ArticleCurrent medicinal chemistry2016
Derivatives of Procaspase-Activating Compound 1 (PAC-1) and their Anticancer Activities.
Article in Current medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT02355535 (), which is not on this map. Cited by 20 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
(STM-03) Phase I Study of Procaspase Activating Compound-1 (PAC-1) in the Treatment of Advanced Malignancies - Component 1
Who cites it
20 citing papers in PubMed.
- A clinical-stage oncology compound selectively targets drug-resistant cancers.bioRxiv : the preprint server for biology · 2026Article
- Phase I clinical trial of a novel procaspase-3 activator SM-1 with temozolomide in recurrent high-grade gliomas.Neoplasia (New York, N.Y.) · 2025Article
- Recent Development in Hydantoins, Thiohydantoins, and Selenohydantoins as Anticancer Agents: Structure-activity Relationship and Design Strategies.Mini reviews in medicinal chemistry · 2025Review
- Novel Bis-1,2,3-triazole-thiazolidinone hybrid as anticancer agents that induce apoptosis and molecular modeling study.Future medicinal chemistry · 2024Article
- Thiazolidinone-linked-1,2,3-triazoles with (R)-Carvone as new potential anticancer agents.Future medicinal chemistry · 2024Article
- Inferring circRNA-drug sensitivity associations via dual hierarchical attention networks and multiple kernel fusion.BMC genomics · 2023Article
- Optical Modulation of Antibiotic Resistance by Photoswitchable Cystobactamids.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Predicting circRNA-drug sensitivity associations via graph attention auto-encoder.BMC bioinformatics · 2022Article
- Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents.Scientific reports · 2022Article
- Design, synthesis, and evaluation of novelJournal of enzyme inhibition and medicinal chemistry · 2020Article
- Design, synthesis, cytotoxic activity, and apoptosis inducing effects of 4- and N-substituted benzoyltaurinamide derivatives.Turkish journal of chemistry · 2020Article
- (E)-N'-Arylidene-2-(4-oxoquinazolin-4(3H)-yl) acetohydrazides: Synthesis and evaluation of antitumor cytotoxicity and caspase activation activity.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Procaspase-3 Overexpression in Cancer: A Paradoxical Observation with Therapeutic Potential.ACS chemical biology · 2019Review
- Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials.Science translational medicine · 2019Article
- Synthesis and Antiproliferative Activity of New Cyclodiprenyl Phenols against Select Cancer Cell Lines.Molecules (Basel, Switzerland) · 2018Article
- Overcoming Resistance to Targeted Anticancer Therapies through Small-Molecule-Mediated MEK Degradation.Cell chemical biology · 2018Article
- Article
- Developing drugs targeting transition metal homeostasis.Current opinion in chemical biology · 2017Review
- Small-Molecule Procaspase-3 Activation Sensitizes Cancer to Treatment with Diverse Chemotherapeutics.ACS central science · 2016Article
- The Combination of Vemurafenib and Procaspase-3 Activation Is Synergistic in Mutant BRAF Melanomas.Molecular cancer therapeutics · 2016Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors.
Funding
Abstract
PAC-1 induces the activation of procaspase-3 in vitro and in cell culture by chelation of inhibitory labile zinc ions via its ortho-hydroxy-N-acylhydrazone moiety. First reported in 2006, PAC-1 has shown promise in cell culture and animal models of cancer, and a Phase I clinical trial in cancer patients began in March 2015 (NCT02355535). Because of the considerable interest in this compound and a well-defined structure-activity relationship, over 1000 PAC-1 derivatives have been synthesized in an effort to vary pharmacological properties such as potency and pharmacokinetics. This article provides a comprehensive examination of all PAC-1 derivatives reported to date. A survey of PAC-1 derivative libraries is provided, with an indepth discussion of four derivatives on which extensive studies have been performed.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.