Cytotoxic Evaluation of Some Fused Pyridazino- and Pyrrolo-quinazolinones Derivatives on Melanoma and Prostate Cell Lines
نویسندگان
چکیده
BACKGROUND Quinazolinon as an important class of heterocycles is attractive in medicinal research areas due to their wide range of biological effects. Cytotoxic activities of the quinazolinone derivatives in various cell lines including: HeLa, L1210 (mouse lymphocytic leukemia) and HT29 (human colon adenocarcinoma) were reported. MATERIALS AND METHODS In this study, a number of newly made tricycles quinazolinone derivatives such as fused pyridazino-quinazolinones and fused pyrrolo-quinazolinones were evaluated on two cancerous cell lines, melanoma (B16F10) and prostate (PC3) using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide colorimetric assay. RESULTS The results of cytotoxicity evaluations indicated that almost all of the compounds at the concentrations of 10 and 100 μM showed significant differences in viability in comparison with negative control at 48 h exposure (P < 0.05). However, during 24 h exposure some of the compounds showed cytotoxicity activity. CONCLUSION Results showed that both cell lines were sensitive to synthesized compounds and longer duration of exposure (48 h) had better results compared to that of 24 h screening.
منابع مشابه
Synthesis and cytotoxicity evaluation of some new 6-nitro derivatives of thiazole-containing 4-(3H)-quinazolinone
Quinazolinones are a group of fused heterocyclic compounds which have valuable biological properties including cytotoxic, antibacterial and antifungal activities. Thiazole group-containing compounds have been also reported to have a wide range of biological activities such as antitumor, anti-inflammatory, analgesic and antibacterial effects. Due to valuable cytotoxic effects of both thiazole gr...
متن کاملDesign and Synthesis of Pyrrolo[2,1-a]Isoquinoline-Based Derivatives as New Cytotoxic Agents
A new series of anti-cancer agents based on 1,2-diaryl-5,6-dihydropyrrolo[2,1-a]isoquinoline scaffold containing N,N-diethylaminoethoxy, piperidinylethoxy or morpholinylethoxy group at the para position of the C-2 phenyl ring were synthesized and their cytotoxic activities were assessed against several human cancer cell lines including MCF-7 (ER positive breast cancer cell), MDA-MB231 (ER-ne...
متن کاملDesign, Synthesis and Cytotoxicity Evaluation of New 2-Aryl-5,6-Dihydropyrrolo[2, 1-a]Isoquinoline Derivatives as Topoisomerase Inhibitors
Two set of 2-aryl-5,6-dihydropyrrolo[2,1-a] isoquinolines were designed and synthesized to evaluate their biological activities as topoisomerase inhibitors. Cytotoxic activity of the synthesized compounds 4a-e and 7a-d was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HepG2 (liver hepatocellular cells), A549 (adenocarcinomic human alveolar basal epithel...
متن کاملDesign, Synthesis and Cytotoxicity Evaluation of New 2-Aryl-5,6-Dihydropyrrolo[2, 1-a]Isoquinoline Derivatives as Topoisomerase Inhibitors
Two set of 2-aryl-5,6-dihydropyrrolo[2,1-a] isoquinolines were designed and synthesized to evaluate their biological activities as topoisomerase inhibitors. Cytotoxic activity of the synthesized compounds 4a-e and 7a-d was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HepG2 (liver hepatocellular cells), A549 (adenocarcinomic human alveolar basal epithel...
متن کاملDesign and Synthesis of Pyrrolo[2,1-a]Isoquinoline-Based Derivatives as New Cytotoxic Agents
A new series of anti-cancer agents based on 1,2-diaryl-5,6-dihydropyrrolo[2,1-a]isoquinoline scaffold containing N,N-diethylaminoethoxy, piperidinylethoxy or morpholinylethoxy group at the para position of the C-2 phenyl ring were synthesized and their cytotoxic activities were assessed against several human cancer cell lines including MCF-7 (ER positive breast cancer cell), MDA-MB231 (ER-ne...
متن کامل