Metal-Based Drugs

Metal-Based Drugs / 1997 / Article

Open Access

Volume 4 |Article ID 460234 |

Merrill C. Miller, Anup Sood, Bernard F. Spielvogel, Ken Bastow, Iris H. Hall, "Cytotoxic Action of Carboxyborane Heterocyclic Amine Adducts", Metal-Based Drugs, vol. 4, Article ID 460234, 13 pages, 1997.

Cytotoxic Action of Carboxyborane Heterocyclic Amine Adducts

Received15 May 1997
Accepted28 May 1997


The heterocyclic carboxyborane amines were found to be potent cytotoxic agents in the murine L1210 lymphoid leukemia and human HeLa suspended carcinoma cells. These agents were observed to inhibit HeLa DNA topoisomerase II activity ~ 200 μM and L1210 topoisomerase II activity ≥ 100 μM. These agents did not cause DNA protein linked breaks themselves, but upon incubation for 14-24 hr did enhance the ability of VP-16 to cause cleavable complexes. The heterocyclic amineboranes inhibited DNA synthesis and caused DNA strand scission. They were additive with VP-16 in affording these results as well as inhibiting colony growth of L1210 cells after co-incubation for 1 hr. The agents inhibited in vitro PKC phosphorylation of both L1210 lymphoid leukemia and human topoisomerase II enzyme.

Copyright © 1997 Hindawi Publishing Corporation. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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