1. Synthesis, characterization and antitumor activity of 2-methyl-9-substituted acridines
- Author
-
Rajesh Kumar, Ankita Sharma, Sarita Sharma, Om Silakari, Mandeep Singh, and Manmeet Kaur
- Subjects
2-Methylacridine ,Aromatic amines ,Antiproliferative activity ,Cyclization ,Intercalation ,Chemistry ,QD1-999 - Abstract
In the field of antitumor DNA-intercalating agents, 9-anilinoacridines play an important role due to their antiproliferative properties. Several cancer chemotherapeutics such as amascrine and nitracrine have been developed as anticancer agents. In the present study, several 2-methyl-9 substituted (AS 0–8) acridines were synthesized by nucleophilic substitution of 2-methyl-9-chloroacridine (AS) with aromatic amines. The structures of novel compounds were determined using spectroscopic methods. Three compounds were evaluated for antiproliferative activity against A-549 (Human, small cell lung carcinoma) and MCF-7 (Human, breast cancer) cell lines using the MTT assay. Compound AS-2 showed higher in vitro cytotoxic activity against A-549 and MCF-7 cancer cell lines with CTC50 187.5 and 212.5 μg/ml respectively. The cancer cell cytotoxicity of acridines against A-549 cell line was found to be more active than MCF-7 cell line.
- Published
- 2017
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