Synthesis of C₆₀ fullerene-quadricyclane hybrid compound and its preliminary in vitro antitumor activity in combination with cisplatin

Abstract

This communication describes preliminary studies of the authors directed towards the possibility of practical implementation of the idea to design efficient antitumor drugs based on hybrid molecules composed of fullerene С60 and quadricyclanes. The essence of the proposed idea is that these hybrid molecules are able to cleave DNA owing to the fullerene moiety they contain and simultaneously to thermally affect tumor cells via cleavage of the carbon-carbon bond in quadricyclanes under the action of Pd and Pt ions. As a result, testing of the cytotoxic activity in vitro for a number of fullerene С60 hybrids with the norbornadiene or quadricyclane moieties against the human T-lymphoblastic leukemia cells (Jurkat cells) in combination of the known cisplatin drug, which was taken as the source of Pt ions, showed a statistically reliable dose-dependent increase in the number of dead cells in each group, which were formed according to the amount of cisplatin added, in comparison with the control, that is, cells treated with cisplatin or quadricyclane fullerene derivatives alone.

Identification of potential descriptors of water-soluble fullerene derivatives responsible for antitumor effects on lung cancer cells via QSAR analysis

“…Fullerenes and their derivatives are one of the most promising types of nanomaterials and have attracted a lot of attention for their perspective biomedical applications. Functionalized fullerene molecules can be utilized as platforms for drug delivery [60] , promising antiviral [61] , and antitumor drugs [62] . For example, the soluble fullerene derivatives can be used as anti-HIV drugs inhibiting viral replication [63] .…”