title: Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors.
abstract: The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis of a series of substituted 4-[2-amino-1,3-thiazolyl]-thiophene-2-carboxamidines is described. Further optimization of this series by substitution of the terminal amine yielded urokinase inhibitors with excellent activities.
authors: 3-Dimensional Pharmaceuticals, Inc., Exton, PA 19341, USA. wilson@3dp.com
authors: K J
authors: KJ
authors: Wilson
authors: C R
authors: CR
authors: Illig
authors: N
authors: N
authors: Subasinghe
authors: J B
authors: JB
authors: Hoffman
authors: M J
authors: MJ
authors: Rudolph
authors: R
authors: R
authors: Soll
authors: C J
authors: CJ
authors: Molloy
authors: R
authors: R
authors: Bone
authors: D
authors: D
authors: Green
authors: T
authors: T
authors: Randall
authors: M
authors: M
authors: Zhang
authors: F A
authors: FA
authors: Lewandowski
authors: Z
authors: Z
authors: Zhou
authors: C
authors: C
authors: Sharp
authors: D
authors: D
authors: Maguire
authors: B
authors: B
authors: Grasberger
authors: R L
authors: RL
authors: DesJarlais
authors: J
authors: J
authors: Spurlino
mesh_terms: D000578:Amidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D010960:Plasminogen Activators / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D013876:Thiophenes / Q000138:chemical synthesis / Q000494:pharmacology; D014568:Urokinase-Type Plasminogen Activator / Q000037:antagonists & inhibitors*
chemical_list: D000578:Amidines; D013844:Thiazoles; D013876:Thiophenes; C004483:2-aminothiazole; D010960:Plasminogen Activators; D014568:Urokinase-Type Plasminogen Activator