113934-27-3Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel benzimidazole amidines as potent multi-target inhibitors for the treatment of non-small cell lung cancer
Bistrovi?, Andrea,Krstulovi?, Luka,Harej, Anja,Grb?i?, Petra,Sedi?, Mirela,Ko?trun, Sanja,Paveli?, Sandra Kraljevi?,Baji?, Miroslav,Rai?-Mali?, Silvana
, p. 1616 - 1634 (2018)
A series of novel amidino 2-substituted benzimidazoles linked to 1,4-disubstituted 1,2,3-triazoles were synthesized by implementation of microwave and ultrasound irradiation in click reaction and subsequent condensation of thus obtained 4-(1,2,3-triazol-1
[HDBU][HSO4]-catalyzed facile synthesis of new 1,2,3-triazole-tethered 2,3-dihydroquinazolin-4[1H]-one derivatives and their DPPH radical scavenging activity
Akolkar, Satish V.,Khedkar, Vijay M.,Nagargoje, Amol A.,Pisal, Parshuram M.,Sangshetti, Jaiprakash N.,Shingate, Bapurao B.,Siddiqui, Madiha M.
, (2022/01/19)
A simple and efficient protocol has been developed for the synthesis of new1,2,3-triazole-2,3-dihydroquinazolin-4[1H]-one (DHQ) conjugates(6a?j) via ultrasound-assisted, solvent-free ionic liquid [HDBU][HSO4]-catalyzed reaction in good to excellent yields. This non-conventional, ultrasound-assisted route has taken the reactions over the conventional reflux method to provide good to excellent yields of the corresponding products (6a?j) in a very short time. In addition, mild reaction conditions, tolerance to functionalized substrates, ease of product isolation, prevention of its over oxidation and reusability of catalyst [HDBU][HSO4] are some key striking features of the methodology. The newly synthesized derivatives (6a?j) were screened for antioxidant activity using 1,1-diphenyl-2-picryl hydrazyl (DPPH) assay and are found to be a potent scavenger. The compounds 6b, 6c, 6d, 6e and 6i showed significant antioxidant activity. Molecular docking studies showed significant binding affinity in the active site of myeloperoxidase (MPO) enzyme and hence scavenged by inhibition of MPO. In silico ADMET and pharmacokinetic studies of the conjugates are very promising; a cumulative body of evidence suggests their medicinal value as a potential orally active drug candidate. Graphical abstract: [Figure not available: see fulltext.]
Synthesis, antiproliferative and antitrypanosomal activities, and DNA binding of novel 6-amidino-2-arylbenzothiazoles
Racané, Livio,Rep, Valentina,Kraljevi? Paveli?, Sandra,Grb?i?, Petra,Zonji?, Iva,Radi? Stojkovi?, Marijana,Taylor, Martin C.,Kelly, John M.,Rai?-Mali?, Silvana
, p. 1952 - 1967 (2021/09/03)
A series of 6-amidinobenzothiazoles, linked via phenoxymethylene or directly to the 1,2,3-triazole ring with a p-substituted phenyl or benzyl moiety, were synthesised and evaluated in?vitro against four human tumour cell lines and the protozoan parasite T
Selective CDK4/6 inhibition of novel 1,2,3-triazole tethered acridinedione derivatives induces G1/S cell cycle transition arrest via Rb phosphorylation blockade in breast cancer models
Praveenkumar,Gurrapu, Nirmala,Kolluri, Prashanth Kumar,Shivaraj,Subhashini,Dokala, Appaji
, (2021/10/12)
CDK4 & CDK6 are essential regulators of initial cell cycle phases and are always considered an exciting choice for anti-cancer therapy. In the present study, we presented the structure-based rational design & synthesis of a new class of 1,2,3-triazole tet
[Et3NH][HSO4] catalyzed solvent-free synthesis of new 1,2,3-triazolidene-indolinone derivatives
Nagargoje, Amol A.,Pisal, Parshuram M.,Raza, Akram K.,Shingate, Bapurao B.,Siddiqui, Madiha M.
, (2022/02/03)
A series of new 1,2,3-triazolidene-indolinone derivatives (17a-j) were designed and synthesized via [Et3NH] [HSO4] catalyzed solvent-free approach. The synthesis strongly relied on Knoevenagel condensation of 1,4-disubstituted 1,2,3-
Synthesis, characterization and photodynamic activity against bladder cancer cells of novel triazole-porphyrin derivatives
Gomes, Ana T.P.C.,Fernandes, Rosa,Ribeiro, Carlos F.,Tomé, Jo?o P.C.,Neves, Maria G.P.M.S.,da Silva, Fernando de C.,Ferreira, Vítor F.,Cavaleiro, José A.S.
, (2020/04/10)
Novel triazole-porphyrin derivatives (TZ-PORs) were synthesized through the Heck reaction and then incorporated into polyvinylpyrrolidone (PVP) micelles. After verifying that this incorporation did not compromise the photophysical and chemical features of
Synthesis and bioevaluation of α,α’-bis(1H-1,2,3-triazol-5-ylmethylene) ketones
Deshmukh, Tejshri R.,Krishna, Vagolu S.,Sriram, Dharmarajan,Sangshetti, Jaiprakash N.,Shingate, Bapurao B.
, p. 809 - 820 (2019/09/06)
Abstract: Curcumin is an active component of turmeric that has poor solubility, stability and bioavailability. The monocarbonyl curcumin analogues were modified from curcumin to achieve more stable and active compounds as compared to curcumin. Therefore,
Synthesis and Anticancer Activity of (E)-5-[(1-Aryl-1H-1,2,3-triazol-4-yl)methylene]thiazolidine-2,4-diones
Manikala, V. K.,Rao, V. M.
, p. 863 - 868 (2020/07/03)
Abstract: A novel series of 1,2,3-triazolylthiazolidinedione analogs have been synthesized by the condensation of the corresponding 1-aryl-1H-1,2,3-triazole-4-carbaldehydes with thiazolidine-2,4-dione in the presence of KOH. The title compounds were evaluated for their in vitro anticancer activity using MTT assay against four cancer cell lines: A549 (lung), HT-29 (colon), MCF-7 (breast), and A375 (melanoma). Most compounds displayed good anticancer activity, but hydroxy- and nitro-substituted derivatives showed higher activity than the others.
Alternative Route Triggering Multistep Spin Crossover with Hysteresis in an Iron(II) Family Mediated by Flexible Anion Ordering
Hagiwara, Hiroaki,Minoura, Ryo,Udagawa, Taro,Mibu, Ko,Okabayashi, Jun
, p. 9866 - 9880 (2020/07/24)
Multistep spin crossover (SCO) compounds have attracted much attention, since they can be great candidates for high-density multinary memory devices. The introduction of substituents, such as methyl (Me), chloro (Cl), bromo (Br), and methoxy (MeO) groups,
An allenylidene Au(i) catalyst derived from triazole units and its initial application
Chen, Bai-Ling,Zhang, Yuan,Lei, Ya-Ru,Wang, Hui-Ming,Chen, Zili
supporting information, p. 5787 - 5790 (2020/06/03)
An allenylidene Au(i) catalyst based on triazolylidene moieties, featuring the high s-donating ability (comparable to that of other NHC ligands) and largely enhanced p-accepting ability of its ligand, was developed for the first time. As compared with the
