4.4 Review

Carbazole Scaffold in Medicinal Chemistry and Natural Products: A Review from 2010-2015

Journal

CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 16, Issue 11, Pages 1290-1313

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026615666150915112647

Keywords

Biological activity; Carbazole; Natural product; SAR; Scaffold; Small molecule

Funding

  1. National Institutes of Health [R15AI092315, P20GM103466]
  2. NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES [R15AI092315] Funding Source: NIH RePORTER
  3. NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [P20GM103466] Funding Source: NIH RePORTER

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9H-carbazole is an aromatic molecule that is tricyclic in nature, with two benzene rings fused onto a 5-membered pyrrole ring. Obtained from natural sources or by synthetic routes, this scaffold has gained much interest due to its wide range of biological activity upon modifications, including antibacterial, antimalarial, anticancer, and anti-Alzheimer properties. This review reports a survey of the literature on carbazole-containing molecules and their medicinal activities from 2010 through 2015. In particular, we focus on their in vitro and in vivo activities and summarize structure-activity relationships (SAR), mechanisms of action, and/or cytotoxicity/selectivity findings when available to provide future guidance for the development of clinically useful agents from this template.

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