title: A general synthetic procedure for 2-chloromethyl-4(3H)-quinazolinone derivatives and their utilization in the preparation of novel anticancer agents with 4-anilinoquinazoline scaffolds.
abstract: In our ongoing research on novel anticancer agents with 4-anilinoquinazoline scaffolds, a series of novel 2-chloromethyl-4(3H)-quinazolinones were needed as key intermediates. An improved one-step synthesis of 2-chloromethyl-4(3H)-quinazolinones utilizing o-anthranilic acids as starting materials was described. Based on it, 2-hydroxy-methyl-4(3H)-quinazolinones were conveniently prepared in one pot. Moreover, two novel 4-anilinoquinazoline derivatives substituted with chloromethyl groups at the 2-position were synthesized and showed promising anticancer activity in vitro.
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medicinal School, Sichuan University, Chengdu 610041, China.
authors.forename: Hong-Ze
authors.initials: HZ
authors.lastname: Li
authors.forename: Hai-Yun
authors.initials: HY
authors.lastname: He
authors.forename: Yuan-Yuan
authors.initials: YY
authors.lastname: Han
authors.forename: Xin
authors.initials: X
authors.lastname: Gu
authors.forename: Lin
authors.initials: L
authors.lastname: He
authors.forename: Qing-Rong
authors.initials: QR
authors.lastname: Qi
authors.forename: Ying-Lan
authors.initials: YL
authors.lastname: Zhao
authors.forename: Li
authors.initials: L
authors.lastname: Yang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D056945:Hep G2 Cells; D006801:Humans; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D011799:Quinazolines