Synthesis and antiproliferative activity of pyrrolo[3,2-b]pyridine derivatives against melanoma.
Synthesis of a new series of diarylureas and amides having pyrrolo[3,2-b]pyridine scaffold is described. Their in vitro antiproliferative activity against human melanoma cell line A375 and HS 27 human fibroblast cell line was tested and the effect of substituents on the pyrrolo[3,2-b]pyridine was investigated. The newly synthesized compounds, except meta-substituted derivatives (Ij-k and Iv-w), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds Ir and It having 5-benzylamide substituted 4'-amide moieties showed the most potent antiproliferative activity against A375.
Kim
Hee Jin
HJ
Biomaterials Research Center, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
Jung
Myung-Ho
MH
Kim
Hwan
H
El-Gamal
Mohammed I
MI
Sim
Tae Bo
TB
Lee
So Ha
SH
Hong
Jun Hee
JH
Hah
Jung-Mi
JM
Cho
Jung-Hyuck
JH
Choi
Jung Hoon
JH
Yoo
Kyung Ho
KH
Oh
Chang-Hyun
CH
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001557:Benzenesulfonates / Q000494:pharmacology; D002460:Cell Line; D006801:Humans; D008545:Melanoma / Q000188:drug therapy; D009536:Niacinamide / Q000031:analogs & derivatives; D010671:Phenylurea Compounds; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000077157:Sorafenib; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D001557:Benzenesulfonates; D010671:Phenylurea Compounds; D011725:Pyridines; D009536:Niacinamide; D000077157:Sorafenib