Abstract
Acridine derivatives were first used as antibacterial and antiparasitic agents, later as antimalarial and anti-HIV drugs, and now as potentially anti-cancer agents due to their high cytotoxic activity. Due to their serious adverse effects, new synthetic derivatives were introduced and tested based on modified naturally occurring substances, such as acridone derivatives, which also exhibit potential anti-tumor activity. Most of them are DNA-damaging substances, causing relatively strong and selective destruction of tumor cells. We have tested in vitro anti-proliferative effects of newly-synthesized tetrahydroacrid derivatives, namely tacrine-coumarin hybrid molecules, on various human and mouse cancer cell lines. Our results showed that tacrine-coumarin hybrids with seven, eight, and nine methylene groups in spacer reduce proliferation of cancer cells. A hybrid with nine methylene groups had the most significant anti-cancer effect.
Highlights
Coumarin and coumarin derivatives are well known anticancer agents
The compounds in which the chlorine was in C-6 and C-7 position on coumarin ring and iodine was in C-4 position on phenoxy moiety exhibited significant anti-cancer activity (MIC = 1.56 μg/mL).[3]
The concentrations of 7b-d hybrids used in both cell cycle as well as cell proliferation assays were derived based on the extensive screening of the cell metabolism and/or cell growth response (MTT)
Summary
Coumarin and coumarin derivatives are well known anticancer agents. The anticancer activity of coumarin derivatives, 3-, 4-, 7-, 8- substituted biscoumarins and fused coumarins, has been described according to the type and position of the side chain of the coumarin core structure.[1]. Basanagouda et al.[3] synthesized a new series of iodinated-4-aryloxymethyl coumarin derivatives 1 (Fig. 1). These compounds were screened for their in vitro anticancer activity against two cancer cell lines, MDA-MB human adenocarcinoma mammary gland and A-549 human lung carcinoma. Bana et al.[4] designed and synthesized a novel coumarin-quinone inhibitor 2 (SV37, Fig. 1), the structure of which is based on both coumarin and quinone moieties as a potent CDC25 inhibitor. Puttaraju et al.[5] designed and synthesized a new series of coumarin substituted dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-4-ones derivatives 3. The coumarin derivative with i-Pr in C-3 position on dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-4-one and chlo rine in C-6 position on coumarin ring was found to be the most potent cytotoxic compound (88%) against Dalton’s Ascitic Lymphoma cell line.[5]
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