Exploring pyrazoline-thiophene hybrids as CDK2 inhibitors: synthesis, mechanism, biological studies, and computational insights

Abosalim, Heba M.; Elmoselhy, Tarek; Sharafeldin, Nabaweya; Nafie, Mohamed S.; Diab, Mohamed K.; El‐Hamamsy, Mervat H.; Tawfik, Haytham O.

doi:10.1039/d5md00910c

articleRSC Medicinal ChemistryJan 1, 2026GREEN OA

Exploring pyrazoline-thiophene hybrids as CDK2 inhibitors: synthesis, mechanism, biological studies, and computational insights

HMHeba M. Abosalim TETarek Elmoselhy NSNabaweya Sharafeldin MSMohamed S. Nafie MKMohamed K. Diab

Tanta University · Suez Canal University · +2 more institutions

PubMed

Indexed incrossrefpubmed

Abstract

Novel pyrazoline-linked thiophenes were synthesized as anticancer agents. Lead compound 4p showed sub-micromolar cytotoxicity, induced CDK2-mediated apoptosis and cell-cycle arrest, and reduced tumor burden in vivo with low toxicity.

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Topics & keywords

Topics

Keywords

Downregulation and upregulation
Cytotoxicity
Apoptosis
Cyclin-dependent kinase 2
Potency
Docking (animal)
Cancer
Structure–activity relationship

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