New derivatives of quinazoline and 1, 2-dihydroquinazoline n3-oxide with expected antitumor activity.
Some derivatives of quinazoline and 1, 2-dihydroquinazoline N(3)-oxide were synthesised and their cytotoxic activities against human leukaemia HL-60 cells under hypoxic and aerobic conditions were tested and compared to tirapazamine as the reference compound. Compound 8 showed 5-fold higher toxicity under hypoxic conditions than in normal oxygen atmosphere. The structure of quinazoline derivatives was established by X-ray crystal structure analysis.
Mikiciuk-Olasik
Elzbieta
E
Department of Pharmaceutical Chemistry and Drug Analysis, Medical University, Łódź, Poland. eolasik@farm.pharm.am.lodz.pl
Baszczak-Swiatkiewiz
Katarzyna
K
Zurek
Elzbieta
E
Krajewska
Urszula
U
Rózalski
Marek
M
Kruszyński
Rafał
R
Bartczak
Tadeusz J
TJ
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015687:Cell Hypoxia; D045744:Cell Line, Tumor; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D018360:Crystallography, X-Ray; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
C487730:1, 2-dihydroquinazoline N3-oxide; D000970:Antineoplastic Agents; D011799:Quinazolines