title: Four-membered heterocycles-containing 4-anilino-quinazoline derivatives as epidermal growth factor receptor (EGFR) kinase inhibitors.
abstract: We report herein the design and synthesis of novel azaspirocycle or azetidine substituted 4-anilinoquinazoline derivatives. The EGFR inhibitory activities and in vitro antitumor potency of these newly synthesized compounds against two lung cancer cell lines HCC827 and A549 were evaluated. Most of the target compounds possess good inhibitory potency. In particular, compounds 21g with 2-oxa-6-azaspiro[3.4]octane substituent was found to possess higher EGFR inhibitory activities and similar antitumor potency comparing to the lead compound gefitinib with improved water solubility.
authors: School of Pharmacy, Fudan University, Shanghai 201203, PR China.
authors: Feng
authors: F
authors: Zhao
authors: Zhaohu
authors: Z
authors: Lin
authors: Feng
authors: F
authors: Wang
authors: Weili
authors: W
authors: Zhao
authors: Xiaochun
authors: X
authors: Dong
mesh_terms: D001372:Aza Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001384:Azetidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004789:Enzyme Activation / Q000187:drug effects; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D000077156:Gefitinib; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D001372:Aza Compounds; D001384:Azetidines; D006571:Heterocyclic Compounds; D011799:Quinazolines; C082735:azetidine; D066246:ErbB Receptors; D000077156:Gefitinib
keywords: Anilinoquinazolines; Anti-tumor agents; EGFR inhibitors; Four-membered heterocycles