199114-62-0Relevant articles and documents
Synthesis and preliminary structure-activity relationship study of 3-methylquinazolinone derivatives as EGFR inhibitors with enhanced antiproliferative activities against tumour cells
Zhang, Yan,Wang, Qin,Li, Luolan,Le, Yi,Liu, Li,Yang, Jing,Li, Yongliang,Bao, Guochen,Yan, Longjia
, p. 1205 - 1216 (2021)
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
Design, synthesis and in vitro biological evaluation of quinazolinone derivatives as EGFR inhibitors for antitumor treatment
Fu, Yihong,Gan, Yiyuan,Le, Yi,Li, Wen,Liu, Jiamin,Ouyang, Guiping,Wang, Zhenchao,Yan, Longjia,Zhou, Zhixu,Zou, Xue
, p. 555 - 564 (2020)
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
Synthesis of benzoxazolthiolyl and benzthiazolthiolyl fused 3- alkylquinazolin-4(3H)-ones
Rafeeq, Md.,Reddy, Ch. Venkata Ramana,Dubey
, p. 405 - 410 (2019/01/21)
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.