2. Academic Validation
  3. Synthesis and Evaluation of the Tetracyclic Ring-System of Isocryptolepine and Regioiso-Mers for Antimalarial, Antiproliferative and Antimicrobial Activities

Synthesis and Evaluation of the Tetracyclic Ring-System of Isocryptolepine and Regioiso-Mers for Antimalarial, Antiproliferative and Antimicrobial Activities

  • Molecules. 2021 May 30;26(11):3268. doi: 10.3390/molecules26113268.
Katja S Håheim 1,  Emil Lindbäck 1,  Kah Ni Tan 2,  Marte Albrigtsen 3,  Ida T Urdal Helgeland 1,  Clémence Lauga 1,  Théodora Matringe 1,  Emily K Kennedy 2,  Jeanette H Andersen 3,  Vicky M Avery 2 4 5,  Magne O Sydnes 1
Affiliations

Affiliations

  • 1 Department of Chemistry, Bioscience and Environmental Engineering, University of Stavanger, NO-4036 Stavanger, Norway.
  • 2 Discovery Biology, Griffith Institute for Drug Discovery, Griffith University, Don Young Road, Nathan, QLD 4111, Australia.
  • 3 The Norwegian College of Fishery Science, Marbio, UiT-The Arctic University of Norway, Breivika, NO-9037 Tromsø, Norway.
  • 4 CRC for Cancer Therapeutics, Griffith University, Nathan, QLD 4111, Australia.
  • 5 School of Environment & Science, Nathan, Griffith University, Nathan, QLD 4111, Australia.
PMID: 34070798 DOI: 10.3390/molecules26113268
Abstract

A series of novel quinoline-based tetracyclic ring-systems were synthesized and evaluated in vitro for their antiplasmodial, antiproliferative and antimicrobial activities. The novel hydroiodide salts 10 and 21 showed the most promising antiplasmodial inhibition, with compound 10 displaying higher selectivity than the employed standards. The antiproliferative assay revealed novel pyridophenanthridine 4b to be significantly more active against human prostate Cancer (IC50 = 24 nM) than Puromycin (IC50 = 270 nM) and Doxorubicin (IC50 = 830 nM), which are used for clinical treatment. Pyridocarbazoles 9 was also moderately effective against all the employed Cancer cell lines and moreover showed excellent biofilm inhibition (9a: MBIC = 100 µM; 9b: MBIC = 100 µM).

Keywords

antimicrobial activity; antiplasmodial activity; antiproliferative activity; biofilm inhibition; indoloquinoline.

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