3-(Dipropylamino)-5-hydroxybenzofuro[2,3-f]quinazolin-1(2H)-one (DPA-HBFQ-1) plays an inhibitory role on breast cancer cell growth and progression

Inhibition of Human Topoisomerase II by N,N,N‐Trimethylethanammonium Iodide Alkylcarbazole Derivatives

“…Finally, total blockade of hTopo II activity was observed for compound 4 f (Figure B), which is the quaternary ammonium iodide derivative of compound 3 f ; its inhibitory activity is evidenced by the disappearance of the bottom DNA bands and the presence of a clear kDNA band at the top of the gel. As a control compound, we used ellipticine, whose inhibitory activity on hTopo II is well established; as expected, it is able to completely block hTopo II activity (Figure C, lane E) but at a concentration five‐fold higher than the most active compound, 4 f . Overall, the obtained results correlate well with the docking studies previously discussed, and indicate compound 4 f as the best candidate for poisoning hTopo II.…”

“…Trimethoxyphenylurea 1,4‐dimethylcarbazoles, N ‐thioalkylcarbazoles, 1,4‐dimethyl‐ N ‐alkylcarbazoles, N ‐(1,4‐dimethyl‐9 H ‐carbazol‐3‐yl)‐ N′ ‐alkylguanidines, benzofuro[2,3‐ f ]quinazolin‐1(2 H )‐ones, and hydrazine‐carbazole derivatives were also prepared, and some of them showed interesting anti‐proliferative activity against breast cancer cells without affecting the viability of non‐tumor cell lines. Several studies have reported that carbazole derivatives, such as ellipticine and celiptium (Figure ), are inhibitors of human topoisomerases I and II …”

“…labill, [19] introduced for the treatment of metastatic breast cancer, [6,[20][21][22][23] but later dismissed because of poor aqueous solubility ands evere side effects, [24,25] were synthesized. [26][27][28][29][30] Trimethoxyphenylurea 1,4-dimethylcarbazoles, [31] N-thioalkylcarbazoles, [15] 1,4-dimethyl-N-alkylcarbazoles, [32] N-(1,4-dimethyl-9H-carbazol-3-yl)-N'-alkylguanidines, [33] benzofuro[2,3-f]quinazolin-1(2H)-ones, [34] and hydrazine-carbazole derivatives [20] were also prepared, and some of them showed interesting anti-proliferative activity against breast cancerc ells withouta ffecting the viability of non-tumor cell lines. Severals tudies have reported that carbazole derivatives, such as ellipticine and celiptium ( Figure 1), are inhibitors of human topoisomerases Ia nd II.…”

Old Drug Scaffold, New Activity: Thalidomide‐Correlated Compounds Exert Different Effects on Breast Cancer Cell Growth and Progression

“…Cells were plated and cultured to form a monolayer, then scratched to form a wound (see Experimental Section) and treated with compounds 1 – 8 at concentrations corresponding to their respective IC 50 values (Table ) for 48 and 72 h, for MDA‐MB‐231 and MCF‐7 cells, respectively. These different endpoint times were experimentally determined, considering that MDA‐MB‐231 cells have a higher growth rate than MCF‐7 cells and tend to give greater metastases in vivo . In MCF‐7 cells compounds 2 , 3 , 7 , and 8 produced higher effects, preventing total wound closure at percentages of ∼52, 77, 72, and 69 % (Figure A).…”

“…We tested the ability of compounds 1-8 to affect the migration of MCF-7 and MDA-MB-231 cells by using as imple, lowcost, and well-developedi nvitro method:t he wound-healing assay.C ells were plated and cultured to formam onolayer, then scratched to form aw ound (see Experimental Section) and treated withc ompounds 1-8 at concentrations corresponding to their respective IC 50 values (Table 1) for 48 and 72 h, for MDA-MB-231 and MCF-7 cells, respectively.T hese different endpoint times were experimentally determined, consid- ering that MDA-MB-231c ells have ah igher growth rate than MCF-7 cells andt end to give greater metastases in vivo. [37] In MCF-7 cells compounds 2, 3, 7,a nd 8 produced higher effects, preventing total wound closure at percentages of~52, 77, 72, and 69 %( Figure 5A). In MDA-MB-231 cells, the same compounds produced as ignificant lack of total wound closure (1 1,2 5, 27, and 25 %, respectively); however,i nc ontrastt o MCF-7 cells, compound 6 exhibited an impressive effect in preventingw ound closure:~32 %( Figure 5B).…”