127034-05-3Relevant academic research and scientific papers
Structure-activity relationship studies and in vitro and in vivo anticancer activity of novel 3-aroyl-1,4-diarylpyrroles against solid tumors and hematological malignancies
Bai, Ruoli,Biagioni, Stefano,Cavallini, Chiara,Coluccia, Addolorata Maria Luce,Coluccia, Antonio,Da Pozzo, Eleonora,Hamel, Ernest,La Regina, Giuseppe,Liu, Te,Martini, Claudia,Mazzoccoli, Carmela,Mazzoni, Cristina,Nalli, Marianna,Orlando, Viviana,Puxeddu, Michela,Shen, Hongliang,Silvestri, Romano
, (2019)
Novel 3-aroyl-1,4-diarylpyrrole derivatives were synthesized to explore structure-activity relationships at the phenyls at positions 1 and 4 of the pyrrole. The presence of amino phenyl rings at positions 1 and 4 of the pyrrole ring were found to be a crucial requirement for potent antitumor activity. Several compounds strongly inhibited tubulin assembly through binding to the colchicine site. Compounds 42, 44, 48, 62 and 69 showed antitumor activity with low nanomolar IC50 values in several cancer cell lines. Compound 48 was generally more effective as an inhibitor of glioblastoma, colorectal and urinary bladder cancer cell lines; 69 consistently inhibited CML cell lines and demonstrated superiority in nilotinib and imatinib resistant LAMA84-R and KBM5-T315I cells. In animal models, compound 48 exhibited significant inhibition of the growth of T24 bladder carcinoma and ES-2 ovarian clear cell carcinoma tumors. Compounds 48 and 69 represent robust lead compounds for the design of new broad-spectrum anticancer agents active in different types of solid and hematological tumors.
Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors
Salum, Lívia B.,Altei, Wanessa F.,Chiaradia, Louise D.,Cordeiro, Marlon N.S.,Canevarolo, Rafael R.,Melo, Carolina P.S.,Winter, Evelyn,Mattei, Bruno,Daghestani, Hikmat N.,Santos-Silva, Maria Cláudia,Creczynski-Pasa, Tania B.,Yunes, Rosendo A.,Yunes, José A.,Andricopulo, Adriano D.,Day, Billy W.,Nunes, Ricardo J.,Vogt, Andreas
supporting information, p. 501 - 510 (2013/07/25)
Based on classical colchicine site ligands and a computational model of the colchicine binding site on beta tubulin, two classes of chalcone derivatives were designed, synthesized and evaluated for inhibition of tubulin assembly and toxicity in human canc
Chalcones: A new class of antimitotic agents
Edwards,Stemerick,Sunkara
, p. 1948 - 1954 (2007/10/02)
A series of chalcones was evaluated as antimitotic agents. One of these, (E)-1-(2,5-dimethoxyphenyl)-3-[4-(dimethylamino)phenyl]-2-methyl-2-propen- 1-one) (73), was found to be an effective antimitotic agent at a concentration of 4 nM in an in vitro HeLa
