Khayyat, Ahdab N. published the artcileDesign, Synthesis, and Antipoliferative Activities of Novel Substituted Imidazole-Thione Linked Benzotriazole Derivatives, Application In Synthesis of 3696-23-9, the publication is Molecules (2021), 26(19), 5983, database is CAplus and MEDLINE.
A new series of benzotriazole moiety bearing substituted imidazol-2-thiones I [R = H, 4-Me, 2-F, etc.] at N1 was designed, synthesized and evaluated for in vitro anticancer activity against the different cancer cell lines MCF-7(breast cancer), HL-60 (Human promyelocytic leukemia), and HCT-116 (colon cancer). Most of the benzotriazole analogs exhibited promising antiproliferative activity against tested cancer cell lines. Among all the synthesized compounds, I [R = 2,4-di-Cl] showed potent activity against the cancer cell lines such as MCF-7, HL-60 and HCT-116 with IC50 3.57, 0.40 and 2.63μM, resp. Compound I [R = 2,4-di-Cl] was taken up for elaborate biol. studies and the HL-60 cells in the cell cycle were arrested in G2/M phase. Compound I [R = 2,4-di-Cl] showed remarkable inhibition of tubulin polymerization with the colchicine binding site of tubulin. In addition, compound I [R = 2,4-di-Cl] promoted apoptosis by regulating the expression of pro-apoptotic protein BAX and anti-apoptotic proteins Bcl-2. These results provide guidance for further rational development of potent tubulin polymerization inhibitors for the treatment of cancer.
Molecules published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, Application In Synthesis of 3696-23-9.
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