900145-33-7Relevant academic research and scientific papers
3-Aroyl-1,4-diarylpyrroles Inhibit Chronic Myeloid Leukemia Cell Growth through an Interaction with Tubulin
La Regina, Giuseppe,Bai, Ruoli,Coluccia, Antonio,Famiglini, Valeria,Passacantilli, Sara,Naccarato, Valentina,Ortar, Giorgio,Mazzoccoli, Carmela,Ruggieri, Vitalba,Agriesti, Francesca,Piccoli, Claudia,Tataranni, Tiziana,Nalli, Marianna,Brancale, Andrea,Vultaggio, Stefania,Mercurio, Ciro,Varasi, Mario,Saponaro, Concetta,Sergio, Sara,Maffia, Michele,Coluccia, Addolorata Maria Luce,Hamel, Ernest,Silvestri, Romano
, p. 521 - 526 (2017)
We designed 3-aroyl-1,4-diarylpyrrole (ARDAP) derivatives as potential anticancer agents having different substituents at the 1- or 4-phenyl ring. ARDAP compounds exhibited potent inhibition of tubulin polymerization, binding of colchicine to tubulin, and cancer cell growth. ARDAP derivative 10 inhibited the proliferation of BCR/ABL-expressing KU812 and LAMA84 cells from chronic myeloid leukemia (CML) patients in blast crisis and of hematopoietic cells ectopically expressing the imatinib mesylate (IM)-sensitive KBM5-WT or its IM-resistant KBM5-T315I mutation. Compound 10 minimally affected the proliferation of normal blood cells, indicating that it may be a promising agent to overcome broad tyrosine kinase inhibitor resistance in relapsed/refractory CML patients. Compound 10 significantly decreased CML proliferation by inducing G2/M phase arrest and apoptosis via a mitochondria-dependent pathway. ARDAP 10 augmented the cytotoxic effects of IM in human CML cells. Compound 10 represents a robust lead compound to develop tubulin inhibitors with potential as novel treatments for CML.
Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines
Ranjan Dwivedi, Ashish,Kumar, Vijay,Kaur, Harmeet,Kumar, Naveen,Prakash Yadav, Ravi,Poduri, Ramarao,Baranwal, Somesh,Kumar, Vinod
supporting information, (2020/08/13)
A series of triphenyl substituted pyrimidines as analogous of colchicine and combretastatin A-4 was synthesized and evaluated for the antiproliferative potential. The compounds were screened against MDA-MB-231, HCT-116 and HT-29 cell lines using MTT assay. Most of the compounds displayed antiproliferative activity in low to sub micro molar concentration. Amongst the synthesized derivatives, compounds HK-2, HK-10 and HK-13 were found to be effective against all the three cancer cell lines. HK-2 exhibited IC50 values of 3.39 μM, 4.78 μM and 4.23 μM, HK-10 showed IC50 values of 0.81 μM, 5.89 μM, 4.96 μM and HK-13 showed IC50 values 3.24 μM, 4.93 μM and 4.73 μM against MDA-MB-231, HCT-116 and HT-29 cancer cell lines, respectively. HK-10 was found to be the most potent compound in the series with IC50 values of 0.81 μM against MDA-MB-231. In the cell cycle analysis, HK-2 and HK-10 showed cell arrest at G2/M phase of the cell cycle while HK-13 inhibited cell growth at the G1/G0 phase. All the three compounds showed cell death induced through apoptosis. In the docking studies, HK-2, HK-10 and HK-13 were found to fit well in the colchicine binding site of the tubulin. Some of the compounds in the current series were found to be promising against all the three cancer cell lines and may act as potent leads for further development.
Identification of 3',4',5'-trimethoxychalcone analogues as potent inhibitors of Helicobacter pylori-induced inflammation in human gastric epithelial cells
Lai, Chih-Ho,Rao, Yerra Koteswara,Fang, Shih-Hua,Sing, Yu-Ting,Tzeng, Yew-Min
supporting information; experimental part, p. 5462 - 5465 (2011/01/03)
Efforts to identify potent small molecule inhibitors of Helicobacter pylori led to the evaluation of 23 3',4',5'-trimethoxychalcone analogues. Some of the compounds displayed potent antibacterial activity against H. pylori. Three most active and selective
