Cytotoxic activities of some benzothiazole-piperazine derivatives

Abstract

Synthesis, characterization and cytotoxic activities of ten benzothiazole-piperazine derivatives were reported. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. Based on the GI 50 values of the compounds, most of the benzothiazole-piperazine derivatives are active against HUH-7, MCF-7 and HCT-116 cancer cell lines. Compound 1d is highly cytotoxic against all tested cancer cell lines. Further investigation of compound 1d by Hoechst Staining and Fluorescence-Activated Cell Sorting Analysis (FACS) revealed that this compound causes apoptosis by cell cycle arrest at subG 1 phase.

Importance of Fluorine in Benzazole Compounds

“…Moreover, the benzothiazole core is a widespread scaffold that has been extensively studied [ 54 , 55 , 56 , 57 , 58 , 59 ] and many derivatives are found to be antimicrobial [ 49 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 , 68 , 69 , 70 , 71 , 72 , 73 , 74 ], anticancer [ 75 , 76 , 77 , 78 , 79 , 80 , 81 , 82 , 83 , 84 , 85 , 86 , 87 , 88 , 89 , 90 , 91 ], anti-Alzheimer’s [ 92 , 93 ], anti-inflammatory [ 94 , 95 , 96 ], anti-HIV [ 97 , 98 , 99 ] anticonvulsant [ 100 , 101 , 102 ], antioxidant [ 39 , 103 ], anti-tuberculosis [ 104 ...…”

Antiproliferative benzothiazoles incorporating a trimethoxyphenyl scaffold as novel colchicine site tubulin polymerisation inhibitors

“…To discovery novel anti-prostate cancer agents and tubulin polymerisation inhibitors, we evaluated the antiproliferative activity of all benzothiazole derivatives 9a~9k and 12a~12d against a prostate cancer cell line 22RV1 using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay. Based on previous references, 5-fluorouracil (5-Fu) and was usually selected as a reference drug in the MTT assay to evaluate the antiproliferative activity of synthetic benzothiazole derivatives 26,27 . Therefore, 5-Fu was used as the control drug in this work.…”

Pd-catalyzed arylation of linear and angular spirodiamine salts under aerobic conditions

“…Screening continued with bicyclic N -aryl chlorides quinolone and quinoxaline, obtaining 4e - f in excellent yields. Efficient coupling continued with benzothiazole and benzooxazxole substrates, 3g - h , compounds with known anti-cancer 17 and antipsychotic properties 18 , respectively. We briefly examined 5-membered heterocycle rings with the chloro and bromo variants of 3i , affording respectable yields for the aminated thiazole product.…”