title: Synthesis and in vitro anti-leukemic activity of structural analogues of JS-K, an anti-cancer lead compound.
abstract: Structural analogues of JS-K, an anti-cancer lead compound, were prepared and their in vitro anti-leukemic activity was determined. The rate of nitric oxide release from the corresponding diazeniumdiolate anions did not appear to affect the anti-leukemic activity of the prodrug forms. Two compounds with potent inhibitory activity and a potentially favorable toxicological profile were identified.
authors.affiliation: Chemistry Section, Laboratory of Comparative Carcinogenesis, National Cancer Institute at Frederick, PO Box B, Frederick, MD 21702, USA. chakrah@ncifcrf.gov
authors.forename: Harinath
authors.initials: H
authors.lastname: Chakrapani
authors.forename: Michael M
authors.initials: MM
authors.lastname: Goodblatt
authors.forename: Vidya
authors.initials: V
authors.lastname: Udupi
authors.forename: Swati
authors.initials: S
authors.lastname: Malaviya
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Shami
authors.forename: Larry K
authors.initials: LK
authors.lastname: Keefer
authors.forename: Joseph E
authors.initials: JE
authors.lastname: Saavedra
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001391:Azo Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D005978:Glutathione / Q000378:metabolism; D005982:Glutathione Transferase / Q000378:metabolism*; D018922:HL-60 Cells; D006801:Humans; D007938:Leukemia / Q000378:metabolism; D008958:Models, Molecular; D015394:Molecular Structure; D020030:Nitric Oxide Donors / Q000737:chemistry / Q000494:pharmacology; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011355:Prodrugs / Q000494:pharmacology
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D001391:Azo Compounds; D020030:Nitric Oxide Donors; C474958:O(2)-(2,4-dinitrophenyl) 1-((4-ethoxycarbonyl)piperazin-1-yl)diazen-1-ium-1,2-diolate; D010879:Piperazines; D011355:Prodrugs; D005982:Glutathione Transferase; D005978:Glutathione