Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2

• Authors: PARUCH Kamil; DWYER Michael; ALVAREZ Carmen; BROWN Courtney; CHAN Tin-Yau; DOLL Ronald; KEERTIKAR Kerry; KNUTSON Chad; MCKITTRICK Brian; RIVERA Jocelyn; ROSSMAN Randall; TUCKER Greg; FISCHMANN Thierry; HRUZA Alan; MADISON Vincent; NOMEIR Amin; WANG Yaolin; LEES Emma; PARRY David; SGAMBELLONE Nicole; SEGHEZZI Wolfgang; SCHULTZ Lesley; SHANAHAN Fran; WISWELL Derek; XU Xiaoying; ZHOU Quiao; JAMES Ray; PARADKAR Vidyadhar; PARK Haengsoon; ROKOSZ Laura; STAUFFER Tara; GUZI Timothy
• Year of publication: 2007
• Type: Article in Periodical
• Magazine / Source: Bioorganic & Medicinal Chemistry Letters
• MU Faculty or unit: Faculty of Science

Web

• http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6TF9-4PMJJYW-5&_user=835458&_coverDate=11%2F15%2F2007&_alid=963411855&_rdoc=2&_fmt=high&_orig=search&_cdi=5221&_sort=r&_docanchor=&view=c&_ct=2&_acct=C000045159&_version=1&_urlVersion=0&_us
• http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6TF9-4PMJJYW-5&_user=835458&_coverDate=11%2F15%2F2007&_alid=963411855&_rdoc=2&_fmt=high&_orig=search&_cdi=5221&_sort=r&_docanchor=&view=c&_ct=2&_acct=C000045159&_version=1&_urlVersion=0&_userid=83

• Field: Pharmacology and pharmaceutical chemistry
• Keywords: CDK2 kinase; inibitor; cancer
• Description: Properly substituted pyrazolo[1,5-a]pyrimidines are potent and selective CDK2 inhibitors. Compound 15j is orally available and showed efficacy in a mouse A2780 xenograft model.