Recent Progress in Anticancer Agents Incorporating Pyrazole Scaffold

Mor, Satbir; Khatri, Mohini; Punia, Ravinder; Sindhu, Suchita

doi:10.2174/1389557521666210325115218

Cited by 40 publications

(34 citation statements)

References 235 publications

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“…There are many reviews that present and demonstrate the anticancer potential of the pyrazole ring, unfused or fused in structures like indazole or pyrazolopyrimidines, but these works present only on the active derivatives [ 32 , 33 , 34 , 35 , 36 , 37 , 38 ]. The researchers tend to publish only works with positive results in order to maximize their scientific impact.…”

Section: Discussionmentioning

confidence: 99%

Quantitative and Qualitative Analysis of the Anti-Proliferative Potential of the Pyrazole Scaffold in the Design of Anticancer Agents

Nițulescu

2022

Molecules

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The current work presents an objective overview of the impact of one important heterocyclic structure, the pyrazole ring, in the development of anti-proliferative drugs. A set of 1551 pyrazole derivatives were extracted from the National Cancer Institute (NCI) database, together with their growth inhibition effects (GI%) on the NCI’s panel of 60 cancer cell lines. The structures of these derivatives were analyzed based on the compounds’ averages of GI% values across NCI-60 cell lines and the averages of the values for the outlier cells. The distribution and the architecture of the Bemis–Murcko skeletons were analyzed, highlighting the impact of certain scaffold structures on the anti-proliferative effect’s potency and selectivity. The drug-likeness, chemical reactivity and promiscuity risks of the compounds were predicted using AMDETlab. The pyrazole ring proved to be a versatile scaffold for the design of anticancer drugs if properly substituted and if connected with other cyclic structures. The 1,3-diphenyl-pyrazole emerged as a useful scaffold for potent and targeted anticancer candidates.

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Section: Discussionmentioning

confidence: 99%

Quantitative and Qualitative Analysis of the Anti-Proliferative Potential of the Pyrazole Scaffold in the Design of Anticancer Agents

Nițulescu

2022

Molecules

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“…ethylbenzthiazoline-6-sulphonic acid)] method. In that comparison was done by ascorbic acid as standard (Figure 11) [54,55].…”

Section: Applications Of Pyrazole Scaffoldmentioning

confidence: 99%

Pyrazole Scaffold: Strategies toward the Synthesis and Their Applications

Nandurkar¹,

Danao²,

Rokde³

et al. 2023

Strategies for the Synthesis of Heterocycles and Their Applications

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Pyrazoles have a wide range of applications in medicinal chemistry, drug discovery, agrochemistry, coordination chemistry, and organometallic chemistry. Their popularity has skyrocketed since the early 1990s. Basically, Pyrazole (C3H3N2H) is a simple doubly unsaturated five membered heterocyclic aromatic ring molecule comprising two nitrogen (N) atoms at positions 1- and 2- and three carbon (C) atoms. Pyrazole nucleus is synthesized with various strategies such as multicomponent approach, dipolar cycloadditions, cyclocondensation of hydrazine with carbonyl system, using heterocyclic system and multicomponent approach. A special emphasis is placed on a thorough examination of response processes. Furthermore, the reasons for the increasing popularity of pyrazoles in several fields of science are examined. Pyrazoles have recently been the focus of many techniques, mostly because of how frequently they are used as scaffolds in the synthesis of bioactive chemicals and reactions in various media. The goal of this chapter is to discuss the current developments in synthetic techniques and biological activity related to pyrazole derivatives. The many pharmacological functions of the pyrazole moiety and different synthesis techniques were discussed. This chapter has summarized novel strategies and wide applications of pyrazole scaffold.

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“…On the other hand, pyrazolopyridine derivatives are another interesting scaffold and have appeared in many medicinal chemistry programs due to their great variety of biological activities. These derivatives possess antimicrobial [ 26 , 27 ], antioxidant [ 28 ], anxiolytic [ 29 ], anticancer [ 30 , 31 ], antiproliferative [ 32 ], cytotoxic [ 33 ], antileishmanial [ 34 , 35 ], and antimalarial [ 36 ] properties, as well as phosphodiesterrase (PDE4) [ 37 ], kinase [ 38 ], and angiogenesis [ 39 ] inhibitory activities.…”

Section: Introductionmentioning

confidence: 99%

Pyrazolo[4,3-c]pyridine Sulfonamides as Carbonic Anhydrase Inhibitors: Synthesis, Biological and In Silico Studies

Angeli

Карцев²,

Petrou

et al. 2022

Pharmaceuticals

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Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the essential reaction of CO2 hydration in all living organisms, being actively involved in the regulation of a plethora of patho-/physiological conditions. A series of chromene-based sulfonamides were synthesized and tested as possible CA inhibitors. On the other hand, in microorganisms, the β- and γ- classes are expressed in addition to the α- class, showing substantial structural differences to the human isoforms. In this scenario, not only human but also bacterial CAs are of particular interest as new antibacterial agents with an alternative mechanism of action for fighting the emerging problem of extensive drug resistance afflicting most countries worldwide. Pyrazolo[4,3-c]pyridine sulfonamides were synthesized using methods of organic chemistry. Their inhibitory activity, assessed against the cytosolic human isoforms hCA I and hCA II, the transmembrane hCA IX and XII, and β- and γ-CAs from three different bacterial strains, was evaluated by a stopped-flow CO2 hydrase assay. Several of the investigated derivatives showed interesting inhibition activity towards the cytosolic associate isoforms hCA I and hCA II, as well as the 3β- and 3γ-CAs. Furthermore, computational procedures were used to investigate the binding mode of this class of compounds within the active site of hCA IX. Four compounds (1f, 1g, 1h and 1k) were more potent than AAZ against hCA I. Furthermore, compound 1f also showed better activity than AAZ against the hCA II isoform. Moreover, ten compounds out of eleven appeared to be very potent against the γ-CA from E.coli, with a Ki much lower than that of the reference drug. Most of the compounds showed better activity than AAZ against hCA I as well as the γ-CA from E.coli and the β-CA from Burkholderia pseudomallei (BpsCAβ). Compounds 1f and 1k showed a good selectivity index against hCA I and hCA XII, while 1b was selective against all 3β-CA isoforms from E.coli, BpsCA, and VhCA and all 3γ-CA isoforms from E.coli, BpsCA and PgiCA.

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Recent Progress in Anticancer Agents Incorporating Pyrazole Scaffold

Cited by 40 publications

References 235 publications

Quantitative and Qualitative Analysis of the Anti-Proliferative Potential of the Pyrazole Scaffold in the Design of Anticancer Agents

Quantitative and Qualitative Analysis of the Anti-Proliferative Potential of the Pyrazole Scaffold in the Design of Anticancer Agents

Pyrazole Scaffold: Strategies toward the Synthesis and Their Applications

Pyrazolo[4,3-c]pyridine Sulfonamides as Carbonic Anhydrase Inhibitors: Synthesis, Biological and In Silico Studies

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