Affiliation:
1. Neuropharmaceutical Research Laboratory, Dr. B.R. Ambedkar Centre For Biomedical Research (ACBR), Mall Road,
University of Delhi, Delhi 110007, India
Abstract
Abstract:
The carbazole skeleton, a key structural motif occurring naturally or chemically synthesized,
showed various biological activities. Molecular hybridization based on the combination of two
or more bioactive pharmacophores has been an important tool to convert the potent structural leads to
form new hybrid compounds with improved biological activity. In recent years, modifications/
substitutions of the carbazole motif at C-3, C-6, and N-9 positions have been carried to develop
novel carbazole-based potential anticancer agents in the therapy of cancer. In the last fifteen years,
several compounds based on carbazole core integrated into pharmacologically active molecular hybrid
having active pharmacophore such as1,3,4-thiadiazole, thiazole, guanidine, sulfonamides, glyoxamides,
imidazoles, phenanthrenes, rhodamines, chalcones, imidazopyridine, platinum, 2-H-chromen-
2-one, hydrazones, piperazines, isoxazole-thiadiazole, pyrazoles, etc. have been synthesized showing
anticancer profile at sub-micromolar to nano-molar concentrations. We have thoroughly reviewed the
design, progress, and development of C-3, C-6, and N-9 positions substituted carbazole derivatives
integrated with various medicinally active pharmacophore as potential anticancer agents evaluated
against various cancer cell lines. Additionally, the anticancer mechanism and in vivo activity of the
reported compounds have been discussed. This study will support in designing of new pharmacophore
that can be linked to the carbazole motif for the development of new, potent, and target-specific anticancer
drugs with improved pharmacokinetics and minimal side effects.
Funder
Department of Science and Technology
Council of Scientific and Industrial Research
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Pharmacology,General Medicine