Synthesis and anticancer activity studies of cyclopamine derivatives.
A diversity-oriented synthesis has been developed for facile construction of a library of carbohydrate-cyclopamine conjugates. The synthetic protocol is suitable for generating cyclopamine derivatives with various structural motifs for exploring the desired activity. From this initial library, we have observed one derivative that exhibits improved activity against lung cancer cell as compared to cyclopamine.
Zhang
Jianjun
J
Department of Chemistry and Biochemistry, Utah State University, 0300 Old Main Hill, Logan, UT 84322-0300, USA.
Garrossian
Massoud
M
Gardner
Dale
D
Garrossian
Arash
A
Chang
Young-Tae
YT
Kim
Yun Kyung
YK
Chang
Cheng-Wei Tom
CW
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002241:Carbohydrates / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D053823:Hedgehog Proteins / Q000378:metabolism; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy / Q000378:metabolism; D013329:Structure-Activity Relationship; D014704:Veratrum Alkaloids / Q000138:chemical synthesis* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D002241:Carbohydrates; D053823:Hedgehog Proteins; D014704:Veratrum Alkaloids; C000541:cyclopamine