Evidence map›Paper›PMID 39501943›Full record

ArticleAnti-cancer agents in medicinal chemistry2025

Synthesis of Chromene-linked Bis-indole Derivatives as Selective Tumor-associated Carbonic Anhydrase IX Inhibitors.

Priti Singh, Sridhar Goud Nerella, Baijayantimala Swain, Andrea Angeli, Samreen Kausar, Qasim Ullah, Claudiu T Supuran, Mohammed Arifuddin

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Article in Anti-cancer agents in medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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5 · Who and what money

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8 authors.

Priti SinghDepartment of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, 500 037, India.ORCID 0009-0004-5582-2316
Sridhar Goud NerellaDepartment of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, 500 037, India.
Baijayantimala SwainDepartment of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, 500 037, India.
Andrea AngeliNeurofarba Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.
Samreen KausarChemistry Section, School of Sciences, Maulana Azad National Urdu University (MANUU), Hyderabad 500032, Telangana, India.
Qasim UllahChemistry Section, School of Sciences, Maulana Azad National Urdu University (MANUU), Hyderabad 500032, Telangana, India.
Claudiu T SupuranNeurofarba Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.
Mohammed ArifuddinDepartment of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, 500 037, India.

Funding

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6 · The paper itself

Abstract

backgroundSulfonamide derivatives are well-reported hCA IX inhibitors; however, they inhibit all types of hCA without any selectivity, leading to severe adverse effects. Hence, developing a novel nonsulfonamide class of tumor-associated hCA IX inhibitors through non-classical inhibition may provide greater selectivity and better pharmacokinetics.

objectiveThe objective of this study was to develop non-sulfonamide derivatives as potential human carbonic anhydrase (hCA) inhibitors and develop a new series of chromene-linked bis-indole derivatives.

methodsWe synthesized and characterized the chromene-linked bis-indole derivatives and further evaluated them against four hCA isoforms, i.e., hCA I, hCA II, hCA IX, and hCA XII, and determined the ADMET parameters by the

resultsMost of the compounds showed significantly greater affinity and selectivity towards the tumorassociated hCA IX over other hCA isoforms within the lower micromolar to submicromolar range. In particular, the bromo-substituted bis-indole derivative 6t showed an excellent inhibition of hCA IX isoform with an affinity (

conclusionTherefore, the chromene-linked bis-indole derivatives can serve as a novel non-sulfonamide class of tumor-associated hCA IX inhibitors.

Indexed as

Antigens, NeoplasmAntineoplastic AgentsBenzopyransCarbonic Anhydrase InhibitorsCarbonic Anhydrase IXIndolesCarbonic AnhydrasesDose-Response Relationship, DrugHumansMolecular StructureStructure-Activity RelationshipAntigens, NeoplasmAntineoplastic AgentsBenzopyransCA9 protein, humanCarbonic Anhydrase InhibitorsCarbonic Anhydrase IXCarbonic AnhydrasesIndolesanticancer agents.bis-indoleChromenehCA IXhuman carbonic anhydrasenon-sulfonamide class

Identifiers

PMID39501943

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