ArticleBioorganic & medicinal chemistry letters2010
Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.
Article in Bioorganic & medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 43 citations in OpenAlex.
- Cathepsin L as a Driver of Tumour Invasion and a Novel Therapeutic Target in Ovarian Cancer.Cancers · 2026Review
- A Review of Small Molecule Inhibitors and Functional Probes of Human Cathepsin L.Molecules (Basel, Switzerland) · 2020Review
- Hydrazone Derivatives Enhance Antileishmanial Activity of Thiochroman-4-ones.Molecules (Basel, Switzerland) · 2017Article
- Cathepsin L inactivation leads to multimodal inhibition of prostate cancer cell dissemination in a preclinical bone metastasis model.International journal of cancer · 2016Article
- Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.Bioorganic & medicinal chemistry · 2015Article
- Cathepsin L targeting in cancer treatment.Pharmacology & therapeutics · 2015Review
- G2/M Cell Cycle Arrest and Tumor Selective Apoptosis of Acute Leukemia Cells by a Promising Benzophenone Thiosemicarbazone Compound.PloS one · 2015Article
- Cathepsin L inhibition by the small molecule KGP94 suppresses tumor microenvironment enhanced metastasis associated cell functions of prostate and breast cancer cells.Clinical & experimental metastasis · 2013Article
- Mechanistic insights into mode of action of novel natural cathepsin L inhibitors.BMC genomics · 2013Article
- Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L.ACS medicinal chemistry letters · 2012Article
Corrections and comments
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A small library of 36 functionalized benzophenone thiosemicarbazone analogs has been prepared by chemical synthesis and evaluated for their ability to inhibit the cysteine proteases cathepsin L and cathepsin B. Inhibitors of cathepsins L and B have the potential to limit or arrest cancer metastasis. The six most active inhibitors of cathepsin L (IC50<85 nM) in this series incorporate a meta-bromo substituent in one aryl ring along with a variety of functional groups in the second aryl ring. These six analogs are selective for their inhibition of cathepsin L versus cathepsin B (IC50>10,000 nM). The most active analog in the series, 3-bromophenyl-2'-fluorophenyl thiosemicarbazone 1, also efficiently inhibits cell invasion of the DU-145 human prostate cancer cell line.
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