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. Author manuscript; available in PMC: 2015 Sep 15.
Published in final edited form as: Bioorg Med Chem Lett. 2012 Oct 24;23(1):340–345. doi: 10.1016/j.bmcl.2012.10.080

Table 2.

Inhibition activities of Cmpd8, Cmpd21, and truncated analogs. Inhibitory effect of compounds on sPLA2-IIA-integrin interaction was assessed in adhesion assays using αvβ3-K562 cells and immobilized sPLA2-IIA. The IC50 and maximum inhibition was calculated with adhesion without inhibitors as 100% and adhesion to BSA only as 0%. Data are shown as means ± S.E. (n=3).

Compound Structural Formulaa Activity
(IC50, μM)
Maximum
Inhibition
(%)
Cmpd8-1 R-OH - N/A
Cmpd8-2 R-Ala - N/A
Cmpd8-3 R-Ala-Trp - N/A
Cmpd8-4 R-Ala-Trp-Asp* - N/A
Cmpd8-5 Ala-Trp-Asp*-Ile - N/A
Cmpd8 R-Ala-Trp-Asp*-Ile 20±1.3 85±1.5
Cmpd21-1 R-Gly 241±33 98±2.4
Cmpd21-2 R-Gly-Arg* 262±6.8 77±1.8
Cmpd21-3 R-Gly-Arg*-Gly 217±14 81±3.0
Cmpd21-4 R-Gly-Arg*-Gly-Asp* 155±3.8 87±1.7
Cmpd21-5 R-Gly-Arg*-Gly-Asp*-Asp* - N/A
Cmpd21-6 Gly-Arg*-Gly-Asp*-Asp*-Asp* - N/A
Cmpd21 R-Gly-Arg*-Gly-Asp*-Asp*-Asp* 71±18 93±10
graphic file with name nihms-721310-t0017.jpg
a

A terminal residue has an ending NH2 group replacing the OH group of its carboxylic acid functionality. Amino acids with an asterisk stand for D-amino acids.