Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

C Yung-Chi, WH Prusoff - Biochemical pharmacology, 1973 - Elsevier
A theoretical analysis has been made of the relationship between the inhibition constant (K I
) of a substance and the (I 50 ) value which expresses the concentration of inhibitor required …

Synthesis and biological activity of several amino analogs of thymidine

TS Lin, WH Prusoff - Journal of Medicinal Chemistry, 1978 - ACS Publications
3', 5'-Diamino-3', 5'-dideoxythymidine (7) was synthesized via a nine-step synthesis from
thymidine in good overall yield. 3'-Amino-3'-deoxythymidine (8) and 5'-amino-5'-…

Early nucleoside reverse transcriptase inhibitors for the treatment of HIV: a brief history of stavudine (D4T) and its comparison with other dideoxynucleosides

JC Martin, MJM Hitchcock, E De Clercq, WH Prusoff - Antiviral research, 2010 - Elsevier
… Because of the company's proximity to Yale in Connecticut, Bristol-Myers (Hitchcock and
Martin) worked closely with Professor Prusoff's group to characterize a variety of nucleoside …

Synthesis of 5-(dihydroxyboryl)-2'-deoxyuridine and related boron-containing pyrimidines

RF Schinazi, WH Prusoff - The Journal of Organic Chemistry, 1985 - ACS Publications
Organoboron derivatives of pyrimidines and of 2,-deoxyribonucleosides have been
synthesized as potential antiviral and anticancer agents. Thefirst 5-boron-substituted pyrimidine …

Selective inhibition of human immunodeficiency virus type 1 replication by the (-) but not the (+) enantiomer of gossypol

…, DK Zheng, LA Huang, WH Prusoff - Antimicrobial agents …, 1989 - Am Soc Microbiol
The (-) enantiomer of gossypol but not the (+) enantiomer had good antiviral activity in
peripheral blood mononuclear cells against human immunodeficiency virus type 1 at a …

1-(2, 3-Dideoxy-. beta.-D-glycero-pent-2-enofuranosyl) thymine. A highly potent and selective anti-HIV agent

…, TS Lin, EM August, WH Prusoff - Journal of medicinal …, 1989 - ACS Publications
The nucleoside analogue l-(2, 3-dideoxy-/3-Dg (ycero-pent-2-enofuranosyl) thymine (d4T, 1)
was prepared by ring opening of the 3', 5'-anhydro compound 5. This method has been …

Anti-HIV-1 activity and cellular pharmacology of various analogs of gossypol

…, S Yikang, W Kemei, H Liang, WH Prusoff - Biochemical …, 1993 - Elsevier
We previously reported that the racemic mixture and both enantiomers of gossypol inhibit
the replication of human immunodeficiency virus-type 1 (HIV-1) (Lin et al., Antimicrob Agents …

Recent advances in chemotherapy of viral diseases

WH PRUSOFF - Pharmacological Reviews, 1967 - ASPET
Within recent years 2 compounds, idoxuridine (IUdR, 5-iodo-2'-deoxyuridine) and amantadine
(Symmetrel), have been approved by the Food and Drug Administration for use in the …

Nucleoside analogs with antiviral activity

WH Prusoff, DC Ward - Biochem. Pharmacol.;(United Kingdom), 1976 - osti.gov
Effects of chemical agents on viruses are discussed with regard to inhibition of virus adsorption,
inhibition of virus penetration and uncoating, and inhibition of an intracellular event. The …

A review of some aspects of 5-iododeoxyuridine and azauridine

WH Prusoff - Cancer research, 1963 - AACR
… by Jaffe and Prusoff (57) were not significantly dif ferent whether the drug was administered
daily in a single dose or in … Prusoff (57) that a 10—SOM excess of thymidine administered …