The receptor tyrosine kinase c-Met was discovered in 1980s as translocated promoter region (TPR)-Met fusion oncogene and has high affinity to its naturally occurring ligand, hepatocyte growth factor (HGF). Binding of HGF to its receptor c-Met, initiates a wide range of cellular signaling, including those involved in proliferation, motility, migration and invasion. Importantly, dysregulated HGF/c-Met signaling is a driving factor for numerous malignancies and promotes tumor growth, invasion, dissemination and/or angiogenesis as well as resistance acquisition to some molecularly targeted therapies. Thus, c-Met kinase is regarded as an emerging anti-cancer target for the novel drug discovery. In the present study, 3D QSAR (CoMFA and CoMSIA), molecular docking and ADMET prediction studies were performed for the design of novel benzimidazole derivatives as c-Met kinase inhibitors and anti-cancer agents. A series of 1,5-disubstituted benzimidazole derivatives were synthesized and characterized by 1H-NMR, 13C-NMR, and Mass. HPLC analysis was carried out to evaluate the purity of compounds. The synthesized compounds were screened for in-vitro cell viability MTT assay against A549, HT-29 and MDA-MB-231 cell lines. Further, the synthesized compounds are under progress for the activity against c-Met kinase.

Discovery of novel benzimidazole derivatives as c-Met kinase inhibitors: Design, synthesis and biological evaluation

Macromolecular Chemistry: The Second Century

[Author Benefits](https://scimeetings.acs.org/?utm_source=pubs_content_marketing&utm_medium=website&utm_campaign=0320_MCF_NPI_Launch_Spring_Homepage&ref=pubs_content_marketing)

[How to use SciMeetings](https://storage.googleapis.com/dl.morressier.com/acs/SciMeetings-ACSSpring2020-HowToGuide_M3020-Final.pdf)

[Frequently Asked Questions](https://storage.googleapis.com/dl.morressier.com/acs/SciMtng_ACSNMSp2020_FAQ_M3120_Final.pdf)

ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.