New antiproliferative agents derived from tricyclic 3,4‐dihydrobenzo[4,5]imidazo[1,2‐a][1,3,5]triazine scaffold: Synthesis and pharmacological effects
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200295
Abstract: A series of novel 3,4‐dihydrobenzo[4,5]imidazo[1,2‐a][1,3,5]triazine (BIT) derivatives were designed and synthesized. In vitro antiproliferative activity was detected toward two human colorectal adenocarcinoma cell lines (CaCo‐2 and HT‐29) and one human dermal microvascular endothelial cell line… read more here.
Keywords: new antiproliferative; imidazo triazine; dihydrobenzo imidazo; antiproliferative agents ... See more keywords
New 1,3,4‐oxadiazole‐chalcone/benzimidazole hybrids as potent antiproliferative agents
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DOI: 10.1002/ardp.202200357
Abstract: A series of new 1,3,4‐oxadiazole‐chalcone/benzimidazole hybrids 9a–o and 10a–k were designed and synthesized as potential antiproliferative agents. Hybrids 9a–o exhibited remarkable antiproliferative activities on different NCI‐60 cell lines in a single‐dose assay. The antiproliferative activities… read more here.
Keywords: chalcone benzimidazole; antiproliferative agents; new oxadiazole; benzimidazole hybrids ... See more keywords
Metal NHC Complexes with Naphthalimide Ligands as DNA‐Interacting Antiproliferative Agents
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DOI: 10.1002/cmdc.201600557
Abstract: Naphthalimide‐based N‐heterocyclic carbene (NHC) complexes of the type [(1,5‐cyclooctadiene)(NHC)RhCl)] (4 a–c), [(p‐cymene)(NHC)RuCl2)] (5 a–c), and [(NHC)CuBr] (6 a–c) were synthesized and investigated as antiproliferative agents that target DNA. The cytotoxic effects were largely driven by the naphthalimide structure,… read more here.
Keywords: metal nhc; complexes naphthalimide; antiproliferative agents; ligands dna ... See more keywords
8-Ethynylxanthines as promising antiproliferative agents, angiogenesis inhibitors, and calcium channel activity modulators
Sign Up to like & getrecommendations! Published in 2020 at "Chemistry of Heterocyclic Compounds"
DOI: 10.1007/s10593-020-02730-4
Abstract: Synthetic procedures for the preparation of 8-ethynylxanthines by treating 8-bromocaffeine and 8-bromopentoxifylline with terminal acetylenes were elaborated. Certain ethynylxanthine derivatives exhibit high in vitro antiproliferative activity against a panel of cancer cell lines, matrix metalloproteinase… read more here.
Keywords: ethynylxanthines promising; antiproliferative agents; agents angiogenesis; channel ... See more keywords
Design, synthesis and biological evaluation of some novel benzothiazole/benzoxazole and/or benzimidazole derivatives incorporating a pyrazole scaffold as antiproliferative agents.
Sign Up to like & getrecommendations! Published in 2017 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2017.07.007
Abstract: In an aim at developing new antiproliferative agents, new series of benzothiazole/benzoxazole and/or benzimidazole substituted pyrazole derivatives 11a-c, 12a-c and 13a-c were prepared and evaluated for their antiproliferative activity against breast carcinoma (MCF-7) and non-small… read more here.
Keywords: benzoxazole benzimidazole; antiproliferative agents; cox; benzothiazole benzoxazole ... See more keywords
Benzothiopyranoindole- and pyridothiopyranoindole-based antiproliferative agents targeting topoisomerases.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.01.015
Abstract: New benzothiopyranoindoles (5a-l) and pyridothiopyranoindoles (5m-t), featuring different combinations of substituents (H, Cl, OCH3) at R2-R4 positions and protonatable R1-dialkylaminoalkyl chains, were synthesized and biologically assayed on three human tumor cell lines, showing significant antiproliferative… read more here.
Keywords: benzothiopyranoindole pyridothiopyranoindole; targeting topoisomerases; pyridothiopyranoindole based; antiproliferative agents ... See more keywords
Selenocoumarins as new multitarget antiproliferative agents: Synthesis, biological evaluation and in silico calculations.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.06.073
Abstract: Herein we report a straightforward preparation of new antiproliferative agents based on the hybridization of a coumarin skeleton and an organoselenium motif. Three families were obtained: isoselenocyanate, selenocarbamates and selenoureas. The main purpose of these… read more here.
Keywords: selenocoumarins new; new multitarget; coumarin; silico calculations ... See more keywords
Lipase-Catalyzed Synthesis and Biological Evaluation of N-Picolineamides as Trypanosoma cruzi Antiproliferative Agents.
Sign Up to like & getrecommendations! Published in 2023 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00425
Abstract: In our search for new safe antiparasitic agents, an enzymatic pathway was applied to synthesize a series of N-pyridinylmethyl amides derived from structurally different carboxylic acids. Thirty derivatives, including 11 new compounds, were prepared through… read more here.
Keywords: synthesis biological; lipase catalyzed; biological evaluation; antiproliferative agents ... See more keywords
Synthesis of Arylpiperazine Derivatives as Protease Activated Receptor 1 Antagonists and Their Evaluation as Antiproliferative Agents.
Sign Up to like & getrecommendations! Published in 2017 at "Anti-cancer agents in medicinal chemistry"
DOI: 10.2174/1871520616666160926120904
Abstract: BACKGROUND Protease activated receptor-1 (PAR1) is a G-coupled receptor activated by α-thrombin and other proteases. Several reports have demonstrated the PAR1 involvement in tumorigenesis and tumor progression. In order to investigate on potential use of… read more here.
Keywords: par1; arylpiperazine derivatives; antiproliferative agents; protease activated ... See more keywords
Development of 1,2,3-Triazole-Based Sphingosine Kinase Inhibitors and Their Evaluation as Antiproliferative Agents
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DOI: 10.3390/ijms18112332
Abstract: Two series of N-(aryl)-1-(hydroxyalkyl)pyrrolidine-2-carboxamides (2a–2g and 3a–3g) and 1,4-disubstituted 1,2,3-triazoles (5a–5h and 8a–8h) were synthesized. All the compounds, containing a lipophilic tail and a polar headgroup, were evaluated as sphingosine kinase (SphK) inhibitors by assessing… read more here.
Keywords: development triazole; sphingosine kinase; based sphingosine; antiproliferative agents ... See more keywords
Synthesis of Bisphenol Neolignans Inspired by Honokiol as Antiproliferative Agents
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DOI: 10.3390/molecules25030733
Abstract: Honokiol (2) is a natural bisphenol neolignan showing a variety of biological properties, including antitumor activity. Some studies pointed out 2 as a potential anticancer agent in view of its antiproliferative and pro-apoptotic activity towards… read more here.
Keywords: bisphenol; neolignans inspired; antiproliferative agents; bisphenol neolignans ... See more keywords