PMID: 15218983Jun 29, 2004Paper

Biological properties of 8-methoxypyrimido[4(1),5(1):4,5]thieno(2,3-b)quinoline-4(3H)-one, a new class of DNA intercalating drugs

The Indian Journal of Medical Research
M Gopal, M S Shahabuddin

Abstract

The compounds containing novel tetracyclic condensed quinoline ring system is of interest because of its close relationship with anticancer drug ellipticine. 8-Methoxypyrimido[4(1),5(1):4,5]thieno(2,3-b)quinoline-4(3H)-one (MPTQ) was investigated to study its effect on in vitro growth inhibition and clonogenic cell survival assay on three tumour cell lines, human promyelocytic leukemia HL-60, melanoma B16F10 and neuro 2a. A systematic study was carried out to evaluate its antitumour efficacy against B16 murine melanoma. Antiinflammatory and analgesic activities of MPTQ were also studied. The cytotoxicity of MPTQ on HL-60, B16F10 and neuro 2a cells was estimated by trypan blue exclusion test. The antitumour activity was evaluated using single dose, multiple/daily injections (days 3-6) or intermittent treatments over two weeks against s.c. implanted B16melanoma, both in terms of increased life span and tumour growth inhibition. Antiinflammatory activity was seen on carrageenan induced hind paw oedema. Counting the number of abdominal constrictions after the injection of acetic acid assessed the analgesic response. MPTQ is cytotoxic to all the cell lines tested and ID50 being in the range of 0.08-1.0 microM. MPTQ was studied for a...Continue Reading

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