ArticleMarine drugs2012
Preclinical evaluation of anticancer efficacy and pharmacological properties of FBA-TPQ, a novel synthetic makaluvamine analog.
Article in Marine drugs, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Exploring Marine Alkaloids: A Natural Approach to Cancer Treatment.Current pharmaceutical biotechnology · 2025Review
- Current Perspectives on Pyrroloiminoquinones: Distribution, Biosynthesis and Drug Discovery Potential.Molecules (Basel, Switzerland) · 2022Review
- Marine Alkaloids: Compounds with In Vivo Activity and Chemical Synthesis.Marine drugs · 2021Review
- Natural products targeting the p53-MDM2 pathway and mutant p53: Recent advances and implications in cancer medicine.Genes & diseases · 2018Review
- A formulation of pancreatic pro-enzymes provides potent anti-tumour efficacy: a pilot study focused on pancreatic and ovarian cancer.Scientific reports · 2017Article
- Another Look at Pyrroloiminoquinone Alkaloids-Perspectives on Their Therapeutic Potential from Known Structures and Semisynthetic Analogues.Marine drugs · 2017Article
- Development and validation of an HPLC-MS/MS analytical method for quantitative analysis of TCBA-TPQ, a novel anticancer makaluvamine analog, and application in a pharmacokinetic study in rats.Chinese journal of natural medicines · 2015Article
- Development and validation of a rapid HPLC method for quantitation of SP-141, a novel pyrido[b]indole anticancer agent, and an initial pharmacokinetic study in mice.Biomedical chromatography : BMC · 2015Article
- Anticancer properties of lamellarins.Marine drugs · 2015Review
- Identification of a new class of MDM2 inhibitor that inhibits growth of orthotopic pancreatic tumors in mice.Gastroenterology · 2014Article
- Total Synthesis of Calothrixins A and B via Oxidative Radical Reaction of Cyclohexenone with Aminophenanthridinedione.Tetrahedron · 2014Article
- Targeting MDM2-p53 interaction for cancer therapy: are we there yet?Current medicinal chemistry · 2014Review
- Identification of the ZAK-MKK4-JNK-TGFβ signaling pathway as a molecular target for novel synthetic iminoquinone anticancer compound BA-TPQ.Current cancer drug targets · 2013Article
- Total synthesis of zyzzyanones A-D.Tetrahedron · 2013Article
- Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
We have recently designed and synthesized a novel iminoquinone anticancer agent, 7-(4-fluorobenzylamino)-1,3,4,8-tetrahydropyrrolo[4,3,2-de]quinolin-8(1H)-one (FBA-TPQ) and initiated its preclinical development. Herein we investigated its efficacy, safety, and pharmacokinetics in in vitro and in vivo models of human pancreatic cancer. Our results demonstrated that FBA-TPQ inhibited pancreatic cancer cell growth, induced apoptosis, and caused cell cycle arrest in vitro. It inhibited the growth of xenograft tumors with minimal host toxicity. To facilitate future preclinical and clinical development of the agent, we also developed and validated a Rapid Resolution Liquid Chromatography (RRLC) method for quantitative analysis of FBA-TPQ in plasma and tissue samples. The method was found to be precise, accurate, and specific. Using this method, we carried out in vitro and in vivo evaluations of the pharmacological properties of FBA-TPQ, including stability in plasma, plasma protein binding, metabolism by S9 enzymes, plasma pharmacokinetics, and tissue distribution. Our results indicate that FBA-TPQ is a potential therapeutic agent for pancreatic cancer, providing a basis for future preclinical and clinical development.
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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.