1. Synthesis and conformational investigation of polysubstituted 4-piperidones
Vatsadze,Krainova,Kovalkina,Zyk
, p. 1185 - 1191 (2007/10/03)
A series of tri- and tetrasubstituted 4-piperidones and their bicyclic analogs has been synthesized. It was established by 1H NMR spectroscopy that all the piperidones obtained have the chair conformation in solution with equatorially disposed
