Anticancer Tetrahydrocarbazoles: A Wide Journey from 2000 till Date

LETTERS IN DRUG DESIGN & DISCOVERY(2024)

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摘要
Tetrahydrocarbazoles (THCz) are widespread in numerous indole alkaloids and have been reported since time for exhibiting profound pharmacological potential. Many pharmaceuticals drugs have tetrahydrocarbazole nucleus in their structure e.g. vinca alkaloids (Vincristine, Vinblastine, Vinorelbine), Frovatriptan, (R)-Ramatroban, Ondansetron, etc. that are used in various multifactorial diseases. In this review article, the anticancer potential of tetrahydrocarbazole based derivatives has been covered, enumerating their vast journey from the year 2000 to 2021. Since the last twenty-one years, tetrahydrocarbazoles have been a matter of focus among researchers worldwide, whereby several novel tetrahydrocarbazole derivatives have been synthesized and reported for their anticancer potential against various cancer cell lines. Tetrahydrocarabzole and its derivatives have exhibited profound anticancer potential mediated via various cancer pathways like apoptosis, cell cycle arrest, microtubule inhibition, Nrf2 Modulators, DNA intercalators, pERK and pRb phosphorylation, VEGF (Vascular Endothelial Growth Factor) and TNF-alpha inhibition, TPSO (translocator protein), Histone Deacetylase (HDAC) Inhibitors also discussed. The present review entails the synthesis, SAR studies, and anticancer mechanism of tetrahydrocarbazoles derivatives reported in review literature till date, and would provide a strong database to the medicinal chemist world over in discovering newer potential anticancer agent against various types of cancer diseases.
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关键词
Cancer,tetrahydrocarbazole (THCz),synthesis,SAR (structure activity relationship),anticancer,TPSO (translocator protein),TNF-alpha (Tumor necrosis factor alpha),histone deacetylase (HDAC) inhibitors,COX-2 (Cyclooxygenase enzyme-2) inhibitors,retinoblastoma protein (Rb),Nrf2:NF-E2-related factor 2,the extracellular-signal-regulated kinase (ERK)
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