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Novel Arginine-containing Macrocyclic MMP Inhibitors: Synthesis, ^99mTc-labeling, and Evaluation.

ABSTRACT: Matrix metalloproteinases (MMPs) are involved in tissue remodeling. Accordingly, MMP inhibitors and related radiolabeled analogs are important tools for MMP-targeted imaging and therapy in a number of diseases. Herein, we report design, synthesis, and evaluation of a new Arginine-containing macrocyclic hydroxamate analog, RYM, its hydrazinonicotinamide conjugate, RYM1 and ^99mTc-labeled analog ^99mTc-RYM1 for molecular imaging. RYM exhibited potent inhibition against a panel of recombinant human (rh) MMPs in vitro. RYM1 was efficiently labeled with ^99mTcO₄^- to give ^99mTc-RYM1 in a high radiochemical yield and high radiochemical purity. RYM1 and its decayed labeling product displayed similar inhibition potencies against rhMMP-1

SUBMITTER: Ye Y

PROVIDER: S-EPMC6076275 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature

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Dataset Information

Novel Arginine-containing Macrocyclic MMP Inhibitors: Synthesis, ^99mTc-labeling, and Evaluation.

OmicsDI is part of the ELIXIR infrastructure

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Dataset Information

Novel Arginine-containing Macrocyclic MMP Inhibitors: Synthesis, 99mTc-labeling, and Evaluation.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Novel Arginine-containing Macrocyclic MMP Inhibitors: Synthesis, ^99mTc-labeling, and Evaluation.