Compounds > 4-benzyl-2-methyl-1-2-4-thiadiazolidine-3-5-dione

4-benzyl-2-methyl-1-2-4-thiadiazolidine-3-5-dione and Leukemia--Myeloid--Acute

4-benzyl-2-methyl-1-2-4-thiadiazolidine-3-5-dione has been researched along with Leukemia--Myeloid--Acute* in 1 studies

Other Studies

1 other study(ies) available for 4-benzyl-2-methyl-1-2-4-thiadiazolidine-3-5-dione and Leukemia--Myeloid--Acute

Article	Year
Discovery of 1,2,4-thiadiazolidine-3,5-dione analogs that exhibit unusual and selective rapid cell death kinetics against acute myelogenous leukemia cells in culture. Bioorganic & medicinal chemistry letters, 2011, Aug-15, Volume: 21, Issue:16 4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione (TDZD-8) was previously identified as an antileukemic agent exhibiting no evident toxicity toward normal hematopoietic cells. An SAR study has been carried out to examine the effect of varying the C-2 and C-4- substituents on the thiadiazolidinone ring of TDZD-8 on antileukemic activity. These studies resulted in the identification of more druglike analogs that exhibited comparable potency to TDZD-8 in killing acute myelogenous leukemia (AML) cells in culture. Surprisingly, the cell death kinetics induced by several of these novel analogs on MV-411 cells were extremely fast, with commitment to death occurring within 30 min. At a concentration of 10 μM, 3f (LD(50)=3.5 μM) completely eradicated cell viability of MV-411 cells within 2h, while analog 3e (LD(50)=2.0 μM) decimated cell viability within 30 min at a concentration of 10 μM and effectively abolished cell viability at 5 μM within 1-2h. Topics: Cell Death; Cell Survival; Dose-Response Relationship, Drug; Drug Discovery; Humans; Kinetics; Leukemia, Myeloid, Acute; Molecular Structure; Stereoisomerism; Structure-Activity Relationship; Thiadiazoles; Tumor Cells, Cultured	2011

Article

Year

Discovery of 1,2,4-thiadiazolidine-3,5-dione analogs that exhibit unusual and selective rapid cell death kinetics against acute myelogenous leukemia cells in culture.

Bioorganic & medicinal chemistry letters, 2011, Aug-15, Volume: 21, Issue:16

4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione (TDZD-8) was previously identified as an antileukemic agent exhibiting no evident toxicity toward normal hematopoietic cells. An SAR study has been carried out to examine the effect of varying the C-2 and C-4- substituents on the thiadiazolidinone ring of TDZD-8 on antileukemic activity. These studies resulted in the identification of more druglike analogs that exhibited comparable potency to TDZD-8 in killing acute myelogenous leukemia (AML) cells in culture. Surprisingly, the cell death kinetics induced by several of these novel analogs on MV-411 cells were extremely fast, with commitment to death occurring within 30 min. At a concentration of 10 μM, 3f (LD(50)=3.5 μM) completely eradicated cell viability of MV-411 cells within 2h, while analog 3e (LD(50)=2.0 μM) decimated cell viability within 30 min at a concentration of 10 μM and effectively abolished cell viability at 5 μM within 1-2h.

Topics: Cell Death; Cell Survival; Dose-Response Relationship, Drug; Drug Discovery; Humans; Kinetics; Leukemia, Myeloid, Acute; Molecular Structure; Stereoisomerism; Structure-Activity Relationship; Thiadiazoles; Tumor Cells, Cultured

2011