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Article

Replacing the terminal piperidine in ceritinib with aliphatic amines confers activities against crizotinib-resistant mutants including G1202R.

European journal of medicinal chemistry - 27 Jan 2017

Mathi Gangadhar Rao, Kang Chung Hyo, Lee Heung Kyoung, Achary Raghavendra, Lee Ha-Yeon, Lee Joo-Youn, Ha Jae Du, Ahn Sunjoo, Park Chi Hoon, Lee Chong Ock, Hwang Jong Yeon, Yun Chang-Soo, Jung Hee Jung, Cho Sung Yun, Kim Hyoung Rae, Kim Pilho

Abstract excerpt

The piperidine fragment in ceritinib was replaced with diverse aliphatic amines to improve inherent resistance issues of ceritinib. While most of the prepared compounds exhibit as similar in vitro activities as ceritinib, compound 10 shows encouraging activities against wild-type ALK as well as crizotinib-resistant mutants including extremely resistant G1202R mutant with an IC50 of 1.8 nM. Furthermore,...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Source

Identifiers

PMID: 27915169
DOI: 10.1016/j.ejmech.2016.11.046

Genes

ALK

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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Replacing the terminal piperidine in ceritinib with aliphatic amines confers activities against crizotinib-resistant mutants including G1202R.PMID 27915169Read ↗

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