851916-81-9Relevant articles and documents
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases
Hamdouchi, Chafiq,Zhong, Boyu,Mendoza, Jose,Collins, Elizabeth,Jaramillo, Carlos,De Diego, Jose Eugenio,Robertson, Daniel,Spencer, Charles D.,Anderson, Bryan D.,Watkins, Scott A.,Zhang, Faming,Brooks, Harold B.
, p. 1943 - 1947 (2007/10/03)
Structure-based design approach was successfully used to guide the evolution of imidazopyridine scaffold yielding new structural class of highly selective inhibitors of cyclin dependent kinases that were able to form a new interaction with an identified residue of the protein, Lys89. Compounds from this series have shown no detectable effect when tested against a representative set of other serine/threonine kinases such as GSK3β, CAMKII, PKA, PKC-α,β,ε,γ. Compound 2i inhibits proliferation in HCT 116 cells in tissue culture. Synthesis, co-crystal structure of CDK2 in complex with compound 2i, and preliminary SAR study are disclosed.