title: Synthesis and antiproliferative activity of pyrrolo[3,2-b]pyridine derivatives against melanoma.
abstract: 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.
authors.affiliation: Biomaterials Research Center, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
authors.forename: Hee Jin
authors.initials: HJ
authors.lastname: Kim
authors.forename: Myung-Ho
authors.initials: MH
authors.lastname: Jung
authors.forename: Hwan
authors.initials: H
authors.lastname: Kim
authors.forename: Mohammed I
authors.initials: MI
authors.lastname: El-Gamal
authors.forename: Tae Bo
authors.initials: TB
authors.lastname: Sim
authors.forename: So Ha
authors.initials: SH
authors.lastname: Lee
authors.forename: Jun Hee
authors.initials: JH
authors.lastname: Hong
authors.forename: Jung-Mi
authors.initials: JM
authors.lastname: Hah
authors.forename: Jung-Hyuck
authors.initials: JH
authors.lastname: Cho
authors.forename: Jung Hoon
authors.initials: JH
authors.lastname: Choi
authors.forename: Kyung Ho
authors.initials: KH
authors.lastname: Yoo
authors.forename: Chang-Hyun
authors.initials: CH
authors.lastname: Oh
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D001557:Benzenesulfonates; D010671:Phenylurea Compounds; D011725:Pyridines; D009536:Niacinamide; D000077157:Sorafenib