Synthesis and evaluation of in vitro cytotoxic effects of triazol/spiroindolinequinazolinedione, triazol/indolin-3-thiosemicarbazone and triazol/thiazol-indolin-2-one conjugates

Nazari, Saeed; Safari, Fatemeh; Mamaghani, Mohammad Barasm; Bazgir, Ayoob

doi:10.1007/s40199-020-00364-7

Cited by 14 publications

(7 citation statements)

References 39 publications

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“…In 2020, Nazari and co-workers [ 42 ] reported the synthesis of triazol/spiroindolinequinazoline dione, triazol/indolin-3-thiosemicarbazone, and triazol/thiazol-indolin-2-one conjugates for their antitumor activity ( Figure 3 b). The furnished derivatives were assessed for their in vitro cytotoxic potential against cancer lines, namely, A375, PC3, LNCaP, MDA, MB231, and normal cell HDF.…”

Section: Development Of Isatin Derivatives As Promising Therapeutic A...mentioning

confidence: 99%

Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

Cheke¹,

Patil²,

Firke

et al. 2022

Pharmaceuticals

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Isatin (1H indole 2, 3-dione) is a heterocyclic, endogenous lead molecule recognized in humans and different plants. The isatin nucleus and its derivatives are owed the attention of researchers due to their diverse pharmacological activities such as anticancer, anti-TB, antifungal, antimicrobial, antioxidant, anti-inflammatory, anticonvulsant, anti-HIV, and so on. Many research chemists take advantage of the gentle structure of isatins, such as NH at position 1 and carbonyl functions at positions 2 and 3, for designing biologically active analogues via different approaches. Literature surveys based on reported preclinical, clinical, and patented details confirm the multitarget profile of isatin analogues and thus their importance in the field of medicinal chemistry as a potent chemotherapeutic agent. This review represents the recent development of isatin analogues possessing potential pharmacological action in the years 2016–2020. The structure–activity relationship is also discussed to provide a pharmacophoric pattern that may contribute in the future to the design and synthesis of potent and less toxic therapeutics.

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Section: Development Of Isatin Derivatives As Promising Therapeutic A...mentioning

confidence: 99%

Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

Cheke¹,

Patil²,

Firke

et al. 2022

Pharmaceuticals

View full text Add to dashboard Cite

show abstract

“…[125] The SAR illustrated that substituents at N-1 and C-3 and were nontoxic (IC 50 : >100 µM) toward normal HDF cells. [126] The antiproliferative SAR of 1,2,3-triazole-isatin hybrids 101…”

Section: Indole-pyridine/quinoline Hybridsmentioning

confidence: 99%

The anti‐breast cancer therapeutic potential of 1,2,3‐triazole‐containing hybrids

Song,

Zhang,

Zhang

et al. 2023

Archiv der Pharmazie

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Breast cancer, as one of the most common invasive malignancies and the leading cause of cancer‐related deaths in women globally, poses a significant challenge in the world health system. Substantial advances in diagnosis and treatment have significantly improved the survival rate of breast cancer patients, but the number of incidences and deaths of breast cancer are projected to increase by 40% and 50%, respectively, by 2040. Chemotherapy is one of the principal treatments for breast cancer therapy, but multidrug resistance and severe side effects remain the major obstacles to the success of treatment. Hence, there is a vital need to develop novel chemotherapeutic agents to combat this deadly disease. 1,2,3‐Triazole, which can be effectively constructed by click chemistry, not only can serve as a linker to connect different anti‐breast cancer pharmacophores but also is a valuable pharmacophore with anti‐breast cancer potential and favorable properties such as hydrogen bonding, moderate dipole moment, and enhanced water solubility. Particularly, 1,2,3‐triazole‐containing hybrids have demonstrated promising in vitro and in vivo anti‐breast cancer potential against both drug‐sensitive and drug‐resistant forms and possessed excellent selectivity by targeting different biological pathways associated with breast cancer, representing privileged scaffolds for the discovery of novel anti‐breast cancer candidates. This review concentrates on the latest advancements of 1,2,3‐triazole‐containing hybrids with anti‐breast cancer potential, including work published between 2020 and the present. The structure–activity relationships (SARs) and mechanisms of action are also reviewed to shed light on the development of more effective and multitargeted candidates.

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“…Imine compounds have a wide range of applications such as catalysts [ 1 ], dyes [ 2 ], components in the polymer industry [ 3 ], and stabilizers [ 4 ]. Moreover, they have proven potent biological actions including anti-bacterial [ 5 ], anti-fungal [ 6 ], anti-inflammatory [ 7 ], anti-cancer [ 8 ], and anti-tumor activities [ 9 ] which make them a very important class of organic compounds in pharmaceutical and medicinal chemistry, as imine groups, thiosemicarbazone, and semicarbazone have no cytotoxicity on normal cells both in vivo and in vitro [ 10 , 11 , 12 , 13 ].…”

Section: Introductionmentioning

confidence: 99%

Exploring Novel Pyridine Carboxamide Derivatives as Urease Inhibitors: Synthesis, Molecular Docking, Kinetic Studies and ADME Profile

et al. 2022

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The rapid development of resistance by ureolytic bacteria which are involved in various life-threatening conditions such as gastric and duodenal cancer has induced the need to develop a new line of therapy which has anti-urease activity. A series of pyridine carboxamide and carbothioamide derivatives which also have some novel structures were synthesized via condensation reaction and investigated against urease for their inhibitory action. Among the series, 5-chloropyridine-2 yl-methylene hydrazine carbothioamide (Rx-6) and pyridine 2-yl-methylene hydrazine carboxamide (Rx-7) IC50 = 1.07 ± 0.043 µM, 2.18 ± 0.058 µM both possessed significant activity. Furthermore, molecular docking and kinetic studies were performed for the most potent inhibitors to demonstrate the binding mode of the active pyridine carbothioamide with the enzyme urease and its mode of interaction. The ADME profile also showed that all the synthesized molecules present oral bioavailability and high GI absorption.

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Synthesis and evaluation of in vitro cytotoxic effects of triazol/spiroindolinequinazolinedione, triazol/indolin-3-thiosemicarbazone and triazol/thiazol-indolin-2-one conjugates

Cited by 14 publications

References 39 publications

Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

The anti‐breast cancer therapeutic potential of 1,2,3‐triazole‐containing hybrids

Exploring Novel Pyridine Carboxamide Derivatives as Urease Inhibitors: Synthesis, Molecular Docking, Kinetic Studies and ADME Profile

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