Antitumor agents. Part 204: synthesis and biological evaluation of substituted 2-aryl quinazolinones.
A series of 2',3',4',6,7-substituted 2-aryl quinazolinones were synthesized and evaluated for biological activity. Among them, 17 displayed significant growth inhibitory action against a panel of tumor cell lines. Compound 17 was also a potent inhibitor of tubulin polymerization. Compounds 8-10 displayed selective activity against P-gp-expressing epidermoid carcinoma of the asopharynx.
Xia
Y
Y
Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill 27599, USA.
Yang
Z Y
ZY
Hour
M J
MJ
Kuo
S C
SC
Xia
P
P
Bastow
K F
KF
Nakanishi
Y
Y
Namrpoothiri
P
P
Hackl
T
T
Hamel
E
E
Lee
H K
HK
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D015658:HIV Infections / Q000188:drug therapy / Q000821:virology; D006801:Humans; D008214:Lymphocytes / Q000187:drug effects / Q000821:virology; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000096:biosynthesis / Q000187:drug effects; D014407:Tumor Cells, Cultured
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D011799:Quinazolines; D014404:Tubulin