Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase

Peng, Fan-Wei; Wu, Tong; Ren, Ziwei; Xue, Jia‐Yu; Shi, Lei

doi:10.1016/j.bmcl.2015.10.006

Cited by 37 publications

(16 citation statements)

References 44 publications

(21 reference statements)

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“…45 Unfortunately, the increased resistance rates against VEGR inhibitors terminated their success, so many strategies to overcome this resistance were adopted, 46 one of them is to develop chimeric VEGFR/HDAC inhibitors, especially when there is great synergy between RTK and HDAC inhibitors as previously mentioned. 47 Peng et al 48 in 2015 developed a dual VEGFR/HDAC inhibitor by combining pharmacophores of two reference drugs, vandetanib (38), which acts as a VEGFR inhibitor, and SAHA, which acts as an HDAC inhibitor, to yield series of chimeric compounds with the most potent compound 38a ( Figure 10). Hybrid 38a showed HDAC isoform and kinase selectivity as well as improving its physiochemical properties.…”

Section: Chimeric Bcr-abl Tyrosine Kinase-hdac Inhibitorsmentioning

confidence: 99%

Chimeric HDAC inhibitors: Comprehensive review on the HDAC‐based strategies developed to combat cancer

Hesham

Lasheen

Abouzid

2018

Medicinal Research Reviews

120

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Recently, molecular hybridization paradigm became an interesting and smart way to defeat the multifaceted cancer disease by a single molecular entity that acts via several mechanisms just like a magic bullet. Also, HDAC is an important epigenetic target in drug discovery, and the HDAC inhibitors showed successful pattern as cytotoxic agents. Because of their flexible structure activity relationship, it was easy to link them to other anticancer scaffolds. So, many dual action HDAC inhibitors have been developed and most of these hybrids have higher potency than the constituting parents in fighting of the cancer cells. This review describes potential applications of chimeric HDAC inhibitors, which simultaneously modulate not only HDAC but also multiple targets, in treatment of relapsing and drug-resistant cancers. We have nearly collected most of the reported dual action HDAC inhibitors yet to provide a comprehensive guide for the drug discovery process for developing more efficient anticancer agents.

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Section: Chimeric Bcr-abl Tyrosine Kinase-hdac Inhibitorsmentioning

confidence: 99%

Chimeric HDAC inhibitors: Comprehensive review on the HDAC‐based strategies developed to combat cancer

Hesham

Lasheen

Abouzid

2018

Medicinal Research Reviews

120

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“…Источником формирования выборок для QSAR-моделирования послужили публикации [Peng et al, 2015;Peng et al, 2016], в каждой из которых приведены экспериментальные значения для соединений, содержащих одновременно N-фенил-4-аминохиназолин и гидроксамовую кислоту, в отношении трех видов активностей: 1) ингибирование HDAC (изоформы); 2) ингибирование VEGFR-2; 3) ингибирование роста клеток рака легкого MCF-7. В настоящее время данная клеточная линия активно используется при исследовании in vitro цитотоксичности противоопухолевых лекарственных средств.…”

Section: методыunclassified

“…В настоящее время данная клеточная линия активно используется при исследовании in vitro цитотоксичности противоопухолевых лекарственных средств. С целью расширения структурного пространства для QSAR-моделирования выборки из двух указанных публикаций [Peng et al, 2015;Peng et al, 2016] объединены по соответствующим видам активностей в общие выборки, что, с нашей точки зрения, допустимо, поскольку имеющиеся в публикациях результаты получены одними авторами в одинаковых условиях и значения трех видов активностей для референтных структур (Вандетаниб и Вориностат) практически совпадают.…”

Section: методыunclassified

“…(1) Экспериментальные значения и структуры соединений, экспортированные из публикаций [Peng et al, 2015;Peng et al, 2016], приведены в таблице 1.…”

Section: методыunclassified

“…Относительно недавно опубликован ряд примеров бифункциональных VEGFR-2/HDACингибиторов [Peng et al, 2015;Peng et al, 2016].…”

Section: Introductionunclassified

See 2 more Smart Citations

Quantitative analysis of "structure - anticancer activity" and rational molecular design of bi-functional VEGFR-2/HDAC-inhibitors

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Harnessing pyrimidine as a building block for histone deacetylase inhibitors

Badran

Abbas

Fujita

et al. 2023

Archiv der Pharmazie

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Histone deacetylase (HDAC) inhibitors are well‐established multifaceted bioactive agents against tumors and neurodegenerative disorders. Pyrimidine and its fused and substituted derivatives were employed as a surface recognition moiety of HDAC inhibitors. De facto, the literature was loaded with different success stories of pyrimidine‐based HDAC inhibitors that garnered much interest. Provoked by our continuous interest in HDAC inhibitors, we summarized and elaborated on the successful harnessing of the pyrimidine scaffold in this regard. Furthermore, we dissect our perspective that may guide medicinal chemists for an effective future design of more active chemotherapeutic agents with potential clinical applications.

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Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase

Cited by 37 publications

References 44 publications

Chimeric HDAC inhibitors: Comprehensive review on the HDAC‐based strategies developed to combat cancer

Chimeric HDAC inhibitors: Comprehensive review on the HDAC‐based strategies developed to combat cancer

Quantitative analysis of "structure - anticancer activity" and rational molecular design of bi-functional VEGFR-2/HDAC-inhibitors

Harnessing pyrimidine as a building block for histone deacetylase inhibitors

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