Abstract

This proposal is concerned with determining the three-dimensional structures of selected compounds with demonstrated or potential usefulness in treatment of AIDS and AIDS associated syndromes and of cancer. The structural results will be used to identify those specific molecular features responsible for anti-AIDS activities, those responsible for anticancer actions and those which cause toxicities. This information will be used for the rational design of new agents which would be expected to be more efficacious, less toxic drugs. Compounds to be studied include: (1) Suramin and suramin analogues. Experiments in this area include structure determinations, modelling of three-dimensional conformations, docking of suramin's three-dimensional conformation to proteins, synthesis and biological testing of new analogues. (2) Glucosidase III inhibitors. (3) New anti-HIV agents from plant sources. (4) Agents useful for PET imagining of HIV-infected cells.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Institute of Allergy and Infectious Diseases (NIAID)
Type
Research Project (R01)
Project #
5R01AI040392-04
Application #
6149823
Study Section
Special Emphasis Panel (ZRG3-PB (02))
Program Officer
Litterst, Charles L
Project Start
1997-02-01
Project End
2002-01-31
Budget Start
2000-02-01
Budget End
2002-01-31
Support Year
4
Fiscal Year
2000
Total Cost
$308,087
Indirect Cost

  Institution

Name
Ardono Research
Department
Type
DUNS #
City
Seattle
State
WA
Country
United States
Zip Code
98105

  Publications

Adhikesavalu, D N; Mastropaolo, D; Camerman, A et al. (2001) Two rhodamine derivatives: 9-[2-(ethoxycarbonyl)phenyl]-3,6-bis-(ethylamino)-2,7-dimethylxanthylium chloride monohydrate and 3,6-diamino-9-[2-(methoxycarbonyl)-phenyl]xanthylium chloride trihydrate. Acta Crystallogr C 57:657-9
Mastropaolo, D; Camerman, A; Camerman, N (2001) Crystal structure of the hydrated strontium salt of methotrexate: two independent molecules with different conformations. J Med Chem 44:269-73
Hempel, A; Camerman, N; Mastropaolo, D et al. (2000) Ranitidine hydrochloride, a polymorphic crystal form. Acta Crystallogr C 56 ( Pt 8):1048-9
Hempel, A; Camerman, N; Mastropaolo, D et al. (2000) The antifolate trimetrexate: observation of the enzyme-binding conformation. Acta Crystallogr C 56 ( Pt 10):1225-7
Hempel, A; Camerman, N; Dauter, Z et al. (2000) The antiestrogen [2-(4-benzylphenoxy)ethyl]diethylammonium chloride. Acta Crystallogr C 56 ( Pt 4):455-6
Hempel, A; Camerman, N; Grierson, J et al. (1999) FF-beta-D-arabinofuranosyluracil. Acta Crystallogr C 55 ( Pt 4):632-3
Hempel, A; Camerman, N; Mastropaolo, D et al. (1999) Bis(2,2-dimethylaziridinyl)phosphinic amide. Acta Crystallogr C 55 ( Pt 7):1173-5
Hempel, A; Camerman, N; Mastropaolo, D et al. (1999) A Schiff base formed from sulfanilic acid and dimethylformamide. Acta Crystallogr C 55 ( Pt 4):697-8