[Synthesis and antitumour activities of some pteridine derivatives].
OBJECTIVE
To study the synthesis and antitumour activities of some aryl-substituted pteridines.


METHODS
A series of aryl-substituted pteridines were synthesized from 4, 6-diamino-5-nitrosopyrimidines by cyclization with 4-aminophenylacetonitriles. The antitumour activities were tested by MTT method.


RESULTS
Nine new compounds (I-III) were synthesized and their structures were characterized by EA, IR, 1HNMR and MS spectra. Compounds I-III showed antitumour activities in vitro.


CONCLUSIONS
Compounds I-III showed remarkable antitumour activities in vitro. No interaction was determined between the title compounds and calf thymus DNA. It indicated that these compounds possibly inhibit dihydrofolate reductase (DHFR) or other enzymes on which folic acid depends.
Ruan
Ji-wu
JW
School of Pharmaceutical Sciences, Sun Yat-sen (Zhongshan) University, Guangzhou 510080, China.
Huang
Jin-feng
JF
Fu
Li-wu
LW
Huang
Zhi-shu
ZS
Ma
Lin
L
Gu
Lian-quan
LQ
D000230:Adenocarcinoma / Q000473:pathology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor / Q000187:drug effects; D006801:Humans; D007624:KB Cells / Q000187:drug effects; D008175:Lung Neoplasms / Q000473:pathology; D015394:Molecular Structure; D011621:Pteridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000970:Antineoplastic Agents; D011621:Pteridines