14755-69-2Relevant academic research and scientific papers
Synthesis and cytotoxic evaluation of some cyclic arylidene ketones and related oximes, oxime esters, and analogs
Dimmock,Sidhu,Chen,Li,Quail,Allen,Kao
, p. 852 - 858 (1994)
A number of arylidene derivatives of alicyclic ketones and some corresponding oximes, oxime esters, and related compounds were prepared as candidate cytotoxic agents. All of the compounds were evaluated against murine L1210 lymphoid leukemia cells. In general, cytotoxicity was greatest with the α,β-unsaturated ketones and diminished with the oximes, and the oxime esters had little or no activity in this screen. When the same compounds were examined in both the in vitro L1210 and P388 leukemia screens, in the majority of cases the L1210 cells were more sensitive to these derivatives. Over half of the compounds prepared were evaluated against approximately 55 human tumors in vitro and showed selective toxicity toward one or more groups of neoplastic diseases, particularly leukemia. Some correlations between structure and bioactivity were discerned. The cytotoxicity screening and stability studies of representative compounds suggested that the ketones, oximes, and oxime esters were stable under the conditions of bioevaluation. X-ray crystallography of four representative compounds revealed structural features associated with cytotoxicity which may be considered in the design of future candidate cytotoxins.
Synthesis and biological activities of some new C-Aminomethylation of 5H-5-Aryl-6,7,8,9-tetrahydrothiazolo[2,3-b]quinazolin-3(2H)-one and 6H-6-Aryl-2,3,7,8,9,10-hexahydrothiazino[2,3-b]quinazolin-4(3H)-one
Kumaraswamy, Damerakonda,Mallareddy
, p. 2231 - 2235 (2016/07/21)
The synthesis of 5H-5-aryl-6,7,8,9-tetrahydrothiazolo[2,3-b]quinazolin-3(2H)-one and 6H-6-aryl-2,3,7,8,9,10-hexahydrothiazino[2,3-b]quinazolin-4(3H)-one, reaction between 4-aryl-3,4,5,6,7,8-hexahydroquinazolin-2-thione and methyl chloroacetate and ethyl β-bromo propionate. The Mannich reaction on 5H-5-aryl-6,7,8,9-tetrahydrothiazolo[2,3-b]quinazolin-3(2H)-one and 6H-6-aryl-2,3,7,8,9,10-hexahydrothiazino[2,3-b]quinazolin-4(3H)-one in ethanol, aqueous formaldehyde and different secondary amines yielded a single product C-Mannich base in each case. The obtained C-Mannich bases (compounds VIII and X) have been characterized on the basis of analytical spectral data. These C-Mannich bases have been screened for their antibacterial, antifungal, anti-inflammatory and analgesic activities.
One-pot synthesis of 2-morpholino-4-phenylbicyclononanones
Ravishankar, Lakshmy,Trivedi, Girish Kumar
, p. 303 - 307 (2007/10/02)
Condensation of 1-morpholinocyclohexene with cinnamaldehyde in the presence of either Eu(fod)3 or CeCl3 gives 2-morpholino-4-phenylbicyclononan-9-one (4) as the major product.Three other minor products formed in the CeCl3 catalysed reaction have been isolated by column chromatography using pyridine deactivated silica gel as the adsorbent.The CeCl3 catalysed condensation has also been extended to the one-pot synthesis of bicyclic compounds 4a-e and 5.
