2019
DOI: 10.1016/j.bioorg.2018.10.027
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Discovery of novel quinazolines as potential anti-tubulin agents occupying three zones of colchicine domain

Abstract: A series of novel quinazolines as tubulin inhibitors occupying three zones of colchicine domain have been designed and synthesized inspired by the recently disclosed crystal structure of verubulin analogue 6 with tubulin. Among the newly synthesized compounds, 19c showed noteworthy potency against K562, HepG2, KB, HCT-8 and MDB-MB-231 cancer cells. In vitro microtubule polymerization assays identified 19c as a potent tubulin assembly inhibitor, the binding mode of which with tubulin was confirmed by molecular … Show more

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Cited by 38 publications
(26 citation statements)
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“…Verubulin (derivative 14 ) had reached phase II of a trial for the treatment of glioblastoma, but it was halted due to cardiovascular toxicity. Recently, Li et al described a new potent tubulin inhibitor with a pyridine ring ( 16 ) showing nanomolar activity against some cancer cell lines ( Figure 3 ) [ 126 ].…”
Section: Are Anticancer Quinazoline Derivatives Good Candidates To Be...mentioning
confidence: 99%
See 1 more Smart Citation
“…Verubulin (derivative 14 ) had reached phase II of a trial for the treatment of glioblastoma, but it was halted due to cardiovascular toxicity. Recently, Li et al described a new potent tubulin inhibitor with a pyridine ring ( 16 ) showing nanomolar activity against some cancer cell lines ( Figure 3 ) [ 126 ].…”
Section: Are Anticancer Quinazoline Derivatives Good Candidates To Be...mentioning
confidence: 99%
“…Another effect of compounds that inhibit tubulin is the ability to inhibit cell migration and invasiveness. Thus, these agents prevent metastases in neoplastic diseases [ 125 , 126 ]. Some compounds act as multifunctional ligands.…”
Section: Are Anticancer Quinazoline Derivatives Good Candidates To Be...mentioning
confidence: 99%
“…Quinazolines can also exhibit apoptotic properties in cancerous cell lines ( Li et al, 2019 ) by means of acting as tubulin inhibitors. Tubulin is the structural protein of microtubules and plays a crucial role in cell division.…”
Section: Antitumor Effects Of Quinazoline Derivativesmentioning
confidence: 99%
“…Vinblastine is used in the treatment of Hodgkin’s disease, a form of lymphoid cancer, and vincristine is used clinically in combating children’s leukemia ( Lönnerholm et al, 2008 ). A series of new effective inhibitors from the group of 2,4-diamino-N,N-disubstituted quinazolines has been described as being effective anti-cancer compounds ( Figure 2 : 14) ( Li et al, 2019 ).…”
Section: Antitumor Effects Of Quinazoline Derivativesmentioning
confidence: 99%
“…Based on these data, this benzo[ e ]pyrimidine emerged as a good candidate for phase I and phase II clinical trials in patients with metastatic melanoma and glioblastoma multiforme [ 12 , 13 , 14 ]. Despite these investigations revealing some cardiotoxicity and leading to the suspension of clinical development in phase II [ 15 ], MPC-6827 remains an excellent model for the design of potential cytotoxic agents [ 16 ].…”
Section: Introductionmentioning
confidence: 99%