Synthesis of Novel Amides Based on Acridone Scaffold with Interesting Antineoplastic Activity

Author(s): Anand A. Mahajan, Rajesh A. Rane, Anish A. Amritkar, Shital S. Naphade, Pankaj B. Miniyar, Pavan Kumar Bangalore, Rajshekhar Karpoormath

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 15 , Issue 5 , 2015

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Graphical Abstract:


In search of novel cytotoxic agents based on acridone scaffold, twenty five derivatives of acridone-2- carboxamide were synthesized and evaluated against a panel of eleven cancer cell lines by using MTT assay. Amides, A5 and A8 (IC50 = 0.3 µM) exhibited good cytotoxicity against MCF7. Compound A22 (IC50 = 4.3 µM) was found to be selectively cytotoxic against cancer cell line MCF7 and KB403. Particularly, promising cytotoxic activities were shown by amides A6 (IC50 = 0.7 µM), A16 (IC50 = 6.3 µM), A8 (IC50 = 0.9 µM ), A21 (IC50 = 1.3 µM), A5 (IC50 = 2.9 µM), A8 (IC50 = 2.8 µM), A14 (IC50 = 0.8 µM), A9 (IC50 = 0.8 µM) and A8 (IC50 = 0.4 µM) against cell lines; PA1, WRL68, CaCO2, TK-10, K-562, PC-3, HOP-92, ECV-304 and UACC-257, respectively. The favorable cytotoxic profile and non-toxicity towards normal human cells displayed by the derivative revealed their potential for further anticancer drug developments.

Keywords: Acridone amides, anticancer, cytotoxicity, MTT assay, tricyclic compounds.

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Article Details

Year: 2015
Page: [555 - 564]
Pages: 10
DOI: 10.2174/1871520614666141130130130
Price: $65

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