Table 2—

Effect of glucocorticoid substitutes on the binding affinity to the progesterone(PROG) receptor

SteroidΔ1Δ4αRαR1R2αR3R4βR5RBAPR
DEX++OHCH3CH2OHFHOH0.21
BET++OHβCH3CH2OHFHOH0.04
PROG+HHCH3HHH100
MF++OCOR'#CH3CH2ClClHOH2580
MO++OHCH3CH2ClClHOH3.5
FP++OCOCH2CH3CH3SCH2FFαFOH152
BMP++OCOCH2CH3βCH3CH2OHClHOH110
BECLO++OHβCH3CH2OHClHOH0.1
BUD++CH2CH2CH3HCH2OHHHOH21
TAA++CH3CH3CH2OHFHOH13
  • RBAPR: PROG relative binding affinity; BET: betamethasone; MF: mometasone furoate; MO: mometasone; FP: fluticasone propionate; BMP: beclomethasone-17-monopropionate; BECLO: beclomethasone; BUD: budesonide; TAA: triamcinolone acetonide. #: where R' =  furyl group. Delta 1(Δ1) and Delta 4 (Δ4) indicate the presence of the unsaturated double bond between C1–C2 and C4–C5, respectively; : refers to the structure in fig. 3b.