Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line.
The synthesis of a novel series of aminoquinazoline derivatives 1a-r and their antiproliferative activities against A375 human melanoma cell line were described. Among them, six compounds showed superior antiproliferative activities to Sorafenib as a reference compound. In particular, the representative compound 1q bearing chromen-4-one moiety exhibited excellent antiproliferative activity (IC(50)=0.006 μM) and good selectivity over HS27 fibroblast cell line.
Lee
Junsang
J
Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
Nam
Bong Soo
BS
Kim
Hwan
H
Oh
Chang-Hyun
CH
Lee
So Ha
SH
Cho
Seung Joo
SJ
Sim
Tae Bo
TB
Hah
Jung-Mi
JM
Kim
Dong Jin
DJ
Tae
Jinsung
J
Yoo
Kyung Ho
KH
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D045744:Cell Line, Tumor; D002867:Chromones / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D008545:Melanoma / Q000188:drug therapy; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D002867:Chromones; D011799:Quinazolines