ArticleJournal of medicinal chemistry2015
Synthesis and Structure-Activity Relationships of Tambjamines and B-Ring Functionalized Prodiginines as Potent Antimalarials.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Chemoselective halogenation of premarineosin A for next-generation antimalarial development.Organic & biomolecular chemistry · 2026Article
- Tambjamines as Promising Leads for the Development of Next-Generation Antifungals againstACS medicinal chemistry letters · 2026Article
- Metabolic engineering and late-stage functionalization expand the chemical space of the antimalarial premarineosin A.Communications chemistry · 2025Article
- Optimization of Prodiginines as Single-Dose Curative Antimalarials.Journal of medicinal chemistry · 2025Article
- Synthesis and Optical Properties of Unsymmetric Aromatically π-Extended BODIPY.The Journal of organic chemistry · 2025Article
- Functionalized in Triplicate: A Ring-By-Ring Approach to Tailored Prodiginine Derivatives for Site-Specific Conjugation Through Click Chemistry.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Optimization of Tambjamines Active against Multiple Stages of Malaria Parasites.Journal of medicinal chemistry · 2025Article
- Tambjamines as Fast-Acting Multistage Antimalarials.ACS infectious diseases · 2024Article
- Optimization of B-Ring-Functionalized Antimalarial Tambjamines and Prodiginines.Journal of medicinal chemistry · 2024Article
- Discovery and Optimization of Tambjamines as a Novel Class of Antileishmanial Agents.Journal of medicinal chemistry · 2024Article
- Anti-Microorganisms · 2023Review
- Isoalantolactone mediates the degradation of BCR-ABL protein in imatinib-resistant CML cells by down-regulating survivin.Cell cycle (Georgetown, Tex.) · 2023Article
- Synthesis and antitumour evaluation of indole-2-carboxamides against paediatric brain cancer cells.RSC medicinal chemistry · 2021Article
- Total Synthesis and Antimalarial Activity of 2-(Journal of medicinal chemistry · 2021Article
- Tambjamines and Prodiginines: Biocidal Activity againstPharmaceutics · 2021Article
- Metabolomics Reveals Minor Tambjamines in a Marine Invertebrate Food Chain.Journal of natural products · 2021Article
- Substrate Flexibility of the Flavin-Dependent Dihydropyrrole Oxidases PigB and HapB Involved in Antibiotic Prodigiosin Biosynthesis.Chembiochem : a European journal of chemical biology · 2020Article
- RedH and PigC Catalyze the Biosynthesis of Hybrubins via Phosphorylation of 4'-Methoxy-2,2'-Bipyrrole-5'-Carbaldehyde.Applied and environmental microbiology · 2020Article
- Novel Prodiginine Derivatives Demonstrate Bioactivities on Plants, Nematodes, and Fungi.Frontiers in plant science · 2020Article
- Isolation and characterization of tambjamine MYP1, a macrocyclic tambjamine analogue from marine bacteriumMedChemComm · 2019Article
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
Synthesis and antimalarial activity of 94 novel bipyrrole tambjamines (TAs) and a library of B-ring functionalized tripyrrole prodiginines (PGs) against a panel of Plasmodium falciparum strains are described. The activity and structure-activity relationships demonstrate that the ring-C of PGs can be replaced by an alkylamine, providing for TAs with retained/enhanced potency. Furthermore, ring-B of PGs/TAs can be substituted with short alkyl substitutions at either 4-position (replacement of OMe) or 3- and 4-positions without impacting potency. Eight representative TAs and two PGs have been evaluated for antimalarial activity against multidrug-resistant P. yoelii in mice in the dose range of 5-100 mg/kg × 4 days by oral administration. The KAR425 TA offered greater efficacy than previously observed for any PG, providing 100% protection to malaria-infected mice until day 28 at doses of 25 and 50 mg/kg × 4 days, and was also curative in this model in a single oral dose (80 mg/kg). This study presents the first account of antimalarial activity in tambjamines.
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