Oxazole and Thiazole Analogs of Sulindac for Cancer Prevention

Mathew, Biji; Hobrath, Judith V.; Connelly, Michele; Guy, R. Kiplin; Reynolds, Robert C.

doi:10.4155/fmc-2017-0182

Cited by 12 publications

(4 citation statements)

References 45 publications

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“…The presence of 4‐methylthiophenyl substituent provided optimal anticancer activity, however its replacement with methoxyphenyl substituent considerably lowered the metabolic susceptibility of the parent compound. Similarly, the amide analogue 43 (Figure 9) demonstrated a considerable activity when appended with N,N‐dimethylaminoethyl substituent; and the thiazole analogues displayed higher activities compared to the oxazole ring containing compounds [40] …”

Section: Anticancer Properties Of Indane and Its Analoguesmentioning

confidence: 93%

Medicinal Chemistry of Indane and Its Analogues: A Mini Review

Prasher

Sharma

2021

ChemistrySelect

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‘Indane′ and its analogues indene, 1‐indenone, and 1,3‐indandione present an attractive biological profile for the rational development of therapeutic molecules. The indane/ indene moieties contain aromatic benzene ring fused with an aliphatic cyclopentane/ cyclopentene ring, which provides a rigid bicyclic ring‐framework enriched with diverse chemical properties. The multifarious possibilities for varying the substituent pattern on these fused ring systems enable the extensive appraisal of structure‐activity relationship analysis of rationally designed therapeutic molecules deliberated at their molecular targets. Indane analogues serve as useful scaffolds for the development of efficacious pharmaceuticals and commercial drugs, including Indinavir, Sulindac, and donepezil; whereas the pharmacophores based on indane moiety such as Aminoindanes and Indanedione contribute towards the development of neuroleptics and neuroprotective molecules. Similarly, the Indane‐carboxamide derivatives present a robust candidature as CGRP receptor antagonists, while substituted Indane and its analogue Indene present a privileged profile for the development of anticancer therapeutics by targeting the multifaceted oncologic pathways. Besides, the indane natural product scaffolds serve as perspective drug candidates with marked therapeutic properties. The present review summarizes the medicinal chemistry aspects of indane nucleus and its analogues as anticancer, anti‐inflammatory, and neuroprotective agents for the coherent development of impending therapeutics.

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Section: Anticancer Properties Of Indane and Its Analoguesmentioning

confidence: 93%

Medicinal Chemistry of Indane and Its Analogues: A Mini Review

Prasher

Sharma

2021

ChemistrySelect

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“…34,35 Other sulindac analogs are active but have not been evaluated in humans. [36][37][38] Sulindac and Erlotinib. The combination of sulindac 300 mg daily and erlotinib, an oral tyrosine kinase inhibitor with anti-EGFR activity, 75 mg daily for 6 months was evaluated versus placebo in 92 patients with FAP.…”

Section: Sulindac and Sulindac-based Combinationsmentioning

confidence: 99%

Chemoprevention in hereditary digestive neoplasia: A comprehensive review

Chevalier,

Benamouzig

2023

Therap Adv Gastroenterol

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Hereditary syndromes, such as familial adenomatous polyposis (FAP), MUTYH polyposis or Lynch syndrome, are particularly predisposing to the development of colorectal cancer. These situations have necessitated the development of adapted prevention strategies based largely on reinforced endoscopic surveillance and the search for complementary prevention strategies. This is the case for chemoprevention, which is the long-term administration of chemical agents limiting carcinogenesis, used as primary or secondary prophylaxis. The aim of this review is to present the available literature and the latest advances in chemoprevention in patients with FAP or MUTYH and other polyposis as well as in patients with Lynch syndrome. The main conclusions of the few available guidelines in these situations are also discussed.

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“…Oxazole and its derivatives are used in treatment of various types of illness [8] . Oxazole shows numerous biological activities such as anti-bacterial [9,10] , antifungal [11,12] , agonist of free fatty acid receptor (GPR40) [13] , highly selective histone deacetylase 6 (HDAC6) [14] , anticancer [15,16] , vegetative growth factor [17] , anti-tubercular, anti-leishmanial [18] , antiprotozoal [19] and anti-inflammatory [20] . Apart from these pharmacological activities, oxazole derivatives can also be used as anti-corrosive agent for stainless steel, dyes [21] , anti-ageing [22] , antioxidant [23] , metabolism enhancing agent [24] , pesticides and herbicides [6] .…”

Section: Pharmacological Activities Of Oxazolementioning

confidence: 99%

Recent Development and Green Approaches for Synthesis of Oxazole Derivatives: A Review

Joshi¹,

Choudhary²

2022

IJPS

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Green Synthetic Methods Synthesis of Oxazole DerivativesThis review compiles green synthetic methods intended for the synthesis of oxazole derivatives. Oxazoles are a class of compounds with a wide range of biological activities. The application and biological activity of oxazoles is highly dependent on their structure. Now-a-days, scientists have been performing the synthesis of oxazole derivatives. High demands in synthesis often result in the production of various hazardous chemical substances. So, to minimize the production of toxic chemical substances, green synthetic approaches are used in this manner. Green synthesis covers different synthetic approaches, including the application of microwave techniques, ultrasound, ionic liquids, deep-eutectic solvents, the use of catalysts and continuous flow synthesis. In this review, the authors mentioned that not only these green synthetic approaches reduce the formation and utilisation of toxic chemicals, but there is an increase in the reaction performance that enhances the product yields, purity, post-synthetic processes and energy consumption when compared to conventional methods. Due to the biological and pharmacological significance of oxazoles and the demands of decreasing toxic solvents, catalysts, and energy consumption, this article gives a full literature survey on the significance of green synthetic methods in oxazole synthesis. It contains a literature survey over the period from 2010-2020. The emphasis of this article is its comprehensive literature survey on oxazole, which is helpful for the researchers working on the oxazole scaffold and gaining information on the green synthetic approaches to their synthesis.

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Oxazole and Thiazole Analogs of Sulindac for Cancer Prevention

Cited by 12 publications

References 45 publications

Medicinal Chemistry of Indane and Its Analogues: A Mini Review

Medicinal Chemistry of Indane and Its Analogues: A Mini Review

Chemoprevention in hereditary digestive neoplasia: A comprehensive review

Recent Development and Green Approaches for Synthesis of Oxazole Derivatives: A Review

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