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Bioorg Med Chem Lett. 2010 Dec 1;20(23):7159-63. doi: 10.1016/j.bmcl.2010.07.054. Epub 2010 Jul 24.

The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part 2: the second clinical candidate having a shorter and favorable human half-life.

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Pfizer Global Research and Development, Chesterfield, MO 63017, USA.


In this Letter, we provide the structure-activity relationships, optimization of design, testing criteria, and human half-life data for a series of selective COX-2 inhibitors. During the course of our structure-based drug design efforts, we discovered two distinct binding modes within the COX-2 active site for differently substituted members of this class. The challenge of a undesirably long human half-life for the first clinical candidate 1t(1/2)=360 h was addressed by multiple strategies, leading to the discovery of 29b-(S) (SC-75416) with t(1/2)=34 h.

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