- Synthesis and preliminary structure-activity relationship study of 3-methylquinazolinone derivatives as EGFR inhibitors with enhanced antiproliferative activities against tumour cells
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In this paper, a set of 3-methylquniazolinone derivatives were designed, synthesised, and studied the preliminary structure-activity relationship for antiproliferative activities. All target compounds performed significantly inhibitory effects against wil
- Zhang, Yan,Wang, Qin,Li, Luolan,Le, Yi,Liu, Li,Yang, Jing,Li, Yongliang,Bao, Guochen,Yan, Longjia
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- Design, synthesis, biological activities and 3D-QSAR studies of quinazolinone derivatives containing hydrazone structural units
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In this study, three series of quinazolinone derivatives containing hydrazone structures were designed and synthesized. Bioactivity assays indicated that these compounds showed good antitumour activities towards human lung cancer cells (A549) and human pr
- Shao, Li-Hui,Fan, Si-Li,Meng, Ying-Fen,Gan, Yi-Yuan,Shao, Wu-Bin,Wang, Zhen-Chao,Chen, Dan-Ping,Ouyang, Gui-Ping
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- Design, synthesis and in vitro biological evaluation of quinazolinone derivatives as EGFR inhibitors for antitumor treatment
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In this paper, a series of novel 3-methyl-quinazolinone derivatives was designed, synthesised and evaluated for antitumor activity in vitro on wild type epidermal growth factor receptor tyrosine kinase (EGFRwt-TK) and three human cancer cell li
- Fu, Yihong,Gan, Yiyuan,Le, Yi,Li, Wen,Liu, Jiamin,Ouyang, Guiping,Wang, Zhenchao,Yan, Longjia,Zhou, Zhixu,Zou, Xue
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Read Online
- Quinazolinone compound containing hydrazone structural unit or stereoisomer, salt or solvate of the quinazolinone compound
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The invention relates to a quinazolinone compound containing a hydrazone structural unit, or a stereoisomer, or a salt or a solvate of the quinazolinone compound. The compound has a structure as shownin a general formula (I) shown in the specification. Th
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- Synthesis of benzoxazolthiolyl and benzthiazolthiolyl fused 3- alkylquinazolin-4(3H)-ones
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Condensation of anthranilamide (1) with chloroacetyl chloride for 1 hr at RT gave 2- (2-chloroacetamido) benzamide (2). The latter, on refluxation in acetic acid for 2 hr gave 2-(chloromethyl) quinazolin-4(3H)-one (3). Condensation of 3, independently, with each one of benz [d] oxazole-2-thiol (4a) and benz [d] thiazole-2-thiol (4b), for 3-4 hr, gave 2-((benz [d] oxazol-2-ylthio) methyl) quinazolin-4(3H)-one (5a) and 2-((benz [d] thiazol-2-ylthio) methyl) quinazolin-4(3H)-one (5b) respectively. Each one of the 5a and 5b, independently and selectively, when treated with alkylating agents (i.e. DMS, DES, PhCH2Cl), gave 2-((benz [d] oxazol-2-ylthio) methyl)-3-alkylquinazolin-4(3H)-ones (6a-c) and 2-((benz [d] thiazol-2-ylthio) methyl)-3-alkylquinazolin-4(3H)-ones (6d-f) respectively. The latter 6a-f could also be prepared, alternatively, by condensing chloromethyl-3-alkylquinazolin-4(3H)-one (7a-c) with 4a-b respectively, in good yields.
- Rafeeq, Md.,Reddy, Ch. Venkata Ramana,Dubey
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p. 405 - 410
(2019/01/21)
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- Microwave-assisted synthesis in aqueous medium of new quinazoline derivatives as anticancer agent precursors
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Fast and eco-friendly microwave-irradiated reactions permitting the "green synthesis" of new 2-substituted quinazoline derivatives in aqueous medium via S-alkylation or SRN1 reaction from 2-chloromethyl-3-methylquinazolin-4(3H)-one derivatives with different benzenesulfinic acids and nitronate anions, are reported herein.
- Kabri,Gellis,Vanelle
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experimental part
p. 201 - 208
(2010/04/22)
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- Therapeutic uses of tri-aryl acid derivatives
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The use of triaryl acid derivatives of formula (I) and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.
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Page/Page column 220
(2010/10/20)
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- 4-heteryl-β-lactams : A facile synthesis of 1-aryl-4- [isopropylideneamino/methyl-4(3H)-oxoquinazolin-2-yl] azetidin-2-ones
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A facile and efficient synthesis of 4-quinazolinonyl-β-lactams 9 and 10 starting from 2-chloromethylquinazolin-4(3H)-ones 1 is reported.
- Reddy,Vasantha,Naga Raju
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