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Design, synthesis and antitumor activity of a novel PEG-A6-conjugated irinotecan derivative.

Abstract：

:A novel PEG-A6-conjugated irinotecan derivative 8 was designed and synthesized as antitumor agent by the PEGylation and A6-peptide modification of irinotecan. In vivo antitumor activity screening assay revealed that 8 exhibited better in vivo antiproliferation activity than irinotecan and its previous PEG-cRGD-conjugated derivative BGC0222 in MIA PaCa-2, NCI-H446, MDA-MB-231, HT-29 and NCI-N87 xenograft models, while the tumor of one in six mice in NCI-H446 assay and the tumors of two in six mice in MIA PaCa-2 assay completely subsided and disappeared within the 21-day period of 8-treatment, indicating that 8 should be a potential antitumor agent.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Huang YQ,Yuan JD,Ding HF,Song YS,Qian G,Wang JL,Ji M,Zhang Y

doi

10.1016/j.bmcl.2019.126847

subject

Has Abstract

pub_date

2020-01-15 00:00:00

pages

126847

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(19)30821-2

journal_volume

30

pub_type

杂志文章

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