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

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

Volume: 15 Issue: 5

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

Affiliation:

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

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.

Cite this article as:

Mahajan A. Anand, Rane A. Rajesh, Amritkar A. Anish, Naphade S. Shital, Miniyar B. Pankaj, Bangalore Kumar Pavan and Karpoormath Rajshekhar, Synthesis of Novel Amides Based on Acridone Scaffold with Interesting Antineoplastic Activity, Anti-Cancer Agents in Medicinal Chemistry 2015; 15(5) . https://dx.doi.org/10.2174/1871520614666141130130130