- Novel 2,4- thiazolidinediones: Synthesis, in?vitro cytotoxic activity, and mechanistic investigation
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Two thiazolidinedione scaffolds different in the position of the thiazolidinedione ring in the molecule were tested for in?vitro cytotoxic activity in a panel of human cancer cell lines namely, prostate cancer cells PC-3, breast carcinoma cells MDA-MB-231
- Metwally, Kamel,Pratsinis, Harris,Kletsas, Dimitris
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p. 340 - 350
(2017/04/13)
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- Design, synthesis and evaluation of novel 2-thiophen-5-yl-3H-quinazolin-4-one analogues as inhibitors of transcription factors NF-k{cyrillic}B and AP-1 mediated transcriptional activation: Their possible utilization as anti-inflammatory and anti-cancer ag
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In an attempt to discover novel inhibitors of NF-κB and AP-1 mediated transcriptional activation utilizing the concept of chemical lead based medicinal chemistry and bioisosterism a series of 2-(2,3-disubstituted-thiophen-5-yl)-3H-quinazolin-4-one analogs
- Giri, Rajan S.,Thaker, Hardik M.,Giordano, Tony,Williams, Jill,Rogers, Donna,Vasu, Kamala K.,Sudarsanam, Vasudevan
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experimental part
p. 2796 - 2808
(2010/07/06)
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- Synthesis of novel new 2-(2-(4-((3,4-dihydro-4-oxo-3-aryl quinazolin-2-yl)methyl)piperazin-1-yl)acetoyloxy)-2-phenyl acetic acid esters
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Stereoselective diazotization of (S)-2-amino-2-phenyl acetic acid (L-phenyl glycine) (4) with NaNO2 in 6% H2SO4 in a mixture of acetone and water gave optically pure (S)-2-hydroxy-2-phenyl acetic acid (L-mandelic acid) (5). Esterification, gave (S)-2-hydroxy-2-phenyl acetic acid esters (6). The latter was treated with chloroacetyl chloride in the presence of triethylamine (TEA) in dichloromethane (DCM) to yield (S)-2-chloroacetyloxy phenyl acetic acid ester (2). In another sequence, the reaction of 2-(chloromethyl)-3-arylquinazolin- 4(3H)-one (9) treated with N-Boc piperazine, followed by deprotection of the Boc group, to obtain 3-aryl-2-((piperazin-1-yl)methyl) quinazolin-4(3H)-one (3). Reaction of 2 with 3 in the presence of K2CO3 and KI gave the title compound, 2-(2-(4-((3,4-dihydro-4-oxo-3-arylquinazolin-2-yl)methyl)piperazin-1-yl) acetoyloxy)-2-phenyl acetic acid esters (1). The structures of all the new compounds obtained in the present work are supported by spectral and analytical data. Copyright Taylor & Francis Group, LLC.
- Acharyulu, Palle V. R.,Dubey,Reddy, P. V. V. Prasada,Suresh, Thatipally
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p. 3217 - 3231
(2011/03/17)
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- THIAZOLE AND THIOPHENE ANALOGUES, AND THEIR USE IN TREATING AUTOIMMUNE DISEASES AND CANCERS
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Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.
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Page/Page column 46
(2008/06/13)
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- Quinazolinones, 2. Syntheses and Some Reactions of 2-Azido-methyl-3-aryl-4-quinazolinones
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Starting with the chloromethyl compounds 7 the new 2-azidomethyl-3-aryl-4-quinazolinones 8a-h were prepared, some of which have been reduced so far to the corresponding amines 9a, b, e, g by H2S in good yield.As a first example for the capability of the a
- Domanig, Rainer
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p. 1195 - 1202
(2007/10/02)
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