Novel carbazole and acyl-indole antimitotics.
In the course of our Heat Shock 90 program, certain carbazole compounds were identified which had an off-target antiproliferative activity. To understand the off-target activity, we studied one analog with strong activity. We discovered that it had an effect on tubulin polymerization kinetics and was competitive with colchicine. Additional analogs were made, and a number of potent compounds were identified.
Barta
Thomas E
TE
thomas_e_barta@yahoo.com
Barabasz
Amy F
AF
Foley
Briana E
BE
Geng
Lifeng
L
Hall
Steven E
SE
Hanson
Gunnar J
GJ
Jenks
Matthew
M
Ma
Wei
W
Rice
John W
JW
Veal
James
J
D050256:Antimitotic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002227:Carbazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D003078:Colchicine / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D018841:HSP90 Heat-Shock Proteins / Q000378:metabolism; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014404:Tubulin / Q000378:metabolism
D050256:Antimitotic Agents; D002227:Carbazoles; D018841:HSP90 Heat-Shock Proteins; D007211:Indoles; D014404:Tubulin; D003078:Colchicine