Scaffold hopping based designing of selective ALDH1A1 inhibitors to overcome cyclophosphamide resistance: synthesis and biological evaluation

Author:

Narendra Gera1,Raju Baddipadige1,Verma Himanshu1,Kumar Manoj1,Jain Subheet Kumar2,Tung Gurleen Kaur3,Thakur Shubham2,Kaur Rasdeep4,Kaur Satwinderjeet4,Sapra Bharti1,Silakari Om1ORCID

Affiliation:

1. Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab, 147002, India

2. Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, India

3. Centre for Basic and Translational Research in Health Sciences, Guru Nanak Dev University, Amritsar, India

4. Department of Botany and Environmental Sciences, Guru Nanak Dev University, Amritsar, India

Abstract

Bioisosteric replacement-based novel benzimidazole derivatives were designed, Synthesized, and evaluated. Combining these ALDH1A1 inhibitors with mafosfamide mitigated cyclophosphamide resistance in A549 and Mia PaCa-2 cell lines.

Funder

Indian Council of Medical Research

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

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