Targeting cancer using scaffold-hopping approaches: illuminating SAR to improve drug design.

Abdul Rahaman, T A; Chaudhary, Sandeep

Abdul Rahaman, T A; Chaudhary, Sandeep.

Afiliación

Shivani; Laboratory of Bioactive Heterocycles and Catalysis (BHC lab), Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research-Raebareli (Transit Campus), Bijnor-Sisendi Road, Near CRPF Base Camp, Sarojini Nagar, Lucknow 226002, India.
Abdul Rahaman TA; Laboratory of Bioactive Heterocycles and Catalysis (BHC lab), Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research-Raebareli (Transit Campus), Bijnor-Sisendi Road, Near CRPF Base Camp, Sarojini Nagar, Lucknow 226002, India.
Chaudhary S; Laboratory of Bioactive Heterocycles and Catalysis (BHC lab), Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research-Raebareli (Transit Campus), Bijnor-Sisendi Road, Near CRPF Base Camp, Sarojini Nagar, Lucknow 226002, India. Electronic address: schaudhary.chy@niperraebareli.edu.in.

Drug Discov Today ; 29(9): 104115, 2024 Sep.

Article en En | MEDLINE | ID: mdl-39067613

ABSTRACT

ABSTRACT

Scaffold hopping is a design approach involving alterations to the core structure of an already bioactive scaffold to generate novel molecules to discover bioactive hit compounds with innovative core structures. Scaffold hopping enhances selectivity and potency while maintaining physicochemical, pharmacodynamic (PD), and pharmacokinetic (PK) properties, including toxicity parameters. Numerous molecules have been designed based on a scaffold-hopping strategy that showed potent inhibition activity against multiple targets for the diverse types of malignancy. In this review, we critically discuss recent applications of scaffold hopping along with essential components of medicinal chemistry, such as structure-activity relationship (SAR) profiles. Moreover, we shed light on the limitations and challenges associated with scaffold hopping-based anticancer drug discovery.

Asunto(s)

Antineoplásicos; Diseño de Fármacos; Neoplasias; Humanos; Diseño de Fármacos/métodos; Antineoplásicos/farmacología; Antineoplásicos/química; Relación Estructura-Actividad; Neoplasias/tratamiento farmacológico; Animales; Descubrimiento de Drogas/métodos; Química Farmacéutica/métodos

Palabras clave

SAR; anticancer drug discovery; cancer; medicinal chemistry aspects; scaffold hopping

Texto completo

Añadir a Mi BVS

Imprimir

XML

PubMed Links

Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Diseño de Fármacos / Neoplasias / Antineoplásicos Límite: Animals / Humans Idioma: En Revista: Drug Discov Today Asunto de la revista: FARMACOLOGIA / TERAPIA POR MEDICAMENTOS Año: 2024 Tipo del documento: Article País de afiliación: India Pais de publicación: Reino Unido

Texto completo

Añadir a Mi BVS

Imprimir

XML

PubMed Links

Buscar en Google