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Start Over Author "L Ransone" Journal bioorganic medicinal chemistry letters

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1. The design and synthesis of novel orally active inhibitors of AP-1 and NF-kappaB mediated transcriptional activation. SAR of in vitro and in vivo studies.

Author

Palanki MS, Erdman PE, Ren M, Suto M, Bennett BL, Manning A, Ransone L, Spooner C, Desai S, Ow A, Totsuka R, Tsao P, and Toriumi W

Subjects
Administration, Oral, Animals, Arthritis, Experimental drug therapy, Disease Models, Animal, Drug Design, Humans, Jurkat Cells, Quinazolines administration & dosage, Rats, Structure-Activity Relationship, NF-kappa B antagonists & inhibitors, Quinazolines chemical synthesis, Quinazolines pharmacology, Transcription Factor AP-1 antagonists & inhibitors, Transcriptional Activation drug effects
Abstract

We have developed novel orally active quinazoline analogues as inhibitors of AP-1 and NF-kappaB mediated transcriptional activation. Among the derivatives prepared, 1-[2-(2-thienyl)quinazolin-4-ylamino]-3-methyl-3-pyrroline-2,5-dione (10) showed significant activity in an adjuvant-induced arthritis rat model by reducing the swelling by 65% in the non-injected foot. The synthesis, structure-activity relationship, and in vivo activity are described.

Published
2003
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