Evidence map›Paper›PMID 39635932›Full record

ArticleChemical biology & drug design2024

Design and Development of Novel Hybrids Based on Pyrrolo[2,1-f][1,2,4]Triazine and 1-(Methylpiperidin-4-yl) Aniline-Based Analogs: Exploring the Utility as Anticancer Agents via MERTK Inhibition.

Balaji Dashrath Sathe, Shivani Jaiswal, Devendra Kumar, Thakur Gurjeet Singh, Nidhi Nainwal, Pramod Rawat, Savita Yadav, Bhupinder Kumar, Ashish Ranjan Dwivedi, S V Rathod

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Article in Chemical biology & drug design, 2024. 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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2 · The registry

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3 · Its place in the literature

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4 · The record

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5 · Who and what money

Authors and funding

10 authors.

Balaji Dashrath SatheDepartment of Chemistry, Bharatiya Vidya Bhavan College, Chowpatty, Mumbai University, Mumbai, India.
Shivani JaiswalInstitute of Pharmaceutical Research, GLA University, Mathura, India.
Devendra KumarSchool of Pharmacy, Narsee Monjee Institute of Management Studies (NMIMS), Dhule, Maharashtra, India.
Thakur Gurjeet SinghCentre for Research Impact & Outcome, Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab, India.
Nidhi NainwalUttaranchal Institute of Pharmaceutical Sciences, Uttaranchal University, Dehradun, Uttarakhand, India.
Pramod RawatDepartment of Biotechnology, Graphic Era (Deemed to Be University), Dehradun, India.
Savita YadavIES Institute of Pharmacy, IES University, Bhopal, Madhya Pradesh, India.
Bhupinder KumarDepartment of Pharmaceutical Sciences, Chauras Campus, HNB Garhwal University (A Central University), Srinagar, Uttarakhand, India.
Ashish Ranjan DwivediGITAM School of Pharmacy, GITAM (Deemed to Be) University, Hyderabad, India.ORCID 0000-0002-0918-6062
S V RathodDepartment of Chemistry, Bharatiya Vidya Bhavan College, Chowpatty, Mumbai University, Mumbai, India.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Mer-tyrosine kinase (MERTK), a member of the AXL, TYRO3, and MERTK (TAM) family, is one of the promising targets for cancer treatment. It plays a key role in cancer cell survival and proliferation and regulates immune responses in cancer. The study aimed to rationally design and develop molecules considering the pharmacophoric requirements of MERTK using a multi-synthetic approach followed by the hybridization of individual pharmacophores. A hybrid drug design approach was employed by hybridization of pyrrolo[2,1-f][1,2,4]triazine and 1-(methylpiperidin-4-yl)aniline pharmacophoric systems to develop novel leads (1K1-1K5). The molecules were synthesized via a multi-step synthetic approach. The synthesized molecules were assessed for their pharmacological potential via cell viability, drug metabolism and pharmacokinetics (DMPK), and MERTK inhibition studies corroborated by in silico studies. IK5 was found to have an IC

Indexed as

Aniline CompoundsAntineoplastic Agentsc-Mer Tyrosine KinaseDrug DesignMolecular Docking SimulationProtein Kinase InhibitorsTriazinesAnimalsCell Line, TumorCell ProliferationCell SurvivalDrug Screening Assays, AntitumorHumansMicrosomes, LiverPiperidinesPyrrolesAniline CompoundsAntineoplastic Agentsc-Mer Tyrosine KinaseMERTK protein, humanPiperidinesProtein Kinase InhibitorsPyrrolesTriazinesAnticancerMER tyrosine kinaseMetabolic studiesSulphonamidesTriazine

Identifiers

PMID39635932
PMCPMC11618975

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