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. Author manuscript; available in PMC: 2018 May 10.
Published in final edited form as: Prog Mol Biol Transl Sci. 2017 May 10;148:355–420. doi: 10.1016/bs.pmbts.2017.04.003

Table 1.

MMP inhibitors, their specificity to MMPs (Ki or IC50 <1 nM to 10 µM), and their effects in preclinical trials.

MMP Inhibitor Category,
Number, Chemistry,
Other Name
MMP Specificity, IC50 or Ki Preclinical Trial

<1 nM 1–10 nM 11–100 nM 0.1–1 µM 1–10 µM

1 ZBGs, Hydroxamic Acids Glioblastoma, breast, lung, ovarian, and prostate cancer
Succinyl Hydroxamate
Batimastat (BB-94) 1, 2, 8, 9 3
Marimastat (BB-2516) 1, 2, 9, 14 7
Ilomastat (GM6001, Galardin) 1, 2, 8, 9, 26 7, 12 3, 14

2 Sulfonamide Hydroxamate, AG3340, Prinomastat 2, 3, 9, 13, 14 1 7 Neovascularization, lung and prostate cancer, uveal melanoma, gliomas

3 Succinyl Hydroxamate 1

4 RS-104966 13 1

7 Sulfonamide Hydroxamate 2 8, 9, 14 1, 3 7 Decrease tumor invasion

8 Sulfonamide Hydroxamate 3 2 9 Chronic non-healing wounds

10 2, 3 1

12 3

5 Carboxylic Acids 13 3, 8 2 7, 9, 14 Osteoarthritis

6 11 3, 12 1, 9, 14 Chronic obstructive pulmonary disease

9 Sulfonylhydrazides 2, 9 1 7 3

16 Thiol- and Cyclic Mercaptosulfides 9 2 1, 7, 14 3

19 Aminomethyl Benzimidazoles 11 2, 9, 13

Phosphorous-Based
17 Sulfonamide Phosphonate 8 2 3

18 Sulfonamide Phosphonate 8 2, 9, 13, 14 1, 3 7 Liver disease, multiple sclerosis, breast cancer

20 Carbamoyl Phosphonate 2 Melanoma

21 Carbamoyl Phosphonate 2 Melanoma, prostate cancer

Nitrogen-Based
22 Oxazoline 11

23 Dionethiones and Pyrimidine-2,4,6 triones, Ro-28-2653 2, 14 8, 9 3 Anti-angiogenic and anti-invasive in tumor models

24 Dionethiones and Pyrimidine-2,4,6 triones 13 2, 9, 12 Osteoarthritis

Heterocyclic Bidentate Chelators
25 Terphenyl Backbone, AM-6 3

26 Biphenyl Backbone, 1,2 -HOPO-2 8, 12 2, 3 13 Cardiac ischemia /reperfusion injury

27 Diphenyl Ether Backbone 2, 9, 13 3 1 Brain edema following ischemia/reperfusion

28 Biphenyl Backbone, Pyrone-based 3, 9, 12 8 2, 13

29 Biphenyl Backbone, Hydroxypyridinone Derivative 8, 12

30 Biphenyl Backbone, AM-2 8, 12 −3 −2

31 Biphenyl Backbone 2, 8, 12, 13

34 Non-ZBGs 13 Osteoarthritis

35 12 2, 8, 13 3, 9

36 2, 8, 13

37 13 Osteoarthritis

38 Pyrimidine Dicarboxamide 13

39 Pyrimidine Dicarboxamide 13

Mechanism-Based
40 Diphenyl Ether Backbone, SB-3CT 2 9, 14 3 Inhibits liver metastasis in T-cell lymphoma and bone metastasis in prostate cancer

42 Diphenyl Ether Backbone, Thiol-Containing 2, 9 14 3

43 Diphenyl Ether Backbone 2 14 9 3

45 Diphenyl Ether Backbone 9 2 3, 14

For details and original references see.11,78,319,320