158 Abstracts

AOl5 -m, -ZmAND-- OFrKnmL F'UTINM LINKED m. D.Gibson, K.F.Gean, M.Roll,

R-Ben-Shoshan, J.Katzhendler, A.Ramu. Hebrew University of Jeruslem, Jerusalem, ISRAEL.

In attwts to systematically probe the synergistic effects between Pt anticancer drugs and intercalators, we have prepared and characterized three novel classes of Pt linked to substituted 9,10-anthracen&iones. Several campaunds (II x=NH,O rr=2,3) displayed ED58 values of 10-7M.against P388 leukemia cells. In vivo soreening and DNA binding studies are in progress. A

A016 PHTHALATE, SALICYLATE, & CATECHOLATE PLATINUM CHELATE COMPLEXES. EFFECTS OF CHELATE RING SIZE ON PHYSICAL & BIOLOGICAL PROPERTIES.

Paul Schwartz and Devinder S. Gill, ANDRULIS Research Corporation, Beltsville, MD 20705, USA.

Platinum binds to phthalic, salicylic and catechol ligands forming complexes with chelate rings of 7, 6, and 5 atoms respectively. A series of such complexes has been prepared and physical and antitumor properties have been compared. Each member of the series possesses broad spectrum antitumor activity, including activity against cisplatin resistant tumor cells. While phthalates form the most potent antitumor agents, they are the least stable. Conversely, the 5-membered catechol chelate rings form the least potent complexes, requiring much higher doses. A phthalate complex has undergone Phase I and Phase II clinical trials.

A017 SYNTHESES, CHEMICAL PROPERTIES AND ANTI-TUMOR ACTIVITIES OF AMIDATE-B?IDGED MULTINUCLEAR PLATINUM COMPLEXES. K. Matsumoto,

Department of Chemistry, Waseda University, Shinjuku-ku, Tokyo 169, Japan

Several multinuclear zigzag chain bridgin 8) and PPt A L ]

amidate &j$ands of the type (A is amine

been synthesize a l6 i and structurally characterized. The chemical and electrochemical redox properties, especially the reactions with water, dioxygen and hydrogen peroxide will be presented. The anti-tumor activities of these complexes have been tested against L1210 and some marginal activities were found. Effects of the amidate ligand and counter anions on the activity will be ccxnpared.