22794-89-4Relevant academic research and scientific papers
A facile one pot synthesis of thiazolo[3,2-: A] benzimidazole and pyran fused polyheterocyclic scaffolds
Mariappan, Arumugam,Rajaguru, Kandasamy,Muthusubramanian, Shanmugam,Bhuvanesh, Nattamai
supporting information, p. 4196 - 4199 (2019/05/06)
An efficient synthesis of dihydro-4H-benzo[4,5]imidazo[2,1-b]pyrano[2,3-d]thiazole by a multicomponent route starting from 2-((1H-benzo[d]imidazol-2-yl)thio)-1-phenylethan-1-one, an aromatic aldehyde and malononitrile is described. This protocol features
Synthesis, crystal study, and anti-proliferative activity of some 2-benzimidazolylthioacetophenones towards triple-negative breast cancer MDA-MB-468 cells as apoptosis-inducing agents
Abdel-Aziz, Hatem A.,Eldehna, Wagdy M.,Ghabbour, Hazem,Al-Ansary, Ghada H.,Assaf, Areej M.,Al-Dhfyan, Abdullah
, (2016/08/05)
On account of its poor prognosis and deficiency of therapeutic stratifications, triple negative breast cancer continues to form the causative platform of an incommensurate number of breast cancer deaths. Aiming at the development of potent anticancer agents as a continuum of our previous efforts, a novel series of 2-((benzimidazol-2-yl)thio)-1-arylethan-1-ones 5a–w was synthesized and evaluated for its anti-proliferative activity towards triple negative breast cancer (TNBC) MDA-MB-468 cells. Compound 5k was the most active analog against MDA-MB-468 (IC50 = 19.90 ± 1.37 μM), with 2.1-fold increased activity compared to 5-fluorouracil (IC50 = 41.26 ± 3.77 μM). Compound 5k was able to induce apoptosis in MDA-MB-468, as evidenced by the marked boosting in the percentage of florecsein isothiocyanate annexin V (Annexin V–FITC)-positive apoptotic cells (upper right (UR) + lower right (LR)) by 2.8-fold in comparison to control accompanied by significant increase in the proportion of cells at pre-G1 (the first gap phase) by 8.13-fold in the cell-cycle analysis. Moreover, a quantitative structure activity relationship (QSAR) model was established to investigate the structural requirements orchestrating the anti-proliferative activity. Finally, we established a theoretical kinetic study.
Synthesis of difluorinated β-ketosulfones and novel gem-difluoromethylsulfone-containing heterocycles as fluorinated building blocks
Loghmani-Khouzani, Hossein,Hajiheidari, Dariush
experimental part, p. 561 - 569 (2010/05/18)
A series of new heterocyclic β-ketosulfides was prepared by the reaction of the corresponding heterocyclic thiols with α-bromoacetophenone and its derivatives. Oxidation of the products using m-CPBA gave the corresponding heterocyclic β-ketosulfones, whic
New styryl sulfones as anticancer agents
Vedula, Manohar Sharma,Pulipaka, Aravind Babu,Venna, Chandrasekhar,Chintakunta, Vamsee Krishna,Jinnapally, Sreenu,Kattuboina, Venkata Adiseshu,Vallakati, Ravi Krishna,Basetti, Vishnu,Akella, Venkateswarlu,Rajgopal, Sriram,Reka, Ajaya Kumar,Teepireddy, Sravan Kumar,Mamnoor, Prem Kumar,Rajagopalan, Ramanujam,Bulusu, Gopalakrishnan,Khandelwal, Akash,Upreti, Vijay V.,Mamidi, Srinivas Rao
, p. 811 - 824 (2007/10/03)
New styryl sulfone compounds have been synthesized and evaluated for their anti-proliferative activity. Among the compounds synthesized, one compound (7k) has shown 51% tumor growth inhibition in mice implanted with HT-29 human carcinoma at 400 mg kg-1 orally.
A convenient one-pot synthesis of 2-benzimidazolyl-thioacetophenones and thiazolo[3,2-a]benzimidazoles
Sarhan, Abd El-Wareth A.O.,El-Sherief, Hasan A.H.,Mahmoud, Abdalla M.
, p. 10485 - 10496 (2007/10/03)
2-Mercaptobenzimidazole (1) reacts with aromatic ketones 2a-d in acidified acetic acid giving 2-benzimidazolylthioacetophenones 3a-d, which on cyclization yield thiazolo[3,2-a]-benzimidazoles 4a-d. Acetylation of 3a,d gave the N-acetyl derivatives 5a,d. C
