Synthesis and Antitumor Properties of New 1,2,4-Triazoles and 1,3,4-Thiadiazoles

Anticancer Activity of Mannich Bases: A Review of Recent Literature

“…[144] Three Mannich bases 148 (Figure 18) having a fluoroquinolone antibiotic as amine moiety introduced through aminomethylation of the triazolthione substrate (X = S) were shown to inhibit the growth of PC-3 prostate cancer cell line by 46 % to 56 % at 10 μM. [145] In a series of papers, the antitumor activity of Mannich bases 149, 150 and 151 (Figure 18) against two models of grafted murine tumors (Ehrlich ascites carcinoma and S-37) has been investigated, [146][147][148] and their ability to inhibit methylation of DNA in tumors was determined to be relatively poor to modest. [146,147] Out of these Mannich bases, compound 150 (R = C 6 H 5 , n = 1) exhibited 54 % tumor growth inhibition of S-37 at 155 mg/kg, and increased the lifespan of mice with Ehrlich ascites carcinoma by 35 %.…”

“…[145] In a series of papers, the antitumor activity of Mannich bases 149, 150 and 151 (Figure 18) against two models of grafted murine tumors (Ehrlich ascites carcinoma and S-37) has been investigated, [146][147][148] and their ability to inhibit methylation of DNA in tumors was determined to be relatively poor to modest. [146,147] Out of these Mannich bases, compound 150 (R = C 6 H 5 , n = 1) exhibited 54 % tumor growth inhibition of S-37 at 155 mg/kg, and increased the lifespan of mice with Ehrlich ascites carcinoma by 35 %. [147] The antiproliferative activity of Mannich bases 152 (Figure 18) of triazolethiones with various cycloalkyl substituents as R 1 was modest irrespective of the cancer cell line that was tested (A549, HeLa, TOV-112D or T47D).…”

“…[146,147] Out of these Mannich bases, compound 150 (R = C 6 H 5 , n = 1) exhibited 54 % tumor growth inhibition of S-37 at 155 mg/kg, and increased the lifespan of mice with Ehrlich ascites carcinoma by 35 %. [147] The antiproliferative activity of Mannich bases 152 (Figure 18) of triazolethiones with various cycloalkyl substituents as R 1 was modest irrespective of the cancer cell line that was tested (A549, HeLa, TOV-112D or T47D). [149] Six Mannich bases 153 derived from monofunctional secondary aliphatic amines and two Mannich bases 154 derived from piperazine as bifunctional secondary aliphatic amine (Figure 18) were evaluated against MDA-MB 231 and Caco-2 cell lines, and while both types of Mannich bases were more active than 5-fluorouracil (IC 50 = 21 μM) against MDA-MB 231 cells, only compounds 154 were superior to 5-fluorouracil (IC 50 = 0.437 μM) against Caco-2 cells.…”

Synthesis and characterization of a new series of thiadiazole derivatives as potential anticancer agents

“…The potential anticancer activity of this structure is one the most interesting areas that have encouraged researchers to focus on it. Hence, a large number of 1,3,4-thiadiazole derivatives have been synthesized and their molecular mechanism of anticancer activity has been investigated [10][11][12][13][14][15].…”