Synthesis and in vitro anticancer activity of the first class of dual inhibitors of REV-ERBβ and autophagy

E Torrente, C Parodi, L Ercolani, C De Mei… - Journal of Medicinal …, 2015 - ACS Publications
… autophagy, may provide a strategy for development of novel anticancer agents with an …
of antitumor activity and potential side effects associated with our dual inhibitors. This will be …

[HTML][HTML] The anti-cancer activity of the mTORC1/2 dual inhibitor XL388 in preclinical osteosarcoma models

YR Zhu, X Zhou, L Zhu, C Yao, JF Fang, F Zhou… - Oncotarget, 2016 - ncbi.nlm.nih.gov
dual inhibitor has displayed anti-tumor activity in preclinical cancer models [14]. In the current
study, we explored its activity … the anti-cancer activity by a number of mTOR inhibitors [18]. …

Optimization of the natural product calothrixin A to discover novel dual topoisomerase I and II inhibitors with improved anticancer activity

X Yang, ZP Wang, S Xiang, D Wang… - Journal of Medicinal …, 2022 - ACS Publications
… C1) groups caused dramatic drops in anticancer activities, while the replacement of the N,N…
activities as compared to CAA. In addition, C5 displayed dual Topo I and II inhibitory activities

Enhanced Anticancer Activity of PF-04691502, a Dual PI3K/mTOR Inhibitor, in Combination With VEGF siRNA Against Non–small-cell Lung Cancer

L Espana-Serrano, MB Chougule - Molecular Therapy-Nucleic Acids, 2016 - cell.com
… and the PI3K/mTOR dual inhibitor PF-04691502. We analyzed the anticancer effect of siRNA
… siRNA VEGF potentiates the PF-04691502 anticancer activity against non–small-cell lung …

Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity

C Cheng, F Yun, S Ullah, Q Yuan - European Journal of Medicinal …, 2020 - Elsevier
… In summary, we have successfully designed and synthesized novel dual HDAC/CDK
inhibitors. The representative compounds (7c and 14a) displayed potent antiproliferative activities

Dual target inhibitors based on EGFR: Promising anticancer agents for the treatment of cancers (2017-)

L Hu, M Fan, S Shi, X Song, F Wang, H He… - European Journal of …, 2022 - Elsevier
… The conjugated N–N–S or N–N–O tridentate ligand system of thiosemicarbazides and
semicarbazones were considered as essential moieties for anticancer activities through inhibiting

Anti-cancer activity of 2, 4-disubstituted thiophene derivatives: dual inhibitors of lipoxygenase and cyclooxygenase

KS Rakesh, S Jagadish, TR Swaroop… - Medicinal …, 2015 - ingentaconnect.com
2,4-Disubstituted thiophene derivatives were synthesized and assessed for antiinflammatory
and anti-cancer activities by targeting two important enzymes of the arachidonic acid …

Synergistic anti-cancer activity of CDK4/6 inhibitor palbociclib and dual mTOR kinase inhibitor MLN0128 in pRb-expressing ER-negative breast cancer

T Yamamoto, N Kanaya, G Somlo, S Chen - Breast cancer research and …, 2019 - Springer
inhibitor palbociclib and the dual mTOR kinase inhibitor MLN0128 had synergistic anti-cancer
activity … This drug combination has a potent synergistic inhibitory effect on pRb-expressing …

Dual or multi-targeting inhibitors: The next generation anticancer agents

NM Raghavendra, D Pingili, S Kadasi, A Mettu… - European journal of …, 2018 - Elsevier
… Apitolisib effectively inhibits PI3Kα with IC 50 of picomolar range and mTOR with IC 50 of
subnanomolar range, it also exhibited excellent in vivo anticancer activity by sustained …

Novel pyrazolo[3,4-d]pyrimidines: design, synthesis, anticancer activity, dual EGFR/ErbB2 receptor tyrosine kinases inhibitory activity, effects on cell cycle profile and …

M Maher, AE Kassab, AF Zaher… - … of enzyme inhibition and …, 2019 - Taylor & Francis
… for their anticancer activity against 60 human tumour cell lines by NCI (USA). Compound 7d
proved prominent anticancer activity. It showed 1.6-fold more potent anti-proliferative activity