Norharmane as a potential chemical entity for development of anticancer drugs

Self Cite

The naturally occurring phyco‐constituent nostocine A, bearing the pyrazolotriazine scaffold in its structural frame, belongs to an organic class of pharmacologically curious candidates with a remarkable anticancer activity. This review summarizes the chemistry of numerous synthetic strategies of demethylated nostocine as “nornostocine derivatives,” in which the substitutes are connected to a few functionalities with the pyrazolotriazine moiety at N‐1, C‐3, and C‐5 positions. These strategies may provide a framework to design and develop a novel potent anticancer drug candidate(s) with an augment of structure activity relationship related to anticancer activities.

Section: Introductionmentioning

confidence: 91%

Nornostocine congeners as potential anticancer drugs: An overview

Sahoo

Paidesetty

Padhy

2019

Self Cite

“…Concomitantly, most of the synthesized congeners are not qualified clinically. There is a prerequisite of the semi‐synthetic derived new potent candidate against the dreadful disease, cancer (Sahoo et al, 2019a, 2019b).…”

Section: Biological Actions Of Thymol Derivativesmentioning

confidence: 99%

The recent development of thymol derivative as a promising pharmacological scaffold

Sahoo

Paidesetty

Padhy

2021

Self Cite

Thymol (a phenol ring bearing active phytoconstituent) is a privileged scaffold, which is diversified in natural sources. This scaffold acts as an obligatory template for scheming and arriving at designing some newer drug‐molecules with potential biological activities. In the pharmacological perspective, the promising active sites of the scaffold are the positions C‐1, C‐4, and C‐6 of thymol that would be accountable for developing potent drug candidates. This review aims to explore the various synthetic routes and the structural‐activity relationship of thymol scaffold with suitable active pharmacophore sites.

“…Nitrogen‐containing heterocycles are recognized as the world's largest selling drugs just because of their flexibility toward different biological scaffolds and pharmaceutical products. Different nitrogen‐containing heterocycles like indole, indazole, quinolone, quinazoline, carbazole, quinoxaline, purine, pyrimidine, antipyrine (J. Sahoo et al, 2020), norharmane (C. R. Sahoo et al, 2019), oxadiazole, thiazole (Pal et al, 2014), so on, are some of the crucial building blocks for several synthetic and semi‐synthetic drugs. Among them, indazole and its derivatives had attracted many researchers over the past as it covers the broad area of medicinal and pharmaceutical activities.…”

Section: Introductionmentioning

confidence: 99%

A review on synthetic strategy, molecular pharmacology of indazole derivatives, and their future perspective

Mal

Malik

Mahapatra

et al. 2022

With different nitrogen-containing heterocyclic moieties, Indazoles earn one of the places among the top investigated molecules in medicinal research. Indazole, an important fused aromatic heterocyclic system containing benzene and pyrazole ring with a chemical formula of C 7 H 6 N 2 , is also called benzopyrazole. Indazoles consist of three tautomeric forms in which 1H-tautomers (indazoles) and 2H-tautomers (isoindazoles) exist in all phases. The tautomerism in indazoles greatly influences synthesis, reactivity, physical and even the biological properties of indazoles.The thermodynamic internal energy calculation of these tautomers points view 1H-indazole as the predominant and stable form over 2H-indazole. The natural source of indazole is limited and exists in alkaloidal nature (i.e., nigellidine, nigeglanine, nigellicine, etc.) found from Nigella plants. Some of the FDA-approved drugs like Axitinib, Entrectinib, Niraparib, Benzydamine, and Granisetron are being used to treat renal cell cancer, non-small cell lung cancer (NSCLC), epithelial ovarian cancer, chronic inflammation, chemotherapy-induced nausea, vomiting, and many more uses. Besides all these advantages regarding its biological activity, the main issue about indazoles is the less abundance in plant sources, and their synthetic derivatives also often face problems with low yield. In this review article, we discuss its chemistry, tautomerism along with their effects, different schematics for the synthesis of indazole derivatives, and their different biological activities.