Table 2. p53 activation by JJ78:1 analogues shown in terms of their relative potency order with the most potent analogue assigned as 1.
Compound | C3 | C4 | C5 | Aryl substituents | Potency order |
---|---|---|---|---|---|
JJ78:12 | CH3 | COAr | CH3 | 3′-Cl | 1 |
JJ78:13 | CH3 | CH2Ar | CH3 | 2′,5′-F2 | 4 |
JJ78:14 | CH3 | COAr | CH3 | 2′-OMe | =3 |
JJ78:15 | CH3 | COAr | CH3 | 2′-OH | =3 |
JJ78:16 | CH3 | COAr | CH3 | 2′-(morpholin-4-yl)-5′-F | 2 |
JJ78:17 | H | COAr | H | 2′,5′-F2 | Inactive |
JJ78:18 | H | H | COAr | 3′-Cl | Inactive |