实验室及研究工作简介.pptVIP

Hansch et al. This work DCK analogs APPLICATION TO ANTI-HIV DRUG DESIGN 3’,4’-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) was identified as a potent anti-HIV agent: EC50 = 2.56×10-2 μM TI = 1.37×105 in H9 lymphocyte AZT (EC50 1.89×10-1 μM and TI 10,000) 4-methyl-DCK : EC50 = 5.94?10-3 mM 4-methyl-DCK was chosen as a drug candidate for pre-clinical studies. However, the low solubility and poor bioavailability of 4-methyl DCK limited its further development. DCK analogs Table 1 Parameter of 3D-QSAR model ? ? ? # R3 R4 R5 R6 # R3 R4 R5 R6 ? CH2CN Me H/OCH3 H ? CH2